TW513422B - Bicycloamino derivative and PGD2 antagonist containing the derivative - Google Patents

Bicycloamino derivative and PGD2 antagonist containing the derivative Download PDF

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TW513422B
TW513422B TW085107425A TW85107425A TW513422B TW 513422 B TW513422 B TW 513422B TW 085107425 A TW085107425 A TW 085107425A TW 85107425 A TW85107425 A TW 85107425A TW 513422 B TW513422 B TW 513422B
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Mitsuaki Ohtani
Akinori Arimura
Tatsuo Tsuri
Junji Kishino
Tsunetoshi Honma
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Shionogi & Amp Co Ltd
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13422 經濟部中央標準局員工消費合作社印製 A7 R7 五、發明説明(1 ) 本發明係有關一種雙環環条胺基衍生物及含有該衍生 物之前列腺素Ds (M下稱PGDS)拮抗劑。 關於本發明之雙環環条胺基衍生物之一部分者已知可 用來作為凝血檄素Aa (TXA2)拮抗劑(特公平5-79060號說 明書)。但,關於記載於特公平5-79060號之化合物並均 不過僅揭示用來作為TXAS拮抗劑之有用性而已,對於本發 明揭寒之P G D 2拮抗劑的用途絲毫未暗示。 亦即,TXAat作用已知有血小板凝集作用、血栓形成 作用等,但,TXA2拮抗劑被認爲可對ΤΧΑ2·行拮抗,可用 來作為抗血栓劑、心肌梗塞、哮喘之治療劑。 另外,本發明之PGDB拮抗劑可用於改善起因於PGD2t 生產過多之症狀,更詳而言之,可用來作為肥胖細胞功能 不全相關之疾病,例如,全身性肥胖細胞症及全身性肥胖 細胞活性化障礙的治療劑、進而係抗氣管收縮劑、抗哮喘 劑、抗過敏性鼻炎劑、抗過敏性結膜炎劑、抗尊麻疹劑、 缺血再灌流傷害治療藥、抗炎症劑。 從上述明顯可知,1%纟2拮抗劑與卩6卩8拮抗劑之作用點 、機序均不同,同時適應亦相異,係完全不同性質者,故 某化合物同時具有此等作用者乃完全無法預測。 PGDa係從肥胖細胞產生游離之最主要的類前列腺素, 以及藉著一受免疫學或非免疫學上剌激而活性化之加環氧 酸(cyclooxygenase),而從花生四烯酸經PGG2、PGHa所產 生者。PGD2具有各種強力生理的、疾病的作用,例如,引 起很強氣管收縮,進而造成支氣管哮喘的疾病,Μ及於全 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 5 $·------、訂-------^^^1 (請先閲讀背面之注意事項再填.舄本頁) 513422 舊土 Λ7 本?, ”月曰1 Τ: 、 ZlL PF --- irr-2~^--] 身性過敏狀態中,使末梢血管擴張,而形成過敏性衝擊之 原因。特別是,M PGDa作為過敏性鼻炎之鼻塞症狀顯現的 原因物質之一的想法,乃倍受注意。因此,以減輕鼻塞症 狀作為目的之藥物曾被想到PGDa2生合成阻礙劑、或受容 體拮抗劑的開發。但,PGD2t生合成阻礙劑因有可能對在 其他活體內之前列腺素類的合成造成很大的影響,故希望 能開發出對於PGD2受容膿非常卓越的PGDa受容體拮抗劑( 遮蔽藥)。 本發明人等為開發對PGD2受容髏非常卓越的PGDa受容 體拮抗劑(遮蔽藥),經銳意硏究之結果,發現Μ下述通 式(I )所示之化合物或其鹽作為PGD2受容體拮抗劑具有很 強的作用,且,為化學性、生化性上安定的化合物,終完 成本發明。 亦即,本發明係提供一種PGD2拮抗劑組成物,其係含 有一K式(I ) (請先閱讀背面之注意事項再填寫本頁)
經濟部中央標準局員工消費合作社印製 所示之雙環之環条胺基衍生物或其鹽亦或水合物作為 有效成分者;(上述式中, α 表示 6 本紙張尺度適用中國國家標準(CNS ) Α4規格(210Χ29?公釐)
經濟部中央標準局員工消費合作社印製 CX ¢( ¢( $ Cx, A亦可介於雜原子或亞苯基,亦可具有氧基,及/或 亦可具有不飽和鍵之院撐基; B為氫、烷基、芳烷基或醸基; R為 COORi、CH2ORs或C0N(Rs)R4;
Ri爲氫或烷基; fU為氫或烷基; R3及IU分別為氫、烷基、羥基或烷基磺酿基;
Xi為單鍵、亞苯基、亞禁基、噻盼二基、B5I跺二基或 噁睡二基; χ2^單鍵、-N = N-、-N = CH-、-CH = N-、-CH = N-N-、 -CH = N-0-、-ONNHCSNH、-C = NNHC0NH-、-CH = CH_、-CH(OH)-、-C(C1)=C(C1)-、-(CHa)n-、乙炔基、 -N(RB)-、 -N(Rei)C0-、-N(Re2)S02-、 -N(Re3)C0N(Re4)-、-C0N(Ree)-、_S〇2N(Re6)--S-、-SO-、-SOr 、-C0-、噁嗪唑二基、_嗪唑二基或四唑二基; X3為烷基、烯基、炔基、芳基、芳烷基、雜環、環烷 基、環烯基、噻唑啉亞基甲基、噻唑烷亞基甲基、-CH = NRs 或-N = C(R77Re ;
Re、Rei、Rea、Rb3、Re·*、Rea 及 Res 為氮或院基; IU為氫、烷基、羥基、烷氧基、氨甲酿基氧基、硫氨 甲醯基氧基、脲基、硫脲基; 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) ---------^0,-----’訂 ------^0— (請先閱讀背面之注意事項再填寫本頁) >13422 Λ7 B7 五、發明説明( 只7及1^分別為烷基、烷氧基或芳基; η為1或2 ; Ζ為-S03-或-C0-; 姐為0或1 ; 於此等定義中,取代基為環狀者亦可被選自硝基、焼 氧基、氨磺醯基、取代或非取代胺基、醯基、醯氧基、經 基、鹵素、烷基、炔基、羧基、烷氧基羰基、芳烷氧基锻 基、芳氧基羰基、甲磺醯氧、氟基、烯氧基、羥烷基、三 氟甲基、烷硫基、-N = PPh3、氧基、硫基、羥亞胺基、烷 氧基亞胺基、苯基及烷撐二氧基中之1〜3艏基所取代) 0 用以奮施發明:> 慕住形能 若進一步具體表示能成為上述PGDS拮抗劑的化合物, 可舉出於式(I)所示之化合物中, 乃表示 經濟部中央榡準局員工消費合作社印製 α m爲0、Ζ為S〇2時,Xi及Χ2均爲單鍵,Χ3為烷基、苯基 、萘基、苯乙烯基、喹啉基或噻盼甲基,於此等取代基之 中,環狀者亦可被選自硝基、烷氧基、取代或非取代胺基 、鹵素、烷基及羥基烷基中之1〜3個基所取代的化合物 或其鹽亦或水和物。 本紙張尺度適用中國國家標準(CNS ) A4規格(21〇X29*7公釐) 8
_ Q --------------IT--------0Φ— (請先閱讀背面之注意事項再填寫本頁) 513422 A7 B7 五、發明説明(5 ) 同樣地,於Μ式(I )所示的雙環之環条胺基衍生物中 ,舉例 ! 乃表示
(請先閲讀背面之注意事項 經濟部中央標準局員工消費合作社印製 DI為1時,Xi及Xa均爲單鍵,Χ3爲亦可被鹵素所取代之 苯基的雙環之環条胺基衍生物或其鹽亦或水和物。 同樣地,於以式(I )所示的雙環之環条胺基衍生物中 ,舉例 Q 乃表示 α % m為1時,X為苯基,Xa為-CHa-或-Ν = Ν-,Χ3為苯基的 雙環之環条胺基衍生物或其鹽或水和物。 同樣地,一種Μ式(I )所示的雙環之環条胺基衍生物 或其鹽或水和物,係Μ式(la)所示,
NIB X1-02 (式中,A、B、R、Xi、乂2及\3乃與前述之定義相同 本紙張尺度適用中國國家標準(CNS ) Α4規格(210Χ 297公釐)
本頁)
、1T 9 513422 B7
A—R
五、發明説明( 但,⑴Xi及χ2為單鍵、χ3為取代或非取代苯基或萘基 、及⑵Α為5-庚亞烯基、R為cOORid爲氫或甲基)、 1,4-亞苯基、X2^單鍵、χ3為苯基時除外)。 同樣地,一種Μ式(I )所示的雙環之環条胺基衍生物 或其鹽或水和物,係Μ式(I b), (lb) co—x 广 x2 · (式中,
Q 係表示 (請先閱讀背面之注意事項再填寫本頁)
‘-VT
或 €ί 經濟部中央榡準局員Η消費合作衽印製 A、B、R、Xi、乂2及乂3乃與前述之定義相同Μ旦,Xi 及X«為單鍵,X3為苯基時及Xi為單鍵、Xa^-0-時,X3為 苯甲基時除外)所示。 進而更具體地,於Μ式(la)所示之化合物中,可舉 例如Xi及X2^單鍵,X3為異噁唑基、__唑基、異噻唑基 、嗎啉基、H5I哚基、苯并呋喃基、二苯并呋喃基、二苯 并二氧基、苯并_盼甲基、二苯并_盼甲基、唑基、氧 雜蒽基、酚三嗪基、二苯并噁吡基、二苯并_吡基、 二氮雜萘基、氧萘基、苯并眯唑基或二氫苯并_吡基之 本紙張尺度適用中國國家標準(CNS ) Α4規格(210Χ297公釐) 10 513422 Α7 Β7 i、發明説明(7 ) 化合物或其鹽或水和物。 同樣地,於Μ式(la)所示之化合物中,可舉例如X* 為單鍵、X»為亞苯基、\3為烷炔基、烷烯基、-CH = NRe或 - N = C(R7)Re之化合物或其鹽或水和物。 同樣地,於Μ式(I a)所示之化合物中,可舉例如R表 示COOR,Xi表示亞苯基或噻盼二基,Xa表示單鍵、-N = N -、-CH = CH_、-CONH-、-NHCO-或亞乙烯基,X3表示苯基、 睡唑烷基甲基、噻唑嗪烷基甲基或睡吩甲基之化合物其鹽 或水和物。 更具體而言,於Μ式(I b>所示之化合物中,可舉例 如 乃表示 α 之化合物或其顗或水和物。進而更佳之態樣係於Μ式(lb )所示之化合物中,可舉例如R乃表COORi (h之定義同於 前述)之化合物或其鹽或水和物。 同樣地,於以式(I b)所示之化合物中,可舉例如 Xi為亞苯基或唾盼二基,Xa^單鍵、-N = N-、-CH = CH- , 1, 2-亞乙烯基、-0_、_S_、-C0_、-C0N(Rae)- (Rae 之定義 同於前述)、-N(Rei)C0- (Rai之定義同於前述)及X3為 苯基之化合物或其鹽或水和物。 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) (請先閱讀背面之注意事項再IP本頁) 、τ 經濟部中央標準局員工消費合作社印製 11 513422 A7 B7 經濟部中央標準局員工消費合作社印製 五、發明説明(8 ) 更具體而g,於以式(I b〉所示之化合物中,可舉例 如Q' 乃表示 之化合物或其鹽或水和物。進而較佳之態樣可舉例如B為 氫,Xi及Xa均為單鍵,X3為睡吩甲基、睡唑基、唾嗪唑基 、異睡唑基、Ift咯基、吡啶基、苯并呋喃基、苯并眯唑基 、苯并睡吩甲基、二苯并呋喃基、二苯并睡吩甲基、喹啉 基或蚓跺基之化合物或其鹽。同樣地,可舉例如Xt為亞苯 基、噻盼二基、8¾哚二基或畷唑二基、乂2為單鍵、-N = N-、-CH = CH-、1,2-亞乙烯基、-S-、或-0-、及X3為芳基或 雜環之化合物或其鹽或水和物。 又,上述通式(la)及(Ib>所示之化合物係本發明人 等所合成出的新穎化合物。 本說明書中所使用之各種語句的定義如以下般。「烷 撐基」乃指G〜C3之直鍵或分枝狀的烷撐基,例如亞甲基 、甲基亞甲基、二甲基亞甲基、甲乙基亞甲基、乙烯、三 亞甲烯、四亞甲基、五亞甲基、六亞甲基、七亞甲基、八 亞甲基或九亞甲基等。上述烷撐基亦可介在雜原子(氧原 子、硫原子或氮原子等)或亞苯基(例如1,4-亞苯基、 1,3-亞苯基、1,2-亞苯基等),亦可具有氧代基、及/或 (請先閱讀背面之注意事項再本頁)
訂 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 12 513422 經濟部中央標準局員工消費合作社印製 A7 B7 五、發明説明(9 ) 於鍵上任意位置亦可含有雙鍵或三鍵1値或1値以上。例 如:一(CHa>a-〇-CHa-、 _(CHa)a-〇-(CH2)a-、-(CHa)a-0-(CHa)3-、-(CH山-0_(CH 山-、-(CH山-〇-(CHa)e-、 -(CHa)a-0-(CHa)s-、-(CHa)a-S-(CHa)a-、-(CHa)3-S-(CHa〉a-、-CHa-S - CHa-、-CHa-S-(CHa)r、- CHa-N(CH3> -CHa_' -CHa-NH -(CH山-、-(CHa〉a-N(CHaCH3)-(CH2)3-、 -(CHa)a-1,4-亞苯基- CHa -、-(CHaia-O-lJ-亞苯基 - 、-(CHa)a-0-1,2-亞苯基-CHa-、-(CHa〉a-0-l,4-亞苯基-CHa-、-CH = CH-S-CHa-l,4-亞苯基-CHa-、_CH = CH-S-1,3-亞苯基-(CHa〉a-、2-氧代丙烯基、3-氧代戊烯基、5-氧代 己烯基、亞乙烯基1-亞丙烯基、2-亞丙烯基、卜亞丁烯基 、2-亞丁烯基、3-亞丁烯基、1,2-亞丁二烯基、1,3-亞丁 二烯基、卜亞戊烯基2-亞戊烯基、3-亞戊烯基、4-亞戊燦 基、1,2-亞戊二烯基、1,3_亞戊二烯基、1,4-亞戊二烯基 、2,3-亞戊二烯基、2,4_亞戊二烯基、卜亞己烯基、2一亞 己烯基、3-亞己烯基、4-亞己烯基、5-亞己烯基、1,2-亞 己二烯基、1,3-亞己二烯基、1,4-亞己二烯基、1,5_亞己 二烯基、2,3-亞己二烯基、2,4-亞己二烯基、2,5-亞己二 烯基、3,4-亞己二烯基、3,5_亞己二烯基、4,5-亞己二嫌 基、1,1_二甲基-4-亞己烯基、1-亞庚烯基、2_亞庚嫌基 、3-亞庚烯基、4-亞庚烯基、5-亞庚烯基、2,2-二甲基-5 -亞庚烯基、6-亞庚烯基、1,2-亞庚二烯基、1,3-亞庚一 烯基、1,4-亞庚二烯基、1,5-亞庚二烯基、1,6_亞庚二嫌 基、2,3-亞庚二烯基、2,4-亞庚二烯基、2,5-亞庚二嫌基 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 13 (請先閱讀背面之注意事項本頁) ,τ 513422
Α7 Β7 五、發明説明(10 ) 經濟部中央標準局員工消費合作社印製 2,6-亞庚二烯基、3,4-亞庚二烯基、3,5-亞庚二烯基、3, 6-亞庚二烯基、4,5_亞庚二烯基、4,6-亞庚二烯基、或5, 6-亞庚二烯基、1-亞丙炔基、3-亞丁炔基、2-亞戊炔基、 5-亞己炔基、6-亞庚炔基、-(CHe)-CH = CH-〇-(CH2)a、 -(:1-5-((:112)3-、-(:112-順位-(:1^(:[1-1,2-亞苯基_(:1^-、 -CH = CH-1,4_亞苯基-(CHa)a-、-4-氧代-4, 5-亞己烯基等 〇 「烷基」乃意指匕〜CaD之直鍵狀或分枝狀的烷基, 例如甲基、乙基、正丙基、異丙基、正丁基、異丁基、第 二丁基、第三丁基、正戊基、異戊基、新戊基、第三戊基 、己基、庚基、辛基、壬基、癸基、十一烷基、十二烷基 、十三烷基、十四烷基、十五烷基、十六烷基、十七烷基 、十八烷基、十九烷基、二十烷基等。 「芳基」乃意指Ce〜Ci 4之單環或縮合環,例如苯基 、萘基(例如卜萘基、2-萘基)、蒽基(例如1-M基、2 -蒽基、9-蒽基)、菲基(例如2-菲基、3-菲基、9-菲基) 、笏基(例如2-笏基)等。尤其Μ苯基爲佳。 「芳烷基」乃指前述芳基取代於前述烷基者,此等係 能於可置換之全部位置進行結合。例如,苯甲基、苯乙基 、苯丙基(例如3-苯丙基)、萘甲基(例如α-萘甲基)、 葸甲基(例如9-蒽甲基)、菲甲基(例如3-菲甲基)等。 「醯基」乃意指源自脂肪族羧酸之(^〜(:3的醯綦,例 如甲酿、乙酿、丙酿、丁酿、戊酿等。 「烷基磺酿基」乃指上述烷基於磺醯基上進行取代者 本紙張尺度適用中國國家標準(CNS ) A4規格(210 X 297公釐) (請先閲讀背面之注意事項r -裝-- Τ本頁) 訂 線 14 513422 A 7 B7 經濟部中央標準局員工消費合作社印製 五、發明説明(11 ) ,例如甲磺醯基、乙磺酿基、丙磺醯基等。 「烷烯基」乃指於上述烷基上具有1値或1値Μ上之 雙鍵的直鏈或分枝狀的Ca〜caa烷烯;例如乙烯基、1-丙 烯基、2-丙烯基、卜丁烯基、2-丁烯基、3-丁烯基、1,2-丁二烯基、卜戊烯基、1,2-戊二烯基、2-己烯基、1,2-己 二烯基、3-庚烯基、1,5-庚二烯基等。 「烷炔基」乃指於上述烷基上具有1個或1値Μ上之 三鍵的直鐽或分枝狀的Ca〜CaD烷炔基,例如,乙炔基、1 -丙炔基、2-丙炔基、1-丁炔基、2-丁炔基、3-丁炔基等 Ο 「雜環」乃指於環内含有1値Μ上任意選自氧原子、 硫原子及/或気原子,且,亦可與磺環或其他雜環進行縮 合之5〜7員環,此等能夠於可置換的位意位置進行結合 。例如,Bit咯基(例如Ι-Blt咯基、3-吡咯基)、蚓跺基( 例如2-蚓哚基、3-蚓哚基、6-蚓跺基 >、咔唑基(例如2-咔唑基、3_咔唑基)、眯唑基(例如卜眯唑基、4-眯唑基 )、吡唑基(例如1-吡唑基、3-吡唑基)、苯并眯唑基( 例如2-苯并眯唑基、5-苯并眯唑基)、||?|跺基(例如3-蚓 哚基 >、蚓跺烷基(例如6-Βζ!跺烷基)、吡啶基(例如2-吡啶基、3-吡啶基、4-吡啶基)、喹啉基(例如8-喹啉基 )、異喹啉基(例如3-異喹啉基)、β丫啶基(例如卜吖啶 基)、菲啶基(例如2-菲啶基、3-菲啶基)、<瞎基(例 如3-述8秦基)、Bit咯烷基(例如4_吡咯烷基)、吡嗪基( 例如2_吡嗪基)、二氮雜萘基(例如3 —二気雜萘基)、酞 (請先閱讀背面之注意事項丈 -裝-- 乘馬本頁)
、1T -線 本紙張尺度適用中國國家標準(CNS ) Α4規格(210X297公釐) 15 513422 A7 B7 i、發明説明(12 ) 經濟部中央標準局員工消費合作社印製 嗪基(例如5-酞嗪基)、喹唑啉基(例如2-喹唑啉基)、 異噁唑基(例如3-異噁唑基、4-異噁唑基)、苯并異噁唑 基(例如1,2-苯并異噁唑-4-基)、2,1-苯并異嗎唑-3-基 )、噁唑基(例如2-噁唑基、4-噁唑基、5-噁唑基)、苯 并噁唑基(例如2-苯并噁唑基)、苯并噁嗪唑基(例如4-苯并噁嗪唑基)、異睡唑基(例如3-異噻唑基、4-異噻唑 基)、苯并異睡唑基(例如1,2-苯并異噻唑-3-基、2,1 -苯并異睡唑-5-基)、噻唑基(例如2-睡唑基 >、苯并《唑基 (例如2-苯并唾唑基)、噻嗪唑基(例如1,2,3-瞎嗪唑-4 -基)、噁嗪唑基(例如,1,3,4-噁嗪唑-2-基)、二氫蠛 B秦唑基(例如4, 5-二気-1,2,4-曛嗪唑-3-基)、呋喃基( 例如2-呋喃基、3-呋喃基)、苯并呋喃基(例如3-苯并呋 喃基)、異苯并呋喃基(例如1-異苯并呋喃基)、_盼甲 基(例如2-睡盼甲基、3-噻盼甲基)、苯并噻盼甲基(例 如卜苯并睡盼-2-基、2-睡吩-1-基)、四唑基(例如5-四 睡基)、苯并二噁唑基(例如1,3-苯并二噁唑-5-基)、 二苯并呋喃基(例如2-二苯并呋喃基、3-二苯并呋喃基) 、二苯并噁吡(例如二苯并[b,f]噁吡基-2-基)、二氫二 苯并噁吡基(例如二氫二苯并[b,f]畷吡基)、氧萘基 (例如2H-氧萘-3-基、4H-氧萘-2-基)、二苯并噻吡基( 例如二苯并[b,f]噻吡-3-基、二氫二苯并[b,f]確吡_3_基 )、嗎啉基(例如1,4-嗎啉-4-基)、盼睡嗪基(例如2-盼噻嗪基)、環五睡盼甲基(例如環五[1>]_盼-3-基)、 環六睡盼甲基(例如環六[b]睡盼-3-基)等。 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) (請先閱讀背面之注意事項再本頁)
訂 16 ϋ’:五、 發明説明(13 A7 B7 經濟部中央標準局員工消費合作社印製 〔環烷基〕乃意指C3〜Ce之環狀烷基,例如環丙基、 環丁基、環戊基、環己基等。 「環烷烯基」乃意指C3〜Ce之環狀烷烯基,例如環丙 烯基(例如卜環丙烯基)、環丁烯基(例如,2-環丁烯-1 -基)、環戊烯基(1-環戊烯-1-基)、環己烯基(例如1 -環己烯-1-基)等。 「烷氧基」乃指G〜“的烷氧基,例如甲氧基、乙氧 基、正丙氧基、異丙氧基、正丁氧基等。 「取代或非取代」中之取代胺基乃例如甲胺基、乙胺 基、二甲胺基、環己胺基、苯胺基、二苯胺基等之單或二 取代胺基、哌啶基、吡阱基、嗎啉基等之環狀胺基。 「醯氧基」乃意指從前述之「酿基」所衍生之酿氧基 ,例如乙酿氧基、丙醢氧基、丁酿氧基、戊酿氧基等。 「鹵素」乃意指氟、氯、溴、碘。 「烷氧羰基」乃意指由前述之「烷氧基」所衍生之烷 氧羰基,例如甲氧羰基、乙氧羰基、苯氧羰基等。 「芳烷基氧羰基」乃意指由前述之「芳烷基」所衍生 之芳烷氧羰基,例如甲基氧羰基、苯乙基氧羰基等。 「芳氧羰基」乃意指由前逑之「芳基」所衍生之芳氧 羰基,例如苯氧羰基、萘氧羰基等。 「烷烯氧基」乃意指由前述之「烷烯基」所衍生的烷 烯氧基,例如乙烯氧基、卜丙烯氧基、2_丁烯氧基等。 「羥烷基」乃意指由前述之「烷基」所衍生的羥烷基 ,例如羥甲基、羥乙基、羥丙基等。 本紙張尺度適用中國國家標準(CNS ) Α4規格(210Χ297公釐)
(請先閱讀背面之注意事項V -裝— 1¾本頁) 訂 線 17 513422 A7 B7 經濟部中央標準局員工消費合作社印製 五、發明説明(14 ) 「烷基硫」乃意指由前述之「烷基」所衍生的烷基硫 ,例如甲基硫、乙基硫、丙基硫等。 「烷撐基二氧」乃指由所衍生的「烷撐基二氧 」,例如甲撐二氧、乙撐二氧、丙撐二氧等。 於「亞苯基」、「亞萘基」、「噻吩二基」、「吲哚 二基」、「噁唑二基」、「噁嗪唑二基」、「四唑二基」 中係可在能取代的任意2處與相鄰的基結合。 又,在前逑定義中,取代基為環狀者亦可被選自硝基 、烷氧基、氨磺醯基、取代或非取代胺基、醢基、酿氧基 、羥基、鹵素、烷基、烷炔基、烷氧羰基、芳烷氧羰基、 芳烷氧羰基、甲磺醯氧基、氰基、烷烯氧基、羥烷基、三 氟甲基、烷硫基、-N = PPh3、氧代、硫代、羥亞胺基、烷 氧亞胺基、苯基及烷撐二氧中1〜3個的基所取代,但於 環上中之此等的取代基亦可於能置換的任意進行取代。 通式(I )之化合物的鹽可舉例如鹼金颶鹽(例如鋰鹽 、納馥或鉀鹽等)、驗土族金屬鹽、(例如鈣鹽等)、與 有機驗(例如三甲醇胺基甲烷、三甲胺、三乙胺、2-胺基 値烷、第三丁基胺、二異丙基乙胺、正丁基甲基胺環己胺 、二環己胺、N-異丙基環己胺、糠基胺、苯甲基胺、甲基 苯甲基胺、二苯甲基胺、N,N_二甲基苯甲基胺、2_氯苯甲 基胺、4-甲氧基苯甲基胺、卜亞萘基甲胺、二苯基苯甲基 胺、三苯基胺、1-萘基胺、卜胺基蒽、2-胺基蒽、脫氫松 脂酿胺、N-甲基嗎啉或吡啶)之鹽、或胺基酸鹽(例如賴 胺酸鹽、精胺酸鹽等)。 (請先閱讀背面之注意事項 本百〇 -裝· 訂 線 本紙張尺度適用中國國家標準(CNS ) A4規格(2l〇X 297公慶) 18
五 • 經濟部中夬標準局員工消費合作社印製 發明説明(15) 水和物乃意指Μ式(I )所示之化合物或其鹽的水和物 ,例如1水和物、2水和物。 本發明化合物係Μ通式(I )所示,且包含其全部的立 體異性體(非鏡像立體異構物、差向立體異構物、鏡像物 等或外消旋髏)。 Μ通式(I >所示之化合物中,a=l之化合物,尤其, 後述之表3b及3c所示的化合物係特開平2-180862說明書中 所記載的公知化合物。 Μ通式(I )所示的化合物中,n=〇之化合物(以通式 (I ’)所示的化合物)係如下逑反應式所示,可藉由使通 式U )所示的胺基化合物與對應於部分構造式Z-Xi-Xa-Xa 的磺酸或羧酸的反應性衍生物進行反應來製造。
QA—R
NH I B (II) ---------裝— 一 i (請先閱讀背面之注意事項^^寫本頁 訂
A—R N—Z — Xr B (I·) (式中,A、B、R、Xt、Χβ、、X3、Y及Z之定義同於前述 )° 對應於部分構造式Z-X1-Xa-X3$磺酸為M通式χ3-Xa-Xi - S〇a〇H所示的化合物。此等磺酸或羧酸之反應性衍生物 乃意指對應的酸鹵化物(例如氯化物、溴化物、碘化物) 、酸無水物(例如與蟻酸或醏酸之混合酸無水物)、'活性 酯(例如,琥珀酿亞胺酯)等,包含使用於一般胺基之酿 化的酿化劑。又,羧酸X3-Xa-Xi-C00H係不限於反應性衍 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 19 線 513422 Α7 Β7 經濟部中央標準局員工消費合作社印製 五、發明説明(16) 生物,亦可於使用在胺與羧酸之縮合反應的縮合劑(例如 二環己基羰二亞酿胺(DCC)、1-乙基-3-(3-二甲基胺基丙 基)羰二亞酿胺、Ν,Ν’-羰基二眯唑)的存在下進行反應。 反應只要依照一般胺基的酿化反應之條件下進行即可 ,例如,Μ酸鹵化物進行縮合反應時,溶劑可使用醚条溶 劑(例如二乙醚、四氫呋喃、1,4_環氧己烷)、苯条溶劑 (例如苯、甲苯、二甲苯)、鹵化碩氫条溶劑(例如二氯 甲烷、二氯乙烷、氯仿)、其他、醋酸乙酯、二甲基甲酿 胺、二甲基亞確I、乙腈等,必要的話,在鹸基(例如三乙 胺、吡啶、Ν,Ν-二甲胺基毗啶、Ν_甲基0馬啉等之有機驗、 或氫氧化鈉、氫氧化鉀、磺酸鉀等之無機鹼)的存在下, 冷卻下乃至室溫或加熱下,較佳係-20t:乃至冰冷下或室 溫乃至反應条的加熱回流溫度,數分鐘乃至數十小時,較 佳係0.5小時乃至24小時,更佳係1小時乃至12小時實施 即可。 卽使於其他之反應性衍生物或游離的酸與胺U)之反 應中,依照各反應性衍生物或游離酸的性質,按公知的方 法,只要決定反應條件即可。 反應生成物係依一般的精製法,例如溶劑萃取、色層 分祈、再結晶法等精製之。 若表示本反應法中之原料化合物(I)的具體例,3-胺 基[2,2, 1]雙環条化合物之具體例可例示7-(3_胺基雙環 [2,2, 1]庚-2-基)_5-庚烯酸、7-(3-胺基雙環[2,2, 1]庚-2 -基〉_2,2-二甲基-5-庚烯酸、7-(Ν-甲基-3-胺基雙環[2,2 (請先閲讀背面之注意事項寫本頁) •裝 訂 線 本紙張尺度適用中國國家標準(CNS ) A4規格(210 X 297公釐) 20 513422 A7 B7 五、發明説明(17 ) 經濟部中央標準局員工消費合作社印製 ,1]庚-2-基)-5-庚烯酸、6-(3-胺基雙環[2,2, 1]庚-2-基) -5-己烯酸等。又,2-胺基-6,6-二甲基[3, 1,1]雙環条化 合物之具體例可例示7-(2-胺基-6,6-二甲基雙環[3, 1,1] 庚-3_基〉-5-庚烯酸等。又,此等原料化合物之庚烯酸鍵 可形成飽和亦可形成庚酸,亦可鏈的中間介入-0-、-S-、 -NH_等之雜原子或雜基或亞苯基,亦可Μ氧代基進行取代 ,可例示如7_(3-胺基雙環[2,2,1]庚-2-基)庚酸、4-[2-( 2-胺基雙環[3,1,1]庚-3-基)乙氧基苯基醋酸,7-(3_胺基 雙環[2,2,1]庚-2-基>-6-氧代庚酸等。此等之原料化合物 係已記載於特公平5-79060號說明書、特公平6-23170號說 明書中,或可依此等說明書之方法而製造。 對應於部分構造式Z-Xi-X3-X3之磺酸X3-Xa-Xi-S〇2〇H 及羧酸X3-X2-Xi-C00H係具有對應於前逑X之取代基的磺酸 或羧酸,亦即,烷磺酸或羧酸、烷烯磺酸或羧酸、烷炔磺 酸或羧酸、環烷磺酸或羧酸、環烷磺酸或羧酸、芳基磺酸 或羧酸、芳烷基氧磺酸或羧酸、雜環取代磺酸或羧酸、雜 芳基烷基磺酸或羧酸、及取代胺基磺酸或羧酸。此等之磺 酸及羧酸可分別具有前述定義之取代基。又,此等磺酸及 羧酸可爲自市售品所得到者,或,從已知的化合物依習知 的方法而很容易合成者。反應之際,此等磺酸及羧酸可依 需要而作為對應之上述反應性衍生物。例如形成酸鹵化物 時,只要依習知的方法(例如新實際化學講座14卷1787頁 (1978) ; Synthesis 852-854 (1986〉;新實驗化學講座 22 卷115頁(1992〉)而與齒化亞硫醯基(例如亞硫酿氯)、 (請先閱讀背面之注意事項再_馬本頁) •裝-
、1T 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 21 513422 A 7 B7 五、發明説明(18 ) 鹵化磷(例如三氯化磷、五氯化磷)、鹵化草醯基(例如 乙二酿氯)等反應即可。有關其他之反應性衍生物同樣地 亦可Μ公知的方法調製。 本發明目的化合物(I )之中,侧鐽Α乃具有不飽和鍵 ,尤其雙鍵之化合物係可使對應於侧鋪A-R部分之殘餘部 分的環烯化合物依Witt ig反應的條件與Μ下述通式(M)所 示之醛衍生物反應而製造之。
(式中,A、B、R、Xi、Xa、Χ3、Υ及Ζ之定義同於前述) 〇 原料化合物(I〉可依例如記載於特開平2-256650號說 明書之方法製造。又,對應於側鏈AR部分之殘餘部分的環 烯化合物係可在鹼的存在下依公知的方法使對應的鹵化烷 酸或其酯衍生物、醚衍生物、醯胺衍生物等與三苯基滕進 行反應而合成之。 經濟部中央標準局員工消費合作社印製 (請先閲讀背面之注意事項本頁) 於本發明目的化合物(I )中,R為C00H之化合物亦可 依所希望的形成對應之酯衍生物、醇衍生物、醚衍生物、 酿胺衍生物。例如酯衍生物係可依公知的方法藉由酯化以 製造羧酸。又,若還原酯衍生物,可形成醇衍生物,若進 行酿胺化亦可形成酿胺衍生物。醚衍生物亦可藉由0-烷基 化而製造醇衍生物。 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 22 513422 Α7 Β7 經濟部中央標隼局員工消費合作社印製 五、發明説明(19 ) 本發明之化合物(I〉係表示藉由Μ活體外與PGD2受容 體結合之卩603拮抗作用,可用來作為起因於PGDat生產過 多的肥胖機能不全相關的疾病治療劑。例如可用來作爲全 身性肥胖細胞症或全身性肥胖細胞活性化障礙的治療劑、 抗氣管收縮劑、抗喘息劑、抗過敏性鼻炎劑、抗過敏性結 膜炎劑、抗尊麻疹劑、缺血再灌流傷害治療劑、抗炎症劑 。尤其,本發明化合物(I )係Μ活體内顯示鼻塞抑制作用 ,故可作為鼻塞症之治療劑。 將本發明之化合物(I)用於治療時,可調製成為一般 經口或非經口投與用的製劑。含有本發明之化合物(I)之 醫藥組成物可採用用Μ經口及非經口投與之劑形。亦卽,亦 可形成錠劑、膠囊劑、顆粒劑、散劑、糖漿劑等之經口投 與製劑、或、靜脈注射、筋肉注射、皮下注射等之注射用 溶液或懸濁液、吸入藥、點眼藥、點鼻藥、痤劑、或、軟 膏劑等之經皮投與用製劑等的非經口製劑。 此等製劑可使用從事此業者已知之適當擔體、賦形劑 、溶劑、基劑等來製造。例如,錠劑時,可使活性成分與 補助成分一起壓縮或成型。補助成分係可使用製劑上所容 許之賦形劑、例如結合劑(例如玉蜀黍澱粉)、充瑱劑( 例乳糖、微結晶性绻維素)、崩壊劑(例如澱粉葡萄糖酸 鈉)或滑澤劑(例硬脂酸鎂)等。錠劑亦可適當被覆。糖 漿劑、液劑、懸濁劑等之液體製劑時,例如使用懸濁化劑 (例甲基纖維素)、乳化劑(例外源凝集素)、保存劑等 。注射用製劑時,可為溶液、懸濁液或油性或水性乳濁液 (請先閱讀背面之注意事項ν •裝-- 零舄本頁) 、1Τ 線 本紙張尺度適用中國國家標準(CNS ) Α4規格(210 X 297公釐) 23 2 A7 B7 五 、發明説明(20 ) 之形態,此等亦可含有懸濁安定劑或分散劑等。使用來作 為吸入劑時,可用來作為能適應於吸入器之液劑,使用來 作為點眼劑時亦可用來作為液劑或懸濁劑。尤其使用來作 為一用以治療鼻塞症之點鼻藥時,依一般製劑化的方法, 可使用來作為液劑、懸濁化劑,或,粉末化劑(例如羥丙 基纖維素、卡巴波爾)等,加入鼻孔作為粉末劑。或,充 填低沸點之溶劑及特殊的容器中,可使用來作為噴射劑。 化合物(I)之投與量依據投與形態、患者年齡、體重 、性別、或所併用的藥物(若有的話)等而異,最終仍委 由翳師的判斷,但,經口投與時,體重每lkg為1日0.01 〜100mg,宜為0·01〜l〇mg,更宜為0.1〜l〇mg,非經口投 與時,髏重每lkg為1日0·001〜lOOing,宜為0.001〜lmg ,更宜為0·01〜lmg。只要將此分開成1〜4次投藥卽可。 Μ下舉實施例詳細說明本發明,此等僅為例示,本發 明並非限制於此等。 實施例1 彳 (請t閲讀背f之注意事項^^寫本頁) 裝· 訂 cooch3 經濟部中央標準局員工消費合作社印製 (la-2)
/NHS〇2— (la-1)
^^vNHS〇2 —(ry^〇 (la-3)
気氣流下,使(2)-7-[(15,211,311,411卜3_胺基雙環[2, 2,1]庚-2-基]-5-庚烯酸甲酯 U -l)(251mg , l.OOnifflol)溶 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 24 513422 A7 B7 五、發明説明(21 經濟部中央標準局員工消費合作社印製 解於二氯甲烷(8ml),加入三乙胺(〇.238ml、2. OOmmol)後 ,冰冷下,加入2-氯磺醯基二苯并呋喃(350mg, 1,31hnb〇1 ),攪拌30分鐘,昇溫至室溫。反應液Μ矽凝膠管柱色層 分析(正己烷、醋酸乙酯1:4)精製,從正己烷(l〇ml)結 晶化,得到(Z)-7-[(1S,2R,3R,4R)_3-(2-二苯并呋喃基) 磺醢基胺基雙環[2,2,1]庚-2-基]-5-庚烯酸甲酯(la-1) (342ing,0·710ππβο1)。收率 71%。 融點:115-116= 元素分析(C 27Η 31Ν〇5 S ) 計算値(%) : C,67.34;H,6.49;N,2.91;S,6.66 實測値(%) : C,67.16;H,6.47;N,2.99;S ,6.66 IR (CHC13) : 3382,3024,2952,2874,1726,1583,1465,1442,1319,1245,1154 ,1121,1104,1071,1019,890,840,817 /cm。 1H NMR(CDC13) δ : 0.94-1.92(14H,m),2.15-2.24(3H,m),2.99.3.07(lH,m), 3.66(3H,s),4.98(lH,d,J=6.6Hz),5.10-5.22(2H,m),7.39-7.46(lH,m),7.51-7 .70(3H,m),7.87-8.13(2H,m),8.53(lH,d,J=2.lHz)。 [ct]D = -0.6〇 (ΟΗα3,ο=1·01%,23ΐ)· ([α]365 = +37·0β (CHC13,c=1.01%,23t:)· 使(Z)-7-[(15,21311,41〇-3-(2-二苯并呋喃基>磺酿 基胺基雙環[2,2,1]庚-2_基]-5 -庚稀酸甲醋(la-1) (234mg ,0·50πιιβο1)溶解於甲醇(6ml〉_四氫呋喃(4·1>,冰冷下, 加入IN氫氧化鉀(1.50ml,1.50fflmol〉後,昇溫至室溫,反 應16小時。餾去溶劑後,於殘渣中加入酯酸乙酯(5〇ml)與 水(10ml),進而加入1N鹽酸(2· 00ml,2. OOfflol),分取有 機層後,以飽和食鹽水洗淨有機層後,Μ無水硫酸鈉乾燥 。餾去溶劑後,殘渣Μ矽凝膠管柱色層分析(正己烷、
(請先閲讀背面之注意事項V 裝-- r本頁) 訂 線 本纸張尺度適用中國國家標準(CNS ) Α4規格(210Χ297公釐) 25 - 513422 A7 B7 五、發明説明(22 經濟部中央標準局員工消費合作社印製 酸乙酯=1 ·· 1,0.2%醋酸)精製,得到(Z)-7_[(1S,2R, 3R,4R〉_3-(2_二苯并呋喃基〉磺醯基胺基雙環[2,2, 1]庚-2 -基]-5-庚烯酸(la-2> (203mg,0.434mniol)。收率 87%。 油 IR (CHC13) : 3266,3026,2952,2874,1708,1465,1443,1423,1319,1267,1245 ,1153,1121,1104,1072,906 /cm。 1H NMR(CDC13) δ : 0.93-1.94(14H,m),2.12-2.19(lH,in),2.26(2H,t,J=7.2H z),3.00-3.08(lH,m),5.12.5.25(2H,m),5.26(lHfd,J=6.6Hz),7.38-7.45(lH,m),7.51-7.70(3H,m),7.87-8.13(2H,m),8.54(lH,d,J=2.lHz)。 [a]D = +6.8〇 (CHC13,c=1.08%,23t:)e 將(Z)-7-[(lS,2R,3R,4R)-3-<2-二苯并呋喃基)磺醢 胺基雙環[2,2, 1]庚 基]-5-庚烯酸(la-2) (453mg,0.97 mmol〉溶解於甲醇(5ml)中,冰冷下加入IN甲氧基鈉/甲醇 溶液(1.034當量,0.937ml,0.97inmol)後,昇溫至室溫, 反應1小時。餾去溶劑,而得到鈉鹽(la-3) (457mg,0.933 mmo 1)。收率 96%。 無晶狀粉末 元素分析(C26H28N〇5SNa.0.6H2〇) 、. 計算値(%) : C,62.41;H,5.88;N,2.80;S,6.41;N a ,4.59 實測値(%) : C,62.45;H,5.92;N,2.99;S ,6.49;N a ,4.46 IR (KBr) : 3434,3280,3074,3007,2952,2873,1566,1467,1444,1417,1344,1 315,1270,1248,1200,1189,1154,1124,1107,1075,1058,895,842,818 /cm。 1H NMR(CD30D) δ : 1.02.2.05(16H,m),2.16.2.23(lH,m),2.94-3.00(lH,m), 4.98-5.05(2H,m),7.41.7.48(lH,m),7.53.7.62(lH,m),7.66(lH,d,J=8.4Hz),7 • 77(lH,d,J=8.4Hz),8.57(lH,d,J=2.1Hz)。 [a]D = -15.2〇 (CH3OH,c=1.07%,22r)e 實施例2 (請先閲讀背面之注意事項本頁) 裝· 訂 線 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 26 五、 發明説明( 23
COOCH3 3COOH (II-2) A7 B7 COOCH3 ^vNHCO—(3^^0 (lk-11) cooh ^vNHCO —<Q)~ 經濟部中央標準局員工消費合作社印製 (lk-12) 將(2>-7-[(15,211,31^41〇-3-胺基雙環[2,2,1]庚-2-基]-5-庚烯酸甲酯三氟醋酸鹽(I -2)(依據特公平5 -79060號、參考例而製得)232mg(0.636mmol)溶解於二氯 甲烷(5ml〉中,冰冷下加入三乙胺〇.279ml(2.0ffiniol)與4-雙苯基羰基氯,在同室溫下攪拌7小時。Μ矽凝膠管柱色 層分析(醋酸乙酯:己烷=1 : 4)精製反應液,得到(Ζ) -7-[(15,28,31^41〇-3-(4-雙苯基)羰基胺基雙環[2,2,1]庚 -2-基]-5-庚烯酸甲酯(11(-11)221料(0.512111111〇1>〇將此化 合物(lK-ll)(190mg,0.440mBiol)溶解於甲醇(6nl)中,冰 冷下加入IN K0H(1. 10ml,1· lOmmol),在室溫下攪拌15小 時。減壓下濃縮反應液後,於殘渣中加入水(20ml)與1N HCl(2ml>,Μ醋酸乙酯萃取。有機層K飽和食鹽水洗淨後 ,以硫酸鈉乾燥後,濃縮。殘渣Μ矽凝膠管柱色層分析( 醋酸乙酯:己烷=1: 1) (〇·3%醋酸)精製而得到<Ζ) - 7 _[(lS,2R,3R,4R)-3-(4-雙苯基)羰基胺基雙環[2,2, 1]庚-2-基]-5-庚烯酸(1K-I2)172iag(0.412ffimol)。收率 94%。 下述所示之化合物亦可Μ如下的方法來製造。 實施例3 、CH〇 __ vNHS02-^ (III-l)
_CO〇- 1/2Ca2+ ,NHS02^Q (3d-l) 本紙張尺度適用中國國家標準(CNS ) A4規格(210 X 297公釐) (請先閱讀背面之注意事項r 裝-- 冒寫本頁) 、11 線 27 經濟部中夬標隼局員工消f合作社印¾ 513422 第85107425號專利申請案 H2 γ 說明書修正頁91年9月27日 Α7 五、發明説明(24) 氮氣氛下,於一由4-浚基丁基三苯基搽溴(14. 8g, 33.3〇111〇1)收回氬呋喃(8〇11)所構成之懸濁液中以室溫加 入第三丁基鉀(7.55g,67.3·βο1)。直接Μ室溫«拌1小 時後,冷郤至-201C而徐缓加入卜[(15,25.35.41〇-3-甲醒 基甲基雙環[2\2, 1]庚-2-基]苯磺醢胺U -1)(持開平2- 256650號、參考例2)(3.25g,ll.liaol)之四氳呋喃溶液 (20ml〉。在-20t:下雄繙魇拌1小時半後,除去冰浴,進 而再漫拌1小時。於反應蔽中加入2N鹽酸,以賭酸乙酯萃 取,以水及食邇水洗淨獯缩。於所得到之粗生成物中加入 甲苯與1N氳氧化納溶液而分取水層。有機層再一次水洗淨 ,合併先前之水層後,加入2N鹽睃。以賭酸乙酯萃取後, 以水及食鹽水洗淨,以硫酸卞乾燥後獾缩。殘渣K矽凝膠 管柱色層分析精裂,得到(Z)-7-[(lR,2S,3S,4S)-3-苯基 磺S基胺基雙環[2,2,1]庚-2-基]-5-庚烯酸鈣(3d-l〇 (3.29g ,收率 7996 )。 ®a:6 2X: 元紊分祈(C 20 Η 27 NO 4 S ) 計算値(%):C· 6 3.6 3;H, 7.2 1;N, 3.7 1;S, 8.4 9 S测値(%):C· 6 3.5 6;Η· 7.2 1;N, 3.8 3;S,8.4 3 · [〇:】D=+5.3±0.5*(CHCl3.C=1.003%,22t:) [a]D=+27.1±0.7*(MeOH,C=1.0 15%.24t:) IR(Nujol) 3282. 3260, 3300. 2400, 1708. 1268. 1248. 1202. 1162. 1153, 1095. 1076/cm 1HNMR δ 0.88-2.10(m, 14H), 2.14(brs, 1H)· 2.34(t. J=7.2Hz. 2H). 2.95-3.07(m. 1H). 5.13-5.35(m. 3H). 7.45—7.64(m. 3H), 7.35-7.94(m. 2H), 9.52(brs· 1H) 與上述實施例同樣地做法而製得之化合物表示於下。- 本紙朵尺度逋用中國國家標率(CNS ) Α4規格(210Χ297公釐) i - ' - I 丨丨 - I - - i I I I (請先閱讀背ώ之注意事項再填寫本頁) 訂 28 513422 A7 B7 五、發明説明(25 ) 表1 a
No. 經濟部中央標準局員工消費合作社印製
la-1 ch3 la-2 H la-3 Na la-4 ch3 la-5 H la-6 ch3 la-7 H la-8 ch3 la-9 H la-10 ch3 la-11 H la-12 la-13 ch3 la-14 ch3 la-15 H la-16 ch3 la-17 H la-18 ch3 la-19 H la-20 ch3 la-21 H la-22 H la-23 H
cf3 /SO2NH2
och3
och3 (請先閱讀背面之注意事項再填_,頁) 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 29 513422 A7 B7 五、發明説明(26 )
COORi NS02—X1-X2-X3 Η
No. la-24 la-25 la-26 la-27 la-28 la-29 la-30 la-31 la-32 la-33 經濟部中央標準局員工消費合作社印製 la-34 la-35 la-36 la-37 la-38 la-39 la-40 la-41 la-42 la-43 la-44 la-45
CH3 H Na CH3 H Na CH3 H CH3 H CH3 ch3 H ch3 H CH3 H
CH3 H CH3 H 、丨厂一 -N=N- 〇Ac (請先閱讀背面之注意事項再本頁) -裝- -N=N- -N=CH- >-CH=CH2
OCH3 —^^CH2CH2^^ 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐)
OH 訂 30 513422 A7 B7 五、發明説明(27
No. XJ-X2-X3 la-46 la-47 la-48 la-49 la-50 la-51 la-52 la-53 la-54 la-55 la-56 la-57 la-58
CH3 H Na CH3 H CH3 H CH3 H CH3 H CH3 H N〇2 nh2
請 先 閱 讀 背 之 注 意 事 項 本 頁 裝 訂 經濟部中央標準局員工消費合作社印製 la-59 la-60 la-61 la-62 la-63 la-64 la-65 la-66 la-67 la-68
CH3 H ch3 H CH3 H ch3 H CH3 H —(CH2)5CH3 ht 本紙張尺度適用中國國家標準(CNS ) Α4規格(210X 297公釐) 31 513422 A 7 B7 五、發明説明(28 )
經濟部中央標準局員工消費合作社印製 la-69 la-70 ch3 H la-71 la-72 ch3 H la-73 la-74 ch3 H -〇-〇Ac la-75 la-76 ch3 H -Qr^ -^^•COOR1 la-77 la-78 ch3 H ~^C5^n〇2 la-79 H "〇-〇CH3 la-80 la-81 ch3 H -p N〇2 la-82 la-83 ch3 H -o- nh2 la-84 H no2 ~{^〇ch3 la-85 H nh2 O"0CH3 la-86 H N〇2 〇^0H la-87 H ο·0Η nh2 (請先閱讀背面之注意事項冩本頁) 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 32 513422 A7 B7 五、發明説明(29
No.
XrXrX3 la-88 la-89 la-90 la-91 la-92 la-93 la-94 la-95 la-96 la-97
CH3 H CH3 H CH3 H 經濟部中央標準局員工消費合作社印製 la-98 la-99 H Na ^〇^n-chQkno2 Η
,och3 /)^〇ch2 och3 (請先閲讀背面之注意事項再ΙΡτ本頁) •裝· 訂 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 33 513422 A7 B7 五、發明説明(30 )
No. Ri XrX2-X3 經濟部中央標準局員工消費合作社印製 la-100 la-101 la-102 la-103 la-104 la-105 la-106 la-107 la-108 la-109 la-110 la-111 la-112 la-113 la-114
(請先閱讀背面之注意事項本頁) -裝_ 訂 線 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 34 513422 Μ B7 五、發明説明(31 )
No. Ri X1-X2-X3 la-115 la-116 la-117 la-118 la-119 la-120 la-121 la-122 la-123 la-124 la-125 la-126 la-127 la-128 la-129 la-130 la-131 la-132 la-133 la-134 經濟部中央標準局員工消費合作社印製 la-135 la-136 la-137 la-138 la-139 la-140 本紙張尺度適用中國國家標準(CNS ) A4規格(210 X 297公釐)
(請先閱讀背面之注意事項v 裝-- 專舄本頁) 訂 線 35 513422 A7 B7 五、發明説明(32)
No. Ri XrX2-X3 經濟部中央標準局員工消費合作社印製 la-141 ch3 la-142 H NC^ la-143 H Ulo /=\ N〇2 la-144 H la-145 H ,Νχ la-146 H /=\ 〇CH3 la-147 H /=x 〇CH3 la-148 H och3 la-149 H V1 -〇iH la-150 H 9 〇Ac la-151 H 〇ch3 (請先閱讀背面之注意事項r •裝-- f本頁) 訂 線 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 36 513422 A7 B7 五、發明説明(33
No. ΧΓΧ2-Χ3 la-152 la-153 la-154
(請先閱讀背面之注意事項 本頁) 裝- 訂 la-155 la-156 七 la-157
線 la-158 經濟部中央標準局員工消費合作社印製 la-159 la-160
本紙張尺度適用中國國家標準(CNS ) A4規格(210 X 297公釐) 37 513422 A7 B7 五、發明説明(34
No. ΧΓΧ2-Χ3 經濟部中央標準局員工消費合作社印製 la-161 la-162 la-163 la-164 la-165 la-166 la-167 la-168 la-169 la-170 la-171 la-172 CH30, C2H50,
(請先閱讀背面之注意事項 巧本百〇 -裝· 訂 線
ch3 H 〇CH3
本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 38 513422 A7 B7 五、發明説明(35
No. xrx2-x3 la-173 la-174 la-175 la-176 la-177 la-178 la-179 la-180
CH3 H CH3 H CH3 H la-181 經濟部中央標準局員工消費合作社印製 la-182 la-183
CH3 H
(請先閱讀背面之注意事項本頁) 裝-
、1T 線 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 39 513422 A7 B7 五、發明説明(36)
經濟部中央標準局員工消費合作社印製
No. Rl xrx2-x3 la-184 H la-185 H la-186 la-187 ch3 H ch3 la-18S la-189 ch3 H ^^X^C〇〇R1 la-190 ch3 la-191 H COOR, la-192 ch3 la-193 H COORi (請先閱讀背面之注意事項再IPr本頁) .裝-
、1T 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 40 513422 A7 B7 五、發明説明(37
No. ΧΓΧ2-Χ3 la-194 CH30
(請先閲讀背面之注意事項v la-195 la-196 la-197 la-198 la-199
CH30, 裝-- 澤舄本頁) la-200 la-0201 經濟部中央標準局員工消費合作社印製 la-202 la-203 CH30
k 本紙張尺度適用中國國家標準(CNS ) A4規格(210 X 297公釐) 41 513422 A7 B7 五、發明説明(38
ΧΓΧ2-Χ3 CH30 la-204
-N=N -o la-205 CH30. (請先閲讀背面之注意事項再本頁)
la-206 la-207
、1T la-208 la-209 la-210 la-211 經濟部中央標準局員工消費合作社印製 la-212 la-213
本紙張尺度適用中國國家標準(CNS ) Α4規格(210X 297公釐) 42 513422 A7 B7 五、發明説明(39
la-214 CH30 o la-215 la-216 la-217 la-218 och3
(請先閱讀背面冬注意事項本頁) -裝· 訂 la-219 ch3o. 線 la-220 經濟部中央標準局員工消費合作社印製 la-221 la-222 la-223 -Oh %-
Cl /)CH3 -och3 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 43 513422 A7 B7 五、發明説明(4Q )
χΓχ2-χ3 ch3o la-224 CH3 la-225 o2n la-226 ch3o
—o la-227 CH3o 〇ch3 la-228 CH3o. h2n CH3o. la-229 la-230 la-231 la-232 nh2
經濟部中央標準局員工消費合作社印製 la-233 la-234 la-235
,CI
〇 N〇2 本紙張尺度適用中國國家標準(CNS ) Α4規格(210Χ297公釐) 44 513422 A7 B7 五、發明説明(41 )
COOH >so2—xrx2-x3 Η
No.
XrXrX3 la-236 .och3 OCH3 la-237 la-238
OCH3 (請先閱讀背面之注意事項 本頁) -裝· la-239 la-240
/〇ch3 -och3 訂 la-241 la-242 la-243 CH3o CH3q CH3o —( CH3o'
Ν-δ-
〇 OCH3 OCH3 k 經濟部中央標準局員工消費合作社印製 la-244 la-245 la-246 \\ /r^c\^~0CH2 ~och3 一 〇 _/〇CH3 一〇CH3 CH3、〇ch3 ch3〇
«I
,〇ch3 〇ch3 〇ch3 ,〇ch3 〇ch3 〇ch3 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 45 513422 A7 B7 五、發明説明(42
COOHpso2—χΓχ2·χ3 Η X]-X2~X3 CH30 la-247
•C~N
,OCH3 OCH3 〇ch3 CH30 la-248
-C_N CH30, la-249 ch3o la-250 〇 0CH3 ^0CH3 (請先閱讀背面之注意事項再-Jill本百〇 燊' ch3o OCH3 la-251 CH3o 〇 OCH3 OCH3 、\呑 r la-252 la-253 〇CH3 ch3o^ och3 -O-hS^ 0CH3 CH3o 〇 0CH3 〇ch3 i la-254 經濟部中央標準局員工消費合作社印製 la-255 la-256 la-257 CH3 ^ch3
ch3 ch3 ch3 ~θ~ΰ"Η^Ϊ^〇αΗ3 CH3(-oh
0CH3 0CH3 0CH3 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 46 513422 A7 B7 五、發明説明(43 )
xrxrx3 經濟部中央標準局員工消費合作社印製 la-258 la-259 la-260 la-261 la-262 la-263 la-264 la-265 la-266 la-267 la-268 la-269 la-270 la-271 CH30,
~^·°Ό och3
-^^nh-^^och3 CHoO
本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) (請先閱讀背面之注意事項再本頁) |裝· 太 、11 47 513422 A7 B7 五、發明説明(44 )
No. xrxrx3 經濟部中央標準局員工消費合作社印製 la-272 la-273 la-274 la-275 la-276 la-277 la-278 la-279 la-280 la-281 la-232 la-283 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐)
48 513422 A7 B7 五、發明説明(45 )
No.
XrX2-X3 la-284 la-285
CH30
CH30, la-286
〇- — I;--J-----^-- (,請先閱讀背面之注意事項再 本頁) la-287 CH30,
NH la-288 CH30, CH30乂
訂 la-289
n,ch3 ch3o, la-290 S02
CH3o, %; la-291 經濟部中央標準局員工消費合作社印製 CH3o,
la-292 la-293 la-294
CH3o,
CH30,
本紙張尺度適用中國國家標準(CNS ) A4規格(210 X 297公釐) 49 513422 A7 B7 五、發明説明(46)
No. xrxrx3 la-295 la-296
la-297 la-293 la-299 la-300
(請先閱讀背面之注意事項再本頁) .裝- 訂 la-301 la-302 經濟部中央標準局員工消費合作社印製 la-303 la-304 la-305
本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 50 513422 A7 B7 五、發明説明(47 )
ch3 經濟部中央標準局員工消費合作社印製 lb-1 lb-2 lb-3 lb-4 lb-5 lb-6 lb-7 lb-8 lb-9 lb-10 ch3 Η ch3o
ch3o
ch3o *ch2 o
(請先閱讀背面之注意事項V 裝-- f本頁) 、-?口 ch3o
ch3o ch2 ch3o
本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) -51 - 513422 A7 五、發明説明(48 )
No._Ri_ ΧγΧ2-Χ3 lb-11 η
O OCH3 lb-12 Η lb-13 „ -C~N~^ ^~QCH3 ^och3 0 y0CH3~0^OCH3 CH3o
0-N CH30、
OCH3 ^-och3 k〇CH3 (請先閱讀背面之注意事項本頁) 裝· 訂
lb-14 H 〇
lb-15 H 經濟部中央標準局員工消費合作社印製 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 52 513422 A7 B7 五、發明説明(49 表lc
No.
XrXrX3 lc-1 lc-2 lc-3 lc-4 lc-5 lc-6
ch3 ch3 K 0 /0CH3一^}(^-〇CH3 ~OCH3 (請先閱讀背面之注意事項 α本頁) lc-7 CH3o
lc-8 Ό^°Ό lc-9 經濟部中央標準局員工消費合作社印製 lc-10 lc-11 lc-12
CH30 OCH3 本紙張尺度適用中國國家標準(CNS ) Α4規格(210X 297公釐) 53 513422 A7 B7 五、發明説明(50 )
ld-l ld-2 ld-3 ld-4 ld-5 H S02CH3 Η H H OH H SO2CH3 H SO2CH3 ν/~Ν=ΝΗ〇 ld-6 H S02CH3
ld-7 H SO2CH3 CH30 -ch2-〇 ld-8 H S02CH3 CH30
ch2 ld-9 H SO2CH3 經濟部中央標準局員工消費合作社印製 ld-10 H SO2CH3
o 本纸張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 54 513422 A7 B7 五、發明説明(51
No. R3 R4 xrxrx3 ld-11 H SO2CH3
/==\ 〇 / \ II OCH3 〇ch3 (請先閱讀背面之注意事項本頁) •裝_ ld-12 Η S02CH3 OCH3 Ο /=/ -QtHrQt 〇ch3 訂 ld-13 η S02CH3 CH30
〇ch3 ^-〇ch3 och3 ld-14 h S02CH3 CH30\ 0 ld-15 H S02CH3 經濟部中央標準局員工消費合作社印製 本紙張尺度適用中國國家標準(CNS ) A4規格(210 X 297公釐) 55 513422 A7 B7 五、發明説明(52 表le
No. X「XrX3 le-l le-2
(請先閱讀背面之注意事項^^一舄本頁) •裝_ le-3 le-4 le-5 〇 /=<0CH3 、〇ch3 訂 le-6 ch3o
線 le-7 經濟部中央標準局員工消費合作社印製 le-8 le-9 lc-10
CH30 〇CH3 CH30、 OCHn 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 56 513422 A7 B7 五、發明説明(53 表1
No. R2 ΧΓΧ2-Χ3 1Μ lf-2
(請先閱讀背面之注意事項r •裝--層舄本頁) lf-3 lf-4 lf-5
-C-N
〇CH3 h〇CH3 〇CH3 訂 CH30 lf-6 lf-7 CH30
CH2 經濟部中央標準局員工消費合作社印製 lf-8 lf.9 lf-10 CH30
CH30 CH30、 • Li I— 1!»·- 〇 /0CH3 〇CH3 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 57 513422 A7 B7 五、發明説明(% ) 經濟部中央標準局員工消費合作社印製
,V/N-S02-XrX2.X3 No. R! X1-X2-X3 lg-1 H lg-2 H u CH3o lg-3 H HU lg-4 H ,0^0 lg-5 H , 0CH3 ~hC^^'h~hC^och3 lg-6 H \)CH3 ch3o ^1 本紙張尺度適用中國國家標準(CNS ) Α4規格(210Χ297公釐) 58 513422 Α7Β7 五、發明説明(55 表Ih
ΧΓΧ2-Χ3 lh-1 Η
請 λ 閲 讀 背 面 之 注 意 事 項 再 lh-2 Η 頁 lh-3 Η lh-4
H OCH3 och3 \)CH3 lh-5
H ch3o
lh-6
H lh-7
H ch3o
ch2 經濟部中央標準局員工消費合作社印製 lh-8 lh-9 lh-10
H
H
H ch3o
CH3o OCH3"^D^6'h"^^OCH3 och3 CH3o. 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 59 513422 A7 B7 經濟部中央標準局員工消費合作社印製
513422 A7 B7 五、發明説明(57 表1 j
No. X1-X2-X3 (請先閱讀背面之注意事項v ij-i lj-2 lj-3 1H ij-5 lj-6 11-7
CH3 H Na H ch3 ch3 H -裝--零舄本頁) lj-8 CH, lj-9 lj-l〇 lj-11 lj-12
CH3 H CH3 H 經濟部中央標準局員工消費合作社印製 lj-13 lj-14 lj-15 lj-16
CH3 H CH3 H
訂 本紙張尺度適用中國國家標準(CNS ) A4規格(210X29?公釐) 61 513422 A7 B7 五、發明説明(58
οι 2 2 1J-1J-
3 CHH
(請先閱讀背面之注意事項舄本頁) •裝· 訂 Η
h3
II
3 3 η*η ^ Η c C 經濟部中央標準局員工消費合作社印製 Η η3χ 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 62 513422 A7 B7 經濟部中央標準局員工消費合作社印製
513422 A7 B7 五、發明説明(60 ) 表Ik
No. X1-X2-X3 (請t閲讀背面之注意事項 經濟部中央標準局員工消費合作社印製 lk-l H -〇'CH2-〇 lk-2 lk-3 ch3 H lk-4 H —ΟΌ lk-5 H lk-6 H -〇 lk-7 H lk-8 H lk-9 H lk-10 H lk-11 ch3 oo lk-12 H 00 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 64 513422 A7 B7 五、發明説明(61 )
No.
XrXrX3 lk-13 Η lk-14
H 一<Q)-N=NH^-〇CH3 ch3o、 (請先閱讀背面之注意事項本頁) .裝· lk-15
H lk-16
H
lk-17 H
訂 lk-18
H 線 經濟部中央標準局員工消費合作社印製 lk-19 h
lk-20 H ~och3 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 65 513422 A7 B7 五、發明説明(62 ) 表lm -口-CO - xrx2-x3 經濟部中央標準局員工消費合作社印製
No. Rl XrX2-X3 lm-l lm-2 ch3 H lm-3 lm-4 ch3 H lm-5 lm-6 ch3 H —Q-n=n-^> lm-7 lm-8 ch3 H lm-9 lm-10 ch3 H ^〇""〇-<0^〇Ac lra-11 lm-12 ch3 H lm-13 lm-14 ch3 H lm-15 ch3 lm-16 H ~\jr\jr0kz lm-17 ch3 f=\ r=\ lm-18 H -ν/Λ>0Η (請先閱讀背面之注意事項本頁)
、1T 本紙張尺度適用中國國家標準(CNS ) A4規格(210 X 297公釐) 66 513422 A7 B7 經濟部中央標準局員工消費合作社印製
513422 A7 B7 經濟部中央標準局員工消費合作社印製
本紙張尺度適用中國國家標準(CNS)A4規格(21〇X29_) 513422 A7 B7 五、發明説明(65 表2a
No.
XrX2-X3 2a-l 2a-2 2a-3 2aM 2a-5 2a-6 2a-7 2a-8 2a-9
CH3 H CH3 H Na CH3 H CH3 H
CHO --.--η-----裝-- (請先閱讀背面之注意事項舄本頁) 2a-10 2a-ll 2a-12 2a-13 CH3 H CH3
、1T 2a-14 2a-15 經濟部中央標準局員工消費合作社印製 2a-16 2a-17 2a-18 2a-19 2a-20 2a-21 2a-22 2a-23 2a-24 CH3 H CH3 H CH3 H CH3 H Na
CH3 H
本紙張尺度適用中國國家標準(CNS ) Α4規格(210Χ297公釐) 69 513422 A7 B7 五、發明説明(66
No. X1-X2-X3 2a-25 2a-26 2a-27 2a-28 2a-29 2a-30
CH3 H CH3 H CH3 H -〇H2-^〇 經濟部中央標準局員工消費合作社印製 2a-31 2a-32 2a-33 2a-34 2a-35 2a-36 2a-37 2a-38 2a-39 2a-40 2a-41 2a-42 2a-43 2a-44 2a-45 2a-46 2a-47
CH3 ch3 H CH3 H CH3 H CH3 H CH3 H CH3 H CH3 H CH3 H
N 一〇H
〇 o s ------j-----裝-- (請先閱讀背面之注意事項^^馬本頁) 訂 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 70 513422 A7 B7 經濟部中央標準局員工消費合作社印裝
513422 A7 B7 五、發明説明(68
No. ΧΓΧ2-Χ3 經濟部中央標準局員工消費合作社印製 2a-68 2a-69 2a-70 2a-71 2a-72 2a-73 2a-74 2a-75 2a-76 2a-77 2a-78 2a-79 2a-80 2a-81 2a-82 2a-83 2a-84 2a-85 2a-86 2a-87
CH3 H
CH3 H CH3 H CH3 H ch3 H CH3 H CH3 H CH3 H CH3 H CH3 H
-OAc -〇CH3 ~C^〇AC ~^^-〇ch3 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 72 _ 7 0 513422 A7 B7 經濟部中央標準局員工消費合作社印製
本紙張尺度適用中國國家標準(CNS ) A4規格(210 X 297公釐) -73 - 513422 A7 B7 五、發明説明(70
No. X1-X2-X3 2a-113 2a-114
ch3 H -cf3 經濟部中央標準局員工消費合作社印製 2a-115 2a-116 2a-117 2a-118 2a-119 2a-120 2a-121 2a-122 2a-123 2a-124 2a-125
CH3 H CH3 H '0 OAc OH OCH3-o
(請先閱讀背面之注意事項寫本頁) •裝- 訂 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 74 513422 A7 B7 五、發明説明(71)
No. 2a-126 2a-127 2a-128
-On~O^N 人 N^O Η H-K-O (請先閱讀背面之注意事項本頁) •裝· 2a-129 2a-130
訂 2a-131
Q 2a-132 2a-133 經濟部中央標準局員工消費合作社印製 2a-134 2a-135 2a-136 -CH2
°O 0
本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 75 513422 A7 B7 五、發明説明(72
No.
XrX2-X3 2a-137 2a-138 H —^-〇H〇HOCH(CH3)2 (請先閱讀背面之注意事項寫本頁) .裝_ 2a-139 ίΓ 2a-140
sch3 經濟部中央標準局員工消費合作社印製 2a-141 2a-142 2a-143 2a-144 2a-145 2a-146 2a-147 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 76 513422 A7 B7 五、發明説明(73 COORi *NHCOXrXrX3
No. 2a-148 2a-149 xrx2-x3-*〇 2a-150 2a-151
V 2a-152 h3c、 2a-153 2a-154 2a-155 2a-156 -a> 經濟部中央標準局員工消費合作社印裝 2a-157 2a-158 2a-159 H3C〆 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 77 513422 A7 B7 經濟部中央標準局員工消費合作社印製
請 閱 · 讀 背 面 * 之 注 意 事 項
訂 513422 A7 B7 經濟部中央標隼局員工消費合作社印製
-79 - 513422 A7 B7 五、發明説明(76
No. XPX2-X3 2a-183 2a-184 2a-185 2a-186
2a-187 H3C〇
2a-188 2a-189 2a-190 經濟部中央標準局員工消費合作社印製 2a-191 2a-192 2a-193 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) CH3 C2H5 N Ac * 80
513422 A7B7 五、發明説明(77 ) 'COOR! ¥NHCOXrX2-x3
No. 2a-194 2a-195 H H3C’、S〆 2a-196
s々ch3 2a-197
>P 2a-198
2a-199 H
2a-200 H
經濟部中央標準局員工消費合作社印製
2a-201 H
2a-202 H
2a-203 H h3c^. 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 81 _ v I 鱗 513422 A7 B7 五、發明説明(78 )
2a-204 'Η3 、sAch3 2a-205 、s〜f3 2a-206 ^Η5 2a-207 、广 c〇h7 2a-208
.CH3 、s' 、ch3 2a-209 2a-210 2a-211 經濟部中央標準局員工消費合作社印製 2a-212 2a-213 、S,>、CH3
本纸張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 82 513422 Μ Β7 五、發明説明(79
2a-214 2a-215 2a-216
2a-217 2a-218
2a-219
2a-220
h3co‘ 經濟部中央標準局員工消費合作社印製 2a-221 2a-222 2a-223 \s^CH2OH 、广 CH2OCH3 、sAc〇ch3 本紙張尺度適用中國國家標準(CNS ) A4規格(21〇Χ297公釐) 83 513422 A7 B7 五、發明説明(
、COOH ¥NHCOXrX2-X3
No. X1-X2-X3 2a-224 2a-225 2a-226
(請先閲讀背面之注意事項V 裝-- 声本頁) 2a-227 2a-228 2a-229 OCH3
訂 2a-230 2a-231 線 經濟部中央標準局員工消費合作社印製 2a-232 2a-233
H3CO
本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 84 _ O - 513422 A7 B7 五、發明説明(81
No.
XpX2-X3 2a-234
H3CO
2a-235 2a-236
(請先閱讀背面之注意事項再本頁) •裝· 2a-237 2a-238
、1T 2a-239 2a-240 2a-241
OCH3 線 經濟部中央標準局員工消費合作社印製 2a-242 2a-243
本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 85 513422 A7 B7 五、發明説明(82)
No. 2a-244 2a-245 2a-246
XrXrX3
(請先閲讀背面之注意事項再本頁) •裝· 2a-247 2a-248 2a-249
訂 線 2a-250 經濟部中央標準局員工消費合作社印製 2a-251 hoh2c
本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 86 513422 A7 B7 五、發明説明(83 )
、COOH vNHCOXrX2-X3
No.
XrXrX3 2a-252 2a-253 ~0~CH3-Q^ch3 2a-254 s 一 h3c ch3 -p 2a-255 2a-256 H3co
經濟部中央標準局員工消費合作社印製 2a-257
COOH 本紙張尺度適用中國國家標準(CNS ) A4規格(210 X 297公釐) 513422 A7 B7 五、發明説明(84
No. X!-X2_X3 2a-258
H3CO
2a-259 2a-260 2a-261
(請先閲讀背面之注意事項再本頁) •裝· 訂 2a-262
// W/^〇CH3 、S 2a-263
OCH3 CH3 2a-264 經濟部中央標準局員工消費合作社印製 2a-265 2a-266 2a-267
CH3 、CH3 CH3 本纸張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 88 513422 A7 B7 五、發明説明(85
、COOH *NHCOXrX2-X3
No.
XrX2-X3 2a-268
2a-269 (請先閲讀背面之注意事項再驾馬本頁)
2a-270 2a-271 2a-272
訂 2a-273
2a-274
o 經濟部中央標準局員工消費合作社印製 2a-275 2a-276 2a-277
HON
本紙張尺度適用中國國家標準(CNS ) A4規格(210 X 297公釐) 89 513422 A7 B7 五、發明説明(86 )
No. X1-X2-X3 2a-278 2a-279
(請先閱讀背面之注意事項再本頁) 2a-280 2a-281 2a-282 COCH3
、1T 2a-283 2a-284
經濟部中央標隼局員工消費合作社印製 2a-285 2a-286 2a-287
本紙張尺度適用中國國家標準(CNS ) A4規格(210 X 297公釐) 90 513422 A7 B7 五、發明説明(87 )
COOH •NHCOXrX2-X3
No.
XrXrX3 2a-288
N 2a-289
COCH3 (請先閱讀背面之注意事項再本頁) ^衣_ 太 2a-290 2a-291 ch3 訂 2a-292 C2H5 2a-293 COCH3 2a-294 經濟部中夬標隼局員X消費合作社中製 2a-295 2a-296 o /0CH3一C^0CH3 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 91 513422 A7 B7 五、發明説明(88
XpX2-X3 2a-297 2a-298 2a-299 h3c〇 〇ch3 -c-nH0K〇ch3 och3 (請先閲讀背面之注意事項再本頁) 2a-300 CH3 I ch3 訂 2a-301 h3c 2a-302 2a-303 經濟部中央標隼局員工消費合作社印製 2a-304 2a-305 2a-306 〇ch3 〇ch3 〇ch3hQ^n-chQ^〇h 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 92 513422 A7 B7 五、發明説明(89 )
No. X1-X2-X3 2a.307 h3co 〇c OCH3 OCH3 OCH3 ,ch3 2a-308 2a-309 2a-310
och3 och3 0CH3 (請先閱讀背面之注意事項再5|^本頁) 裝_
、1T 2a-311 h3c 2a-312 2a-313 ~〇-n-c-nH〇^〇h -〇-K-c-nH^〇ch3 *k· 經濟部中央標準局員工消費合作社印製 ch3 2a-314 2a-315
H3CO ch3 OCH3 〇 r=( 〇CH3 OCH3 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 93 513422 A7 B7 五、發明説明(9〇 表2b 表2c 表2d COORi "N-COXrX2-X3 CH^
No. xrx2-x3 2b-l 2b-2 -o (請先閲讀背面之注意事項再
^^N-COX! ·Χ2·Χ3 No. Ri xrx2-x3 2c-l H -o 2c-2 H -o 2c-3 H ~hO^°'hO
COOR, ▼NHCOXrXrX3
經濟部中央標準局員工消費合作社印製
No. R,
XrX2-X3 2d-l 2d-2 2d-3 表纸張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) -94 513422 A7 B7 五、發明説明(91 表2e
No. 2e-l 2e-2
H H
XrX2-X3 o 2e-3 (請先閱讀背面之注意事項再本頁) 表2f
No. ΧΓΧ2-Χ3 訂 2f-l 2f-2 2f-3 表2g 經濟部中央標準局員工消費合作社印製
No. r3 r4 xrx2-x3 2g.l H S02CH3 本紙張尺度適用中國國家標準(CNS )八4規格(210X297公釐) 95 513422 A7 B7 五、發明説明(92 表2h
、COOH ¥NHCOXrX2-X3
No. ΧΓΧ2-Χ3 2h-l 2h-2 2h-3 2h-4 2h-5 2h-6 、s’CH3
0 (請先閱讀背面之注意事項再本頁) -裝_ 表2i
.COOH 〇 *NHCOXrX2-X3
No.
XrX2-X3 經濟部中央標準局員工消費合作社印製 2i-l 2i-2 2i-3 2i-4 2i-5 2i-6
S 、广 ch3 /
線 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 96 513422 A7 B7 五、發明説明(93 表2j
xrxrx3 2j-l 2j-2 2j-3 2H 2j-5 2j-6
(請先閱讀背面之注意事項再 1裝-- 本頁) 、-ιτ 表2k
xrx2-x3 經濟部中央標準局員工消費合作社印製 12 3 4. 5 k.k.kk-k-2 2 2 2 2
本紙張尺度適用中國國家標準(CNS ) A4規格(210 X 297公釐) 97 513422 A7 B7 五、發明説明(94 ) 表3a
No. Ri XrXrX3 3a· -3-4-5-6 3 3 3 3 3 3 3 3 3a 經濟部中央標準局員工消費合作社印製 3a-9 3a-10 3a-ll 3a-12 3a-13 3a-14 3a-15 3a-16 3a-17 3a-18
CH3 H H CH3 H CH3 H CH3 ch3 H CH3 H
CH3 H H3N*C(CH2〇H)3 Na 1/2 Ca H (請先閲讀背面之注意事項再本頁) -裝· 訂 線 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 98 513422 A7 B7 五、發明説明(95 )
co〇Ri >S02-XrX2-X3 Η No. Ri xrxrx3 3a-19 3a-20 ch3 H h3c -<P^ch3 h3c 3a-21 3a-22 ch3 H 3a-23 3a-24 ch3 H —ch2〇h 3a-25 H 一(CH2)3〇H3 3a-26 3a-27 ch3 H 一 (ch2)7ch3 3a-28 ch3 丨 (請先閱讀背面之注意事項再^^本頁) •裝.
'1T 經濟部中央標準局員工消費合作社印製 3a-29 3a-30 3a-31 3a-32 3a-33 3a-34 3a-35 CH3 ch3 H Na H Na N〇2
本紙張尺度適用中國國家標準(CNS ) A4規格(210Χ297公釐) 99 513422 A7 B7 五、發明説明(96 ) 表3b
No. Rl XrXrX3 3b-l ch3 3b_2 H 3b-3 H 3b-4 H 表3c 經 濟 部 中 央 標 準 局 員 工 消 合 作 社 印 製
No._Rj_XrX2-X3 3c-l Η 本紙張尺度適用中國國家標準(CNS ) Α4規格(210X297公釐) 100
-1UU 5 242 3 A7 B7 經濟部中央標準局員工消費合作社印製
本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 101 513422 A7 B7 五、發明説明(98
No. X1-X2-X3 3d-16 3d-17 3d-18 3d-19 3d-20 3d-21 3d-22 3d-23 3d-24 3d-25 3d-26
ch3 H CH3 H -^^-(ch2)4ch3 一 (ch2)3ch3 -NHCH3
-Br
請 閲讀背 之 注意事 項 經濟部中央標準局員工消費合作社印製
NaKa C2卜 外消旋體 外消旋髏 表3e COOR, •NHS02XrXrX3
No. R, 3e-l 1/2Ca c2h5
Br 外消旋體
XrXrX3 ~0~ch3 本纸張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 102 513422 A7 B7 五、發明説明(99 ) 上述化D物之物性值如下所不,另,上逑化合物N〇係指 相對應於表中化合物No.者
No.l a - 4 [a]D= -11.5° (CHC13,c=1.01,23.5t:).
No.l a - 5 [a]D= -10.0° (CHC13,c=1.01,25.0t:).
No.l a - 6 CDC13 300MHz 0.93-1.96(14H,m),2.20-2.26(3H,m),3.03j(lHlm),3.67(3H,s),4.99(lH,d,J=6.6Hz), 5.1〇.5.24(2H,m)>7.37.7.51(3H,m),7.54-7.64(3Hlm),7.76-7.88<2H,m),8-ll(lH>m ). IR(CHC13):3384,3278,3026,2952,2874,1727,1436,1411,1324,1155,1097 /cm. [a】D= ·9.0。(CHC13,c=1.04,22·0t:)·
No·l a - 7 CDC13 300MHz 0.93-2.00(14H,m),2.18(lH,m),2.28(2H,t,J=7.2Hz),3.04(lHrra)t5.15-5.25(2Hfm)f 5.28(lH,d,J=6.9Hz),7.36-7.50(3H,m),7.54-7.63(3H,m),7.76-7.89(2H,m), 8.12(lH,m). 經濟部中央標準局員工消費合作社印製 IR(CHC13):3268,3028,2952,2872,1708,1452,1410,1324,1155,1097 /cm· [a!D=-9.1。(CHCac^l.Ol.M.Ot^-
No· 1 a — 8 CDC13 300MHz 0.94-L99(UH,m),2.2i-2.29(3H,m),3.05(lH,m)I3.G7(3H,s),4.92(lH,dtJ=G.3Hz), 5.14-5.30(2H,m),7.70*7.78(6H,m),7.96-8.01(2H,m). 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐] '" 一 103 - 513422 A7 B7 五、發明説明(1〇〇) IR<CHC13):3376,3272,3018,2946,2868,1727,1616,1435,1388,1324,1162,1130,1 069 /cm.
[a]D=+1.60 (CHC13,c=1.01,24.0t:)· mp.ll7-119t:.
No.l a - 9 CDC13 300MHz 0.95-2.08(14H,m),2.19(lH,m), 2.32(2H,t,J=7.2Hz),3.06(lH,m),5.20-5.30(2H,m ),5.34(lH,d,J=6.6Hz),7.69-7.78(6H,m),7.96.8.03<2H,m). IR(CHC13):3260,3020,2950,2868,1708,1389,1324,1162,1130,1069 /cm.
[a]D= +13.3。(CHC13,c=1.05,24.0t:)· mp.llS-120t:
No.l a - 1 0 ' CDC13 300MHz 0.96-1.98(14H,m),2.15.2.32(3H,m),3.04(lH,m),3.66(3H,s),5.12. 5.26(5Hfm),7.67-7.78(4H,m),7.93-8.07(4H,m). IR(CHC13):3276,30IS,2946,2868,1726,1595,1435,1341,1162,1095 /cm.
[a]D= ·1.5° (CHC13,c=l.01,25.0t:). mp.l33-139X:.
No.l a - 1 1 CD30D 300MHz 經濟部中央標準局員工消費合作社印製 1.05-1.98(14H,m)(2.13-2.22(3H,m),2.97(lH,m),5.09.5.22(2H,m),7.85- 7.92(4H,m),7.95-8.05(4H,m). IR(KBr):3385,3261,3069,3003,2954,2872,1708,1596,1428,14 13,1378,1343,132 6,1236,1186,1160,1096 /cm. mp. 144 -146^1.
No.l a - 1 2 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 104 513422 A7 B7 五、發明説明(101 經濟部中央標準局員工消費合作社印製 CDC13 300MHz0.96-1.96(14H,m),2.22-2.27(3H,m),3.03(lH,m),3.66(3H,s),3.87(3H,s),4.86(lH,d,J=6.9Hz),5.18-5.24(2H,m),6.99-7.02(2H,m),7.55-7.66(2H,m),7.66.7.69<2H,in)f 7.89-7.92(2H,m). IR(CHC13):3374>3270,3016,2948,2870#1726,1608,1518,1487,145S, 1437,1248,1 157,1037. [a]D=+4.2° ((311013,0=1.01,24=). mp.85.87t:. No.l a — 1 3 CDC13 300iMHz 0.97-1.99(14H,m),2.18(lH,m),2.30(2H,t,J=7.2Hz),3.04(lH,m),3.86(3H,s),5.18( lH,d,J=5.7Hz),5.23-5.26(2H,m),6.99-V.02(2H,m),7.55-7.58(2H,m),7.66-7.6S(2 H,m),7.89-7.92(2H,m). IR(CHC13):3380,3260>3020>2948,2868,1708,1608,1519,14S7,145S,1306,1293>1 248,1156 /cm. [a]D=+18.3〇 (CHC13,c=1.00,25.5r). No.l a - 1 4 CDC13 300MHz 0.98-2.00(14H,m),2.20(lH,m),2.25(2H,t,J=7.2Hz),3.02(lH,m),3.67(3H,s),4.85( lH,d,J=6.3Hz),5.19-5.25(2H,m),7.13(lH,dd,J=4.8,3.6Hz),7.39(lH,d,J=4.8Hz), 7.40(lH,d,J=3.6Hz),7.71.7.74{2H,m),7.86-7.89(2H,m). IR(CHC13):3374,3270,3018,2946,2868,1727,1593,1434,1322/cm. [cr]D=+5.6° (CHC13,c=l.01,24=). mp.69-7lt:. '* j No.l a - 1 5 CDC13 300MHz (請先閱讀背面之注意事項再HI本頁) -裝· 訂 線 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 105 513422 A7 B7 五、發明説明(102 經濟部中央標準局員工消費合作社印製 0.95-2.00(14H,m),2.17(lH,m),2.32(2H,t,J=7.2Hz),3.03(lH,m),5.20(lH,d,J=6.9 Hz),5.24-5.2S(2H,m),7.13(lH,dd,J=4.8,3.3Hz),7.38(lH,d,J=4.8Hz),7.43(lH,d,J =3.3Hz),7.73(2H,d,J=8.4Hz),7.87(2H,d,J=8.4Hz). IR(CHC13):3260,3022,2948,2868,1709,1593,1404,1321,1154/cm. [a]D=+20.8° (CHC13,c=1.07,23t:).mp.71-73^3. No.l a — 1 6 CDC13 300MHz 0.98.2.00<14H,m)>2.27(2H,t>J=7.5Hz),2.28(lH,m),3.13(lH,m),3.66(3H,s),4.90( lH,d,J=6.9Hz),5.25-5.29(2H,m),7.40-7.65(6H,m),7.76(lH,d,J=S.4Hz),7.90-8.02 IR(CHC13):3376,3276,3018,2946,2868,1726,1593,1435,1394,1322,1159/cm. [a]D= +7.0° (CHC13,c=1.07,24t:). No.l a - 1 7 CDC13 300MHz 1.02-2.07(14H,m),2.25(lH,m),2.34(2H,t,J=6.6Hz),3.14(lH,m),5.2S-5.33(3H,m), 7.39-7.57(4H,m),7.62.7.65(2H,m),7.76(lH,d,J=8.1Hz),7.89.8.02(4H,m). IR(CHC13):3260,2948,2868,1709,1593,1394,1324,1157/cm. [a]D=+20.2〇 (CHC13,c=1.02,24t:). No.l a — 1 8 CDC13 300MHz 1.05-1.97(14H,m),2.25(2H,t,J=7.2Hz),2.33(lH,m),3.12(lH,m),3.67(3H.s),4.91( lH,d,J=6.6Hz),5.24-5.29(2H,m),7.24(lHtdfJ=3.9Hz),*7.39-7.45(3H,m),7.56(lH, d,J = 3.9Hz),7.59-7.62(2H,m). IR(CHC13):3372,3272,,30 18,2946,2868,1727,1433,133 1,1 152/cm. [alD=-5.7〇(CHC13,c=1.01,23X:). (請先閱讀背面之注意事項再本頁) -裝·
、1T 線 本紙張尺度適用中國國家標準(CNS ) A4規格(210 X 297公釐) 106 513422 A7 B7 五、發明説明(103
No.l a - 1 9 CDC13 300MHz 1.05- 2.05(14H,m),2.28-2.33(3H,m),3.13(lHfm),5.18(lH,d,J=6.3Hz),5.27-5.31(2 H,m),7.24(lH,d,J=4.2Hz)l7.39.7.42(3H,m),7.56(lH,d,J=4.2Hz),7.5S-7.62(2H,m ). m(CHC13):3372l3254,3018,2948,2868,n〇7,1431,1328,1151/cm. [a]D=+4.5〇 (CHC13,c=1.01,21.5t:). No.l a - 2 0 CDC13 300MHz 1.05- 2.00(14H,m),2.26(2H,t,J=7.5Hz),2.33(lH,m),3.11(lH,m),3.68(3H,s),4.92( lH,d,J=6.0Hz),5.27(2H,m),7.05(lH,m)’,7.10(lH,d,J=3.6Hz),7.25(lH,m),7.32(l H, m),7.49(lH,d,J=3.6Hz). IR(CHC13):3372,3272,3018,2946,2686,1727,1438,1417,1333,1151/cm. [a]D=-9.2〇 (CHC13,c=1.01,25t:). No.l a - 2 1 CDC13 300MHz I. 02-2.01(14H,m),2.28-2.34(3H,m),3.13(lH,m),5.12(lH,d,J=6.9Hz),5.28-5.32(2 H,m),7.06(lH,m),7.10(lH,d,J=3.9Hz),7.25(lH,m),7.32(lH,m),7.50(lH,d,J=3.9 Hz). IR<CHC13):3350,3250,2948,1709,1440,1420,1330,1151. [ctjD=十2·5〇 (011(:13/=1.00,251). (請先閱讀背面之注意事項再Jll本頁) 裝· 訂 -線 經濟部中央標準局員工消費合作社印製
No.l a — 2 2 CDC13 300MHz 0.96-2.05( 14H, m), 2.25( lH,m),2.35(2H,t,J=7.0Hz),3.11(1 H,m),5.20-5.34(2H,m), 5.41(lH,d,J=6.6Hz),7.31-7.49(5H,m),7.62(iH,d,J=7.8Hz),8.11(lH,d.d,J=1.8an 本纸張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 107 513422 A7 B7 五 、發明説明(仙 經濟部中央標準局員工消費合作社印製 d7.8Hz),8.35(lH,d,J=1.8Hz). IR(CHC13):3384,3271,3025,2958,1708,16O8,1559,1537,1357,1168/cm. [a]D=+l8.3(CHC13,C=0.31,22t:). No.l a — 2 3 CDC13 300MHz 0.97.2.07(14H,m),2.24(lH;in),2.35(2Hft,J=6.9Hz),3.09(lH,m),3.86(3Hfs),5.24. 5.35(2H,m),5.44(lH,d,J=6.3Hz),6.97.7.00(2H,m),7.26-7.28(2H,m),7.59(lH,d,J =8.lHz),8.06(lH,d.d,J=2.1and8.lHz),8.29(lH,d,J=2.lHz). IR(CHC13):3384,3270,2959,1709,1609,1535,1519,1357,1302,1255,1226,1169/c m. [a]D=+l7.0* (CHC13rC=1.00,2lt:). No.lNo.l a - 2 4 CDC13 300MHz 0.95.2.00(14H,m),2.20-2.25(lH,m),2.26(2H,t,J=T.2Hz),3.02-3.10(lH,m), 3.66(3H,s),4.92(lH)d,J=6.6Hz),5.16-5.31(2Hfm),7.52-7.60(3H,m),7.94- 8.06(6H,m). IR(CHC13):3376,3020,2946,2868,1726,1436,1366,1298,1164,1090,S90/cm. [a]D==+11.2±0.5· (CHC13,c=1.04,23.5t:.) mp. 101- 103*C No.l a — 2 5 CDC13 300MHz 0,95-2.08(14H,m),2.15-2.22(lH,m),2.33(2H,t,J=6.9Hz),3.02.3.10(lH,m),5.21, 5.31(2HIm)>5.34(lH,d,J=6.3Hz),7.51.7.59(3Htm),7.92.8.07(6H,m). IR(CHC13):3258,3022,2948,2868,1707,1399,1328,1298,1163,1089,105 1,892/cm [a ]D==+29.8 士 0.7· (CHCl3,c=1.05,25X)) 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 108 (請先閱讀背面之注意事項再m*本頁) 裝. 訂 線_ 513422 A7 B7 五、發明説明(1Q5 mp.l58-160t:
No.l a ~ 2 6
Anal. Calcd for C26H30N304SNa 0.8H2O:C,60.29;H,6.15;N,8.11;S,6.19;Na, 4.44.
Found:C,60.15;H,6.19;N,8.15;S,6.03;Na,4.98· [a]B= -16.6° (CHC13,c=1.04,25.0t:).
No.l a ~ 2 7 CDC13 300MHz 0.92-1.98(14H,m),2.20(lH,m),2.26(2H,t,J=7.5Hz),3.03(lH,m),3.12(6H,s),3.66( 3H,s),4.87(lH,d,J=6.6Hz),5.16-5.32(2H,m),6.73-6.80(2H,in),?.88-8.00(6H,m). IR(CHC13):3376,3020,2946,1726,1601,1518,1442,1419,1362,1312,1163,1133,1 088 /cm.
[a]D==+55.3。(CHC13,c=0.53,24.0t:)· mp.158.168X:
No.l a — 2 8 CDC13+CD30D 300MHz 0.99-2.14(14H,m),2.21(lH,m),2.31(2H,t,J=7.2Hz),2.94(lH,m),3.12(6H,s),5.22- 5.38(2H,m)f6.73.6.81(2H,m),7.87-8.00(6H,m). 經濟部中央標準局員工消費合作社印製 IR(KBr):3434,3309,2946,1708,1604,1520,1442,1416,1366,1312,1252,1164,115 5,1134,1091 /cm.
[ajD=無法测定(著色,能量不足) mp.193.196t:
No.l a — 2 9 CD30D 300MHz 1.02-1.96(l4H,m),2.10(2H,t,J=7.8Hz),2.16(lH,m),2.98(lH,m),3.1L(6H,s),5.07- 本纸張尺度適用中國國家標準(CNS ) A4規格(210X297公釐), 109 513422 A7 B7五、發明説明(106 ) 經濟部中央標準局員工消費合作社印製 5.27(2H,m),6.80-6.87(2H,m)>7.84.8.00(6H,m). IR(KBr):3433,3087,3004,2949,2871,1604,1565,1520,1444,1420,1364,1312,125 3,11638,1136,1090 /cm. [or]D=無法測定 No.l a — 3 0 CDC13 300MHz 0.95-1.99(14H,m),2.22(lH,m),2.26(2H,t,J=7.2Hz),2.35(3H,s),3.06(lH,m),3.66( 3H,s),4.95(lH,dfJ=6.9Hz),5.15-5.30(2H,m),7.26-7.32(2H,m),7.97-8.06(6H,m). IR(CHC13):3374,2996,2946,2868,1763,1728,1591,1495,1435,1368,1299,1228,1 192,1163,1139 /cm. [a]D==+12.9° (CHC13,c=1.04,26.0t:)· No.l a ~ 3 1 CDC13 300MHz 0.93-2.01(14H,m),2.19(lH,m),2.31(2H,t,J=7.2Hz),2.35(3H>s),3.06(lH,m),5.17- 5.32(2H,m),7.25-7.32(2H,m),7.96-8.07(6H,m). IR(CHC13):3267,3028,2952f2874,1759,1708,1592,1495,1368,1328,1299,1163,1 138,1088,1050,1008/cm. [a]D=+21.7* (CHC13,C=0.51,22t:). No.l a — 3 2 CDC13 300MHz 0.93· 1·99(14Η, m),2.2 l(lH,m),2.27(2H,t,J=7.2Hz),3.05(lH,m), 3.67(3H,s), 4.92( lH,d,J=6.6Hz),5.15-5.30(2H,m),6.72(lH,s)f6.96-7.00(2HIm)>7.86.8.04(6H>m). IR(CHC13):3374,3276>3〇 18,2946,2686,1725,1605,1589,1502,1433,1396,1330,1 j 271,1164,1135,1089 /cm· [a]D= +18.6° (CHC13,c=1.00,26.0t:). j No.l a - 3 3 丨 (請先閱讀背面之注意事項再—本頁) •装·
、1T 線 本纸浪尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) - 110 513422 經濟部中央標準局員工消費合作社印製 A7B7__ 五、發明説明(107 ) CDC13+CD30D 300MHz 0.98-2.08(14H,m),2.20(lH,m),2.28(2H,t,J=7.2Hz),2.98(lH,m),5.18-5.32(2H,m), 6.92-6.99(2H,m),7.85-8.02(6H,m). IR(KBr):3385,3248,2948,2876,1717,1601,1505,1430,1399,1296,1280,1219,116 5,1136,1092 /cm. [a]D= ·16·0° ((:Η3ΟΗ^=1·08,26·0Χ:)·. mp.208-210t: No.l a - 3 4 mp.82.83t: { a ]D=+10.6。(CHC13,c=1.01,23.5t:). No.l a — 3 5 : mp.80-82t: [a】D= ·1.8〇 (¢11013^=1.07,22.(^). No.l a — 3 6 TLC Rf=0.25 (醋酸乙酯 _n_ 己烷=1 : 1(〇.3%醋酸)) No.l a - 3 7 CDC13 300MHz 0.92-1.96(14H,m),2.21(lH,m),2.27(2H,t,J=7.4Hz),3.01(lH,m),3.66(3H,s),4.71( lHtd,J=6.6Hz),5.14.5.29(2H,m),7.12(lH>dlJ=16.2Hz),7.24(lH,dlJ=16.2Hz),7.2 8-7.42(3H,m),7.52.7.56(2Hfra),7.62(2H,dlJ=8.7Hz)f7.85(2H,d,J=8.7Hz). IR(CHC13):3384,3283,3023,2954,2876,1730,1595,1494,1317,1163,1147 /cm. [a】D=+10.5。(CHC13,c=1.01,24t:). mp 116-117 °C. No.l a - 3 8 CDC13 300MHz 0.92-1.99(I4H,m),2.17(lHtm),2.32(2H,t,J=7.2Hz),3.02(lH,m),5.23-5.29(3H,m), (請先閱讀背面之注意事項再本頁 裝· 訂 線 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 111 513422 A7 _____ B7五、發明説明(1〇8 ) 經濟部中央標準局員工消費合作社印製 7.11(lH,d,J=16.2Hz),7.23(lH,d,J=16.2Hz),7.28-7.41(3H,m),7.52-7.55(2Hfin),7. 61(2H,d,J=8.7Hz),7.86(2H,d,J=8.7Hz)? IR(CHC13):3515,3384,3270,3022,3015,2957,2876,2669,1708,1595,1496,1320,1 157 /cm. [o:】D=+27.r (011013/=1.02,241). No.l a — 3 9 CDC13 300MHz 0.92-1.99(14H,m),2.15(lH,m),2.28(2H,t,J=7.4Hz),3.01(lH,m),3.68(3H,s),4.96( lH,d,J=6.6Hz),5.16-5.32(2H,m),6.60(lH,d,J=12.0Hz),6.74(lH,d,J=12.0Hz),7.1 6-7.23(5H,m),7.35(2H,d,J=8.4Hz),7.72(2H,d,J=8.4Hz). IR(CHC13):3384,3283,3023,3015,2954,2876,1730,1595,1493,1324,1163,1147 /cm. [a]D=+13.7e (CHC13,c=1.00,24t:)· No.l a - 4 0 CDC13 300MHz 0.90-2.16(14H,m),2.12(lH,m),2.34(2H,t,J=7.2Hz),3.02(lH,m),5.16(lH,d,J=6.9 Hz),5.23-5.34(2H,m),6.60(lH,d,J=12.3Hz),6.74(lH,d,J=12.3Hz),7.14-7.24(5H, m),7.35(2H,d,J=8.lHz),7.72(2H,d,J=8.lHz). IR(CHC13):3515,3384,3269,3025,3021,3014,2957,2876,2668,1709,1595,1322,1 162,1147 /cm. [a】D=+26.4e (CHC13,c=1.00,24t:)· No.l a — 4 1 CDC13 300MHz | I 0.98-1.99(14H,m)f2.17(lH,m),2.32(2H,t,J=7.2Hz),3.00(lHtm),3.84(3Hfs),5.20. :1 5.26(3H,m),6.90-6.95(2H,m),6.98(lH>d,J=16.2Hz)>7.17(lH,dfJ=16.2Hz)f7.46- 7.49(2H,m),7.58(2H,d,J=8.4Hz),7.83(2H,d,J=8.4Hz). (請先閱讀背面之Ϊ事項再nf. 本頁)
、-IT 線 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 112 513422 A7 B7 五、發明説明(109) 經濟部中央標準局員工消費合作社印製 IR(CHC13):3258,3018,3002,2950,1709,1590,1509,1457,1404,1302,1250,1153 /cm. [or】D=+30.2e (ΟΗα3,ο=1·00,23Χ:). mp.99-100 No.l a — 4 2 CDC13 300MHz 1.0M.99(14H,m),2.28(2H,t>J=7.2Hz),2.30(lHlm),3.10(lH,m),3.66(3H,s),5.07( 1H,br),5.25-5.30(2H,m),6.98-7.04(2H,m),7.16(lH,d,J=16.2Hz)>7.28-7.37(3H,m), 7.47-7.50(3H,m). IR(CHC13):3372,3276,3020,2946,2870,1727,1491,1433,1331,1152 /cm. [<x]D= ·11·5。(ΟΗΟαο^Ι.ΟΤβΙ.δΧ^- Νο.Ι a — 4 3 CDC13 300MHz 0.98-2.00(14H,m),2.11-2.36(3H,m),3.12(lH,m)l5.10(lH,d,J=6.6Hz),5.29-5.32(2H,m),6.99-7.04(2H,m),7.23(lH,d,J=21.6Hz),7.32.7.49(6H,m). IR(CHC13):3380,3248,3020,2948,2868,1709,1491,1430,1329,1151/cm. [a]D=+3.40 (CHC13,c=1.03,25t:>· No.l a - 4 4 CDC13 300MHz 1.00-2.00(14H,m),2.13(lH,m),2.29(2H,t,J=7.4Hz),2.90-3.13(5H,m),3.68(3H,s), 4.74(lH,d,J=6.6Hz),5.15-5.30(2H,m),7.18-7.29(7H,m),7.76(2H,d,J=8.1Hz). IR(CHC13):3384,3282,3063,3028,3023,3016,2953,2876,1730,1599,1496,1319,1 157 /cm. I [a]D=+2.3〇 (CHC13,c=1.00>25t:). mp.85.0-86.0^ 本纸張又度適用中國國家標準(CNS ) A4規格(210X 297公釐) (請先閲讀背面之注意事項再頁) -裝.
、1T 線 113 513422 A7 B7 五、發明説明(110 經濟部中央標準局員工消費合作社印製
No.l a — 4 5 CDC13 300MHz 0.90-2.05(14H,m),2.09(lH,m),2.35(2H,t,J=6.9Hz),2.90-3.13<5H,m),5.18(lH,d,J =6.6Hz),5.24-5.34(2H,m),7.10-7.27(7H,m),7.76(2H,d,J=8.4Hz). IR(CHC13):3510,3384,3270,3087,3063,3026,3018,3014,2955,2876,2670, Π〇8,1 599,1496,1318,1157/cm. [a]D=+8.5〇 <CHC13,c=1.01,25t:)e No.l a - 4 6 [a】D=+6.S° (CHC13,c=1.05,25t:)· mp.99-100t:. No.l a — 4 7 .. CDC13 300MHz 0.97.2.01(14H,m),2.14(lH,m),2.36(2H,t,J=7.2Hz),3.02(lH,m),5.23(lH,d,J=5.4 Hz),5.26-5.30(2H,m),7.37-7.39(3H>m),7.54.7.58(2H,m),7.63-7.66(2H,m),7.85-7. 88(2H,m). IR(CHC13):3375,3260,3022,2948,2212,1707,1596,1497,1396,1322,1160/cm. [〇f]D=+25.0° (CHC13,c=1.02,24t:). mp.ll7-118t:. No.l a - 4 8 CD30D 300MHz 1.05-1.93(14H,m),2.10.2.15(3H,m)(2.96(lH,m),5.08-5.28(2HIm),7.38-7.40(3H> m),7.554-7.56(2H,m),7.69(lH,d,J=8.4Hz),7.87(lH,d,J=8.4Hz)· No.l a - 4 9 CDC13 300MHz 0.96-l,97(14H,m),2.24(lH,m),2.31(2H,t,J=6.9Hz),3.05(lH,m),3.69(3H,s),5.15( lH,d,J=6.6Hz),5.25-5.27(2H,m),7.4〇.7.43(3H,m)f7.61-7.64(2H,m),7.85(lH,d,J =8.lHz),8.07(lH,dd,J=8.1,1.8Hz),8.58(lH,d,J=1.8Hz). (請先閱讀背面之注意事項再本頁)
、1T 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 114 513422 A7 B7 五、發明説明(111 ) IR(CHC13):3374,3020,2948,2870,2212,1726,1606,1530,1493,1437,1345,1167/c m.
[cr]D=+2.4° (CHC13,c=1.03,25t:)· mp.77-79^C.
No.l a — 5 0 CDC13 300MHz 1.00.2.02(14H,m),2.20(lH,m),2.34(2H,t,J=6.6Hz),3.08(lH,m),5.26-5.29(2H,m), 5.41(lH,d,J=6.9Hz),7.40-7.43(3H,m),7.61-7.64(2H,m),7.84(lH,d,J=8.lHz),8.07 (lH,dd,J=8.4,1.8Hz),8.57(lH,dd,J=1.8Hz). IR(CHC13):3380,3254,2952,2880,2212,1707,1606,1531,1493,1409,1344,1166. [a]D=+23.4〇 (CHC13,c=1.00,25t:).
No.l a — 5 1 CDC13 300MHz 0.95-1.98(14H,m),2.23(lH,m),2.30(2H,t,J=7.2Hz),3.00(lH,m),3.66(3H,s),4.56( 2H,br),4.70(lH,d,J=6.9Hz),5.20.5.29(2H,m),7.15(lH,dd,J=7.8,1.8Hz),7.23(lH, d,J=1.8Hz),7.36-7.39(3H,m),7.46(lH,d,J=7.8Hz),7.53-7.56(2H,m)· IR(CHC13):3494,3386,3028,2952,2874,1725,1611,1559,1497,1422,1317,1162/c
No.l a ~ 5 2 CDC13 300MHz 0.96-2.04(16H,m),2.20(lH,m),2.36(2HftfJ=6.9Hz),2.99(lH,m)>5.17(lH,d,J=6.3 經濟部中央襟準局員工消費合作社印製
Hz),5.28-5.31(2H,m),7.18(lH,dd,J=9.6,1.8Hz),7.25(lH,m),7.36-7.39(3H,m),7.4 6(lH,d,J=7.8Hz),7.52-7.56(2H,m)· IR(CHC13):3482,3378,3260,3022,2948,2868,1708,161 2,1495,1422,1317/cm.
[a]D=-fl5.0° (CHC13,c=1.00,24t:). 本紙張尺度適用中國國家標準(CNS ) A4規格(2丨〇'乂297公釐) 115 513422 A7 B7 五、發明説明(112 )
No.l a — 5 3 CDC13 300MHz 1.01.2.05(15H,m)l2.31(2H,t,J=7.2Hz),3.10(lH,m),3.67(3H,s),5.02(lH,br),5.26-5.33(2H,m),7.18(lH,d,J=4.2Hz),7.36-7.39(3H,m),7.48(lH,d,J=4.2Hz),7.51-7.5-5 (2H,m)· IR(CHC13):3372,3270,3018,3004,2946,2868,2202,1726,1486,1433,1336,1154/ cm.
[a]D=+〇.6° (ΟΗ013,ο=1.11,25ΐ:), [a]436 +17.8° (CHC13,c=l.ll,25iC).
No.l a — 5 4 CDC13 300MHz 0.99-2.11(14H,m)l2.27(lH,m),2.37(2H,t,J=7.5Hz),3.13(lH,m),5.16(lH,d>J=6.6
Hz),5.31-5.35(2H>m)f7.18(lH,d,J=3.6Hz),7.37.7.39(3H,m),7.50(lH,d,J=3.6Hz), 7.52-7.55(2H,m). IR(CHC13):3484,3370,3246,2948,2868,2202,1708,1486,1429,1335,1153/cm. [a]D=+17.8〇 (ΟΗ013,〇=1.00,24Χ:). mp.95-96t:
No.l a — 5 5 CDC13 300MHz 0.95-1.92(14H,m),2.15(lH,m),2.24(2H,t,J=7.5Hz),3.00(lH,m),3.66(3H,s),5.10-5.30(3H,m)>7.40-7.60(7H>m),7.70(lH,dlJ=7.8Hz),8.08(lH,d,J=8.lHz). IR(CH C13):3356,3020,2948,2868,2210,1727,1490,1458,1437,1341,1165/cm.
[a 】D=-58.4e ((^013,(:=1.00,261). mp.84-85t:.
No.l a — 5 6 CDC13 300MHz 0.95-L95(14Hfm),2.10(lH,m),2.27(2H,t,J=6:9Hz),3.00(lH,m),5.17-5.21(2H,m), 5.38(m,d,J=6.9Hz),7.39-7.60(7H,m),7.70(lH,dd,J=7.8,1.5Hz),8.07(lH,J=6.6,l. 5Hz). 本紙張尺度適用中國國家標準(CNS ) A4規格(210 X 297公釐) (請先閱讀背面之注意事項再
經濟部中央標準局員工消費合作社印製 116 513422 A7 B7 五、發明説明(113) 經濟部中央標準局員工消費合作社印製 IR(CHC13):3364,3026,2952,2874,2212,1707,1597,1491,1458,1411,1341,1164/cm. [a]D=-43.1° (CHC13,c=1.00,25t:). No.l a — 5 7 CDC13 300MHz 0.99.1.97(14H,m),2.23.2.30(3H,m),3.01(lH,m),3.67(3H,s),5.17-5.26(3H,m),7.3 6.7.38(3H,m),7.50-7.56(3H,m),7.60(lH,m),7.83(lH,m),8.05<lH,m). IR{CHC13):3376,3020,2946,2870,1727,1598,1491,1437,1412,1330,1245,1163/ cm. [a】D=-12.7e (CHC13,c=1.00,24t:). No.l a — 5 8 CDC13 300MHz 0.97-1.98(14H,m),2.20(lH,m),2.33(2H,t,J=6.9Hz),3.02(lH,m),5.19-5.28(3H,m), 7.36-7.38(3H,m),7.47-7.55(3H,m),7.69(lH,m),7.83(lH,m),8.04(lH,m)· IR(CHC13):3376,3260,3022,3002,2948,2868,2220,1708,1598,1490,1455,1412,1 327,1162/cm. [〇f]D=-8.6。(CHC13,c=1.01,24t:)· No.l a — 5 9 CDC13 300MHz 0.95· 1.99(24H,m),2.20(lH,m),2.28(2H,t,J=7.8Hz),2.53(lH,s),2.S)6(lH,m),3.69( 3H,s),4.99(lH,d,J=6.6Hz),5.18-5.20(2H,m),7.53(2H,d,J=8.4Hz),7.82(2H,d,J=8. j 4Hz). I I IR(CHCI3):3583,3376,3002,2936,2852,1725,159 1,1490, H37.1393,1325,1160/ cm. [arjD=-8.8e (CHa3,c=1.00,24T:). (請先閲讀背面之注意事項再本頁) 裝·
、1T 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 117 513422 經濟部中央標準局員工消費合作社印製 A7 B7_ _五、發明説明(114 ) No.l a — 6 0 i CDC13 300MHz 0.96-2.05(24H,m),2.22(lH,m),2.33(2H,m),2.88(lH,m),5.22-5.26(2H,m),5.30(lH,; d,J=5.7Hz),7.50(2Hfd,J=8.7Hz),7.80(2H,d,J=8.7Hz). IR(CHC13):3376,3260,3022,2936,2852,1710,1592,1491,1452,1395,1325,1159/c | j m. [a]D=-8.9〇 (CHC13,c=1.06,24t:), mp.88-91^3 No.l a - 6 1 CDC13 300MHz 0.95-2.24(23H,m),2.29(2H,m),2.99(lH,m),3.69(3H,s),4.76(lH,d,J=6.3Hz),5.21· 5.24(2H,m),6..28(lH,m),7.50-7.53(2H,m),7.77.7.80(2H,m). IR(CHC13):3374,3270,3018,2942,2868,2196,1726,1589,1490,1435,1324,1158/0 m. [a]D=+7.7〇 (CHC13,c=1.02,24t:), mp.93-95t: No. 1 a — 6 2 CDC13 300MHz 0.96-2.45(23H,m),2.36(2H,d,J=6.9Hz),2.99(lH,m),5.24(lH,d,J=6.3Hz),5.24-5.3 2(2H,m),6.28(lH,m),7.5〇.7.53(2H,m),7.78-7.81(2H,m). IR(CHC13):3468,3374, 3260,3020,2942,2868,2196,1598,1490,1455,1398,1322,1157/cm. [or]D=+19.4° (CHC13,c=1.03,24t:). No. 1 a — 6 3 CDC13 300MHz 0.93-1.95(25H,m),2.16(lH,m),2.29(2H,t,J = 7.2Hz),2.43(2H,t,J=6.9H2〇,2.94(lH, m)(3.G9(3H,s)I4.95(lH,dtJ=6.9Hz)l5.21.5.24(2H,m),7.49(2H,d,J=8.7Hz),7.79(2 H,J=8.7Hz). (請先閱讀背面之注意事項再本頁) .裝· 訂 線 本纸張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 118 513422 A7 B7 五、發明説明(115 IR(CHC13):3376,3018,2946,2866,2222,1727,1592,1456,1435,1325,1158/cm. [a]D=+3.79 (CHC13,c=1.00,25t:). No.l a - 6 4 CDC13 300MHz 0.93-1.97(26H,m),2.35(2H,t,J=7.2Hz),2.43(2H,t,J=7.2Hz),3.0O(lH,m),5.08(lH, d,J=6.6Hz),5.26.5.27{2H,m),7.49(2Hld,J=8.7Hz),7.78(2H,d,J=8.7Hz). IR(CHC13):3260,3020,2948,2864,2222,1708,1592,1489,1456,1397,1324,1156/c m. [a 】D=+14.4e (CHC13,c=1.00,25t:) mp.70-7lt: · 請 先 閎ik 背 之 注 意 項 再 m 本 頁 裝 經濟部中央標準局員工消費合作社印製
No.l a - 6 5 CDC13 300MHz 0.95-1.98(14H,m),2.18(lH,m),2.30(2H,t,J=7.2Hz),3.00(lH,m),3.67(3H,s),4.83( lH,d,J=6.9Hz),5.22-5.25(2H,m),5.54(lH,br),6.82-6.85(2H,ra)l7.42.7.45(2H>m), 7.59-7.62(2H,m),7.82-7.85(2H>m). IR(CHC13):3576,3374,3018,2946,2868,2208,1725,1607,1587,1514,1435,1325,1 270,1162,1133/cm. [a]D=+9.1° (CHC13,c=1.03,24t:), mp.lll-112r No.l a — 6 6 CDC13 300MHz 0.97-2.03(14H,m),2.15(lH,m),2.35(2H,t,J=7.5Hz),3.00(lH,m),5.17(lH,d,J=6.6 Hz),5.26-5.30(2H,m),6.82-6.85(2H,m),7.42-7.45(2H,m),7.59-7.62(2H,m),7.82-7. 85(2H,m). IR(CHC13):3260,2948,2870,2203,1709,1607,1587,1514,139G. 1325,1270· 1162,1 133/cm. [ajD二·21.0〇 (CHC13,c=1.00,23t:), mp.161.162t: 訂 ►線 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 119 513422 A7 B7 五、發明説明(116 經濟部中央標準局員工消費合作社印製
No.l a — 6 7 CDC13 300MHz 0.95-1.98(14H,m),2.20(lH,m),2.29(2H,t,J=7.2Hz)>3.01(lH,m),3.67(3H,s),4.82( lH,d,J=6.6Hz),5.19-5.27(2H>m),7.05-7.10(2H,m),7.51-7.56(2H,m),7.61-7.64(2 H,m),7.84-7.87(2H,m). IR(CHC13):3374,3280,3020,2946,2868,2214,1727,1589,1509,1435,1327,1233,1 161,1134/cm. [a]D=+6.7° (CHC13,c=1.01,24t:),mp.84-85t: No.l a - 6 8 CDC13 300MHz 0.96-2.01(14H,m),2.15(lH,m),2.34(2H,t,J=6.9Hz),3.02(lH,m),5.23-5.27(3H,m), 7.04·7.10(2Η,ιη),7.51·7·56(2Η,ιη),7.61·7.64(2Η,ιη),7.85·7,88(2Η,πι). IR(CHC13):3374,3258,3020,2948,2868,2214,1708,1589,1509,1455,139S, 1322,1 156/cm. [a ]D=+22.6° No.l a - 6 9 CDC13 300MHz 0.95-L98(14H,m),2.19(lH,m),2.29(2H,t,J=7.2Hz),2.39(3H,s),3.01(lH,m),3.69( 3H,s),4.80(lH,d,J=6.6Hz),5.20-5.29(2H,m),7.18(2H,d,J=8.lHz),7.44(2H,d,J=8. lHz),7.62(2H,d,J=8.4Hz),7.84(2Htd,J=8.4Hz). IR(CHC13):3374,3022,2946>2868I2210,1727,1589,1511,1436,1323,1161,1133/c m. [a]D=+9.2〇 (CHC13,c=1.02,2‘ir). mp. 116-118*C
No. 1 a - 7 0 CDC13 300MHz 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) (請先閱讀背面之注意事項再本頁) -裝· 訂 線 120 513422 A7 B7 五、發明説明(117) 經濟部中央標準局員工消費合作社印製 1.15-2.00(14H,m),2.13(lH,m),2.33-2.38(5H,m),3.04(lH,m),5.14(lH,d,J=6.6Hz), 5.25-5.30(2H,m),7.17(2H,d,J=7.8Hz),7.44(2H,d,J=7.8Hz),7.62(2H,d,J=8.4Hz), 7.85(2H,d,J=8.4Hz). IR(CHC13):3380,3260,3020,2948,2868,2210,1708,1590,1511,1396,1324,1160,1 133/cm. [a]D=+24.6〇 (CHC13,c=1.00,24t:). No.l a - 7 1 CDC13 300MHz 0.95.1.96(14H,m),2.19(lH,m),2.29(2H,t,J=7.2H2),3.00(lH,m),3.20(lH,s),3.65( 3H,s),4.81(lH,d,J=6.6Hz),5.2〇.5.27(2H,m),7.46-7.54(4H,m),7.62.7.65(2Hfm),7. 85-7.88(2H,m). IR(CHC13):3374,3290,3018,3002,2946,2868,2212,2110,1726,1591,1507,1435, 1401,1324,1161/cm. [a]D=+9.6° (CHC13,c=1.01,24t:),mp.136.138t:, No.l a — 7 2 CDC13 300MHz 0.96-2.01(14H,m),2.14(lH,m),2.35(2H,t,J=7.2Hz),3.05(lH,m)>3.20(lH,s),5.16( | 1H,d, J=7.2Hz), 5.26-5.29(2H,m),7.45-7.53(4H,m),7.63(2H,d,J=8.4Hz),7.87(2H, d,J=8.4Hz). IR(CHC13):3462,3374,3290,3024,2948,2868,2212,2 110,1708,1591,1508,1455,1 401,1321,1274,1160,1132/cm. [a 】D=+24.3e (0^1013,0=1.03,241), 11^.96-991 No.l a ~ 7 3 CDC13 300MHz 0.95-1.98(14H,m),2.19(lH,m),2.27.2.32(5H,m),3.01(lHtm),3.67(3Hls),4.80(lH, d,J=6.6Hz),5.2〇.5.27(2H,m),7.12(2H,m),7.56(2H,m),7.63(2H(m),7.84(2Hfm). IR(CHC13):3374,3276,3018,2946,2868,2214, Π62,1730,1589,1506,1435,1368,1 (請先閱讀背面之注-ή思事項再HI本頁) 裝· 訂 -線 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 121 513422 A7 B7 五、發明説明(118 經濟部中央標準局員工消費合作社印製 161/cm. [a]D=+7.8° (CHC13,c=1.02,24t:),mp.102-104*0 No.l a ~ 7 4 CDC13 300MHz 0.95-2.05(14H,m),2.15(lH,m),2.32.2.37(5Hrm),3.02(lH,m),5.14(lH,d,J=6.6Hz), 5.26-5.30(2H,m),7.10-7.13(2H,m),7.54-7.57(2H,m),7.62-7.64(2H,m),7.84-7.87( 2H,m). IR(CHC13):3482,3250,3022,2946,2868,2214,1716,1709,1589,1507,1454,1396,1 368,1322,1195,1161/cm. [a]D=+15.0〇 (CHC13,c=1.00,24t:),mp.l29-13lt: No.l a — 7 5 CDC13 300MHz 0.95-1.99(14H,m),2.20(lH,m),2.30(2H,t,J=7.2Hz),3.02(lH,m),3.67(3H,s),3.94( 3H,s),4.79(lH>d,J=6.6Hz),5.19.5.29(2H,m),7.60-7.63(2H,m),7.65-7.67(2H,m),7. 86-7.89(2H,m),8.04-8.06(2H,m). IR(CHC13)..3378,3018,2946,2380,1720,1604,1435,1307,1276,1161,1106 /cm. [a]D=+7.3° (CHC13,c=1.01,25t:),mp.132.133t: No.l a - 7 6 CDC13+CD30D 300MHz 1.04-2.05(14H,m),2.19(lH,m),2.32(2H,t,J=6.9Hz),2.93(lH,m),5.27-5.3U2H,m), 7.60-7.63(2H,m),7.65-7.68(2H,m),7.86-7.89(2H,m),8.05-8.O7(2H,m). IR(CHC13):3402,3299,2955,2876,2665,2549,1455,1422,1313,1281,U64 /cm. [a]D=-21.1° (CH3OH,c=1.03,23X:)t mp.227-229(dec.)
No.l a - 7 7 CDC13 300MHz 本纸張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) (請先閱讀背面之注意事項再Jll本頁) •裝·
、1T 線_ 122 513422 A7 _____B7五、發明説明(119 ) 經濟中央標準局員工消費合作社印製 0.96.1.99(14H,m),2.20(lH,m),2.30(2H,t,J=7.2Hz),3.02(lH,m),3.68(3H,s),4.88( lH,d,J=6.3Hz),5.19-5.29(2H,m),7.67-7.72(4H,m),7.89-7.91(2H,m),8.24-8.27(2 H,m). IR(CHC13):3376,3276,3020,2946,2870,2214,1726,1594,1519,1455,1435,1389, 1344,1161/cm. [a]D=+7.7° (CHC13,c=1.02), mp.87-89t: No.l a — 7 8 CDC13 300MHz 0.98-2.00(14H,m),2.18(lH,m),2.34(2H,t,J=7.2Hz),3.02(lH,m),5.24-5.28(2H,m), 5.32(lH,d>J=5.7Hz),7.67-7.72(4H,m),7.89-7.92(2H,m)>8.23-8.26(2H,m). IR(CHC13):3374,3260,2948,2214,1708,1595,1344,1160/cm. [a]D=+23.3e (CHC13,c=1.00), mp.102-103^: No.l a ~ 7 9 0.93-2.02(14H,m),2.13(lH,m),2.36(2H,t,J=7.1Hz),3.05(lH,m),3.84(3H,s),5.18( 1H,br),5.27-5.31(2H,m),6.88-6.91(2H,m),7.48-7.50(2H,m),7.60-7.63(2H,m),7.8 3-7.85(2H,m). IR(CHC13):3380,3252,3020,2950,2868,2208,1708,1589,1511,1457,1396,1321,1 286,1160/cm. [a 】D=+26.7。(CHC13,C=l.〇〇). mp.75.77t: No.l a — 8 0 CDC13 300MHz 0.96-L99(14H,m),2.21(lH,m),2.30(2H,t,J=T.8Hz),3.02(lH,m)t3.68(3H,s),4.80( lH,d,J=6.6Hz),5.19-5.28(2H,m),7.51-7.77(5H,m),7.87'7.90(2H,m),8.13(lH,m). IR(CHC13):3374,3270,3013,2946,2868,2216,1726,1607,1567,1527,1495,1456,1 本纸張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) (請先閱讀背面之注意事項 本百〇 .裝· 、-ιτ 絲 123 ~ 513422 A7 B7 五、發明説明(12〇 ) 436,1344,1296,1161/cm. [a]D=+7.4° (CHC13,c=1.00,22t:), 1^.68-701 No.l a - 8 1 CDC13 300MHz 0.97-2.01(14H,m),2.16(lH,m),2.34(2H,t,J=7.2Hz),3.01(lH,m),5.22.5.28(3H,m), 7.51(lH,m),7.65(lH,m)7.70-7.76(3H,m),7.88.7.91(2H,m),8.12(lH,dd,J=6.9Hz, 1.5Hz). IR(CHC13):3480,3382,3262,3026,2952,2872,2218,1708,1607,1567,1526,1396,1 343,1225,1160/cm. [a]D=+22.0〇 (CHC13,c=1.00), mp.92-94t: No.l a — 8 2 CDC13 300MHz 0.95-1.98(14H,m),2.20(lH,m)>2.29(2H,t,J=7.2Hz),3.01(lH,m),3.67(3H,s),4.30( 2H,br),4.79(lH,d,J=6.9Hz),5.20-5.29(2H,m),6.71-6.76(2H,m),7.18(lH,m),7.37( lH,dd,J=7.8,1.2Hz),7.61-7.65(2H,m),7.83-7.87(2H,m). IR(CHC13):3376,3020,2946,2868,2202,1725,1613,1589,1484,1454,1315,1253,1 161/cm. [a]D=+8.9° (ΟΗαΐ3,ο=1.00,22Χ:). mp.ee-TOt: (請先閱讀背面之注意事項再本頁) •裝· 訂 線 經濟部中央標準局員工消費合作社印製
No.l a ~ 8 3 CDC13 300MHz 0.97-1.99(14H,m),2.17(lH,m),2.33(2H,t,J=6.9Hz)f2.99(lH,m),5.20.5.28(2H,m), 5.37(lH>d,J=6.9Hz),6.45(2Hfbr),6.71-6.76(2H,m)f7.19(lHfdd,J=7.8,6.6Hz),7.3 7(lH>m),7.62(2H,dlJ=8.4Hz),7.85(2H,d,J=8.4Hz). IR(CHCU3):3478,3378,3260,3022,2950,2868;2204,1708,1613,1589|1484T1454,1 396,1316,1160/cm. [crjD=+n.r (CHC13,c=1.01)· 本紙張尺度適用中國國家標準(CNS ) Α4規格(210Χ 297公釐) 124 513422 A7 B7 五、發明説明(121) Νο·1 a — 8 4 CDC13 300MHz 1.00-2.08(14H,m),2.21(lH,m),2.37(2H,t,J=6.9Hz),3.06(lH,m),3.86(3H,s),5.29· 5.33(2H,m),5.45(lH,d,J=6.6Hz),6.91-6.94(2H,m),7.56-7.59(2H,m),7.81(lH,d.t, J=8.1Hz),8.04(lH,d.d,J=8.1&1.8Hz),8.57(lH,d,J=2.lHz). IR(CHC13):3492,3254,3028,2954,2202,1708,1597,1512,1344,1291,1250/cm. [a]D=+27.4° (CHC13,C=0.53,23t:).
No.l a — 8 5 CDC13 300MHz 0.96-2.05(14H,m),2.20(lH,m),2.35(2H,t,J=6.9Hz),2.99(lH,m),3.84(3H,s),5.22-5.31(3H,m),6.89(2H,d,J=8.7Hz),7.19(lH,brs),7.29(lH,brs),7.45-7:50(3H,m)· IR(CHC13):3478,3378,3020,2950,2868,2202,1708,1606,1511,1421,1311,1287,丨 1248,1155/cm. [a]D=+17.1e (CHC13,C=1.00,23t:)· No.l a — 8 6 CDC13 300MHz 1.03-2.05(14H,m),2.21(lH,m),2.37(2H,t,J=6.9Hz),3.04(lH,m),5.29.5.33(2H,m), 5.57(lH,d,J=6.3Hz),6.84.6.87(2H,m),7.50-7.53(2H,m),7.79(lH,d,J=8.lHz),8.03 (lH,d,d,J=L5and8.1Hz),8.57(lHfd,J=1.5Hz). IR(CHC13):3250,3024,2950,2868,2200,1707,1515,1344,1271,1166,1143/cm. [cr]D=+21.2° (CHC13,C=0.26,22t:)· (請先閲讀背面之注意事項再本頁) •裝_ 訂 線 經濟部中央標準局員工消費合作社印製
No.l a - 8 7 CD30D 300MHz 1.04-2.00(14Hfm)>2.18(lH,m),2.26(2Hft,J=5.4Hz),2.93(lHfm),5.19-5.24(2H,m)> 6.77-6.80(2H,m),7.05(lH,d.d,J=2.1and8.lHz),7.22(lH,d,J=2.lHz),7.38-7.42(3 本紙張尺度適用中國國家標準(CNS ) A4規格(21〇X 297公釐) 125 513422 A7 B7五、發明説明(122) 經濟部中央標準局員工消費合作社印製 H,m)· IR(CHC13):3377,2952,2873,2204,1705,1607,1515,1425,1312,1267,1222,1153/ cm. [a]D=-15.6° (CH3OH,C=1.02,22t:)· No.l a — 8 8 CDC13 300MHz 0.9〇.1.96(14H,m),2.22-2.31(3H,m),2.95(lHfm),3.65(3H,s),4.87(lH,cl,J=6.6Hz), 5.13.5.28(2H,m),7.46-7.62(3H,m),7.82-7.89(4H,m),7.90.7.96(2H,m),8.42(lH,br s)· IR(CHC13):3376,3016,2946,2868,1720,1677,1592,1514,1498,1429,1376,1314,1 241,1156,1094 /cm. ; [a】D= -10.7。((:11(:13,0=1.04,22.01) mp.l34-136t: No.l a — 8 9 CDC13+CD30D 300MHz 0.96-2.08(14H,m),2.23(lH,m),2.28(2H,t,J=7.2Hz),2.89(lH,m),5.20-5.32(2H,m), j 7.46-7.62(3H,m),7.82.7.97(6H,m). IR(KBr):3272,3007,2952,2874,1708,1660,1592,1527,1498,1433,1400,1317,126 0,1152,1094 /cm. [a】D= ·24.4。(¢^3011,0=1.02,25.01)0 No.l a ~ 9 0 CDC13 300MHz 0.89-1.96(14H,m),2.23-2.33(3Hlm),2.92(lH>m),3.67(3H,s),4.85(lH>dlJ=6.3Hz), j 5.10.5.25(2H,m),7.81-7.90(4H,m),8.10-8.18(2H,m),8.31-8.40(2H,m),8.77(lH,s)· | IR(CHC13):3372,3018,2946,2868,1718,1685; 1592,1527,1436,1397,1346,1318,1 256,1154,1099 /cm. [a]D= -16.Γ (CHC13,c=l.00.23.Ot:), (請先閱讀背面之注意事項再本頁) 、言 本紙張尺度適用中國國家標準(CNS ) A4規格(2l〇x 297公釐) 513422 一五 .__ 經濟部中央標準局員工消費合作社印製 A7 B7 發明说明(123 Νο·1 a - 9 1 CDC13+CD30D 300MHz 0.94-2.02(14H,m),2.18-2.36(3H,m),2.87(lH,m),5.15·5·30(2Η,πι),7.82-7.92(4H, ! m),8.09-8.16(2H,m),8.30-8.37(2H,m). ! IR(KBr):3284,3112,3006,2952,2874,1707,1593,1528,1498,1399,1348,1320,125 1 9,1153,1093 /cm.
[o:]D= ·26.3° (CH3OH,c=1.01,22t:)·
No.l a - 9 2 CDC13 300MHz 0.93-1.95(14H,m),2.22-2.31(3H,m),2.98(lH,m),3.68(3H,s),5.07(lH,d,J=6.9Hz), 5.10-5.24(2H,m),7.18(lH,m),7.35-7.43(2H,m)f7.70(2H,d,J=7.8Hz),7.88.8.05(4 H, m),8.50(lH,brs). IR(CHC13):3382,3008,2952,1720,1675,1599,1525,1499,1438,1321,1253,1161,1 087 /cm.
[a]D= ·16·6° (ΟΗ(:13/=1·03,24.0Χ:) mp.lOO-lOlC No.l a — 9 3 CDC13+CD30D 300MHz 0.96-2.00(14H,m),2.18-2.35(3H,m),2.90(lH,m),5.15-5.30(2H,m),7.18(lH,m),7.3 3-7.42(2H,m)l7.65-7.74(2Hfm),7.90-8.08(4H,m). IR(KBr):3347,3194,3011,2955,2875,1706,1650,1602,1544,1499,1443,1325,12 65,1165,1091 /cm.
[a】D= -19.4° (CH30H,c=1.00,24.0t:) 1^.158-159=
No.l a — 9 4 CD30D 300MHz ; I. 05-2.00(14H,m),2.14(lH,m),2.23(2H,t,J=7.2Hz),2.98(m,m),3.80(3H,s),5.13·; (請先閱讀背面之注意事項再本頁) 裝.
、1T 本紙張尺度適用中國國家標準(CNS ) Μ規格(210X 297公釐) 127 _ 1 07 - 經濟部中央標準局員工消費合作社印製 1 Μ ^___Β7__— 五、發明説明(124 ) 5·27(2Η,ιη),6·88·6·98(2Η,ιη),7·54·7·64(2Η,ιη),7·94·8·12(4Η,ιη). \ IR(KBr):3370,3006,2953,1708,1649,1604,1541,1512,1460,1441,1414,1328,130 2,1248,1162,1107,1090,l〇32/cm. [a]D= ·19·1° (CH30H,c=l.01,24=). Νο·1 a — 9 5 CD30D 300MHz 1.04- 2.02(14H,m),2.14(lH,m),2.23(2H,t,J=7.2Hz),2.93-3.02(7H,m),5.13-5.27(2 H,m),6.82-6.92(2H,m),7.51-7.59(2H,m),7.95-8.02(2H,m),8.04-8.11(2H,m). IR(KBr):3370,3006,2953,1708,1649,1604,1541,1512,1460,1441,1414,1328,130 2,1248,1162,1107,1090,1032/cm. [a]D==-17.6e (CH3OH,c=1.01,24t:)· No.l a — 9 6 CD30D 300MHz 1.05- 2.02(14H,m),2.14(lH,m),2.23(2H,t,J=7.2Hz),2.98(lH,m),5.13-5.27(2H,m), 6.75-6.84(2H,m),7.43-7.52(2H,m),7.94-8.12(4H,m). IR(KBr):3339,3197,2953,2875,1707,1644,1606,1541,1514,1446,1325,1293,125 9,1240,1225,1161,1091/cm. [a]D= -18.7° (CH30H,c=1.00,24t:). mp.l93-196t: No.l a - 9 7 d6-DMSO 300MHz 1.05- 2.08(15H,m),2.15(2H,t,J=7.5Hz),2.89(lH,m),5.18-5.28(2H,m),6.78-7.12(3 Hlm),7.73(lH,d.d,J=1.4and7.8Hz),7.91-7.95(3Hfm)f8.14(2H,d,J=8.4Hz)l9.71(l H,s). IR(KBr):3407,3191,2953,1711,1646,1614,1603,1537,1457,1326,1162,1151/cm [a]D=-20.7e (CH3OH,C=1.01,2lt:). 本紙浪又度適用中國國家標準(CNS ) A4規格(210X 297公釐) (請先閱讀背面之注意事項再本頁) •裝_ 訂 線 513422 A7 B7 五、發明説明) 經濟部中央標準局員工消費合作社印製
No.l a — 9 8 CDC13 300MHz 0.93-2.00(14H,m),2.21(lH,m)>2.31(2H,t,J=7.2Hz),2.93(lH>m),3.84(3H,s),3.85( 6H,s),5.15-5.30(2H,m),5.45(lH,d,J=6.3Hz),7.04(2H,s),7.78-7.86(2H,m),7.90-7.: 98(2H,m),8.58(lH,s). IR(CHC13):3264,3008,2954,2874,1707,1670,1607,1537,1506,1451,1421,1308,1 158,1129,1088/cm. [a]D= -7.2° (CHC13,C=1.01,23.5t:). mp.147-149*0 No.l a - 9 9 CD30D 300MHz 1.04.1.98(14H,m),2.21(lH,m),2.10(2H,t,J=7.2Hz),2.95(lH,m),3.76(3H,s),3.86( 6H,s),5.07-5.24(2H,m),7.19(2H,s),7.99(2H,d,J=8.7Hz),8.13(lH,d,J=8.7Hz). IR(KBr):3354,3002,2950,2874,1656,1607,1570,1508,1452,1413,1314,1233,118 5,1157,1127,1092/cm. [〇f]D= ·20·3β (CH30H,C=1.00,23.5t:). No.l a - 1 0 0 CDC13 300MHz 1.14-1.97(14H,m),2.19(lH,m),2.28(2H,t,J=7.4Hz),3.04(lH,m),3.69(3H,s),5.03( lH,d,J=6.9Hz),5.15-5.29(2H,m),7.65(2H,d,J=8.4Hz)>7.87(lHls),7.98(2H,dfJ=8. 4Hz). IR(CHC13):3386,3271,3025>3015,2955,2877,1755,1712,1608,1331,1162/cm. [c〇D= -29.4。(CH3OH,c=1.01,25t:)e No.l a ~ 1 0 1 d6-DMS0 1.00.2.20(17H,m),2_84(lH,m),5.00-5.20(2H,m),7.78(2H,d,J=8.2Hz),7.84(lH,s), (請先閲讀背面之注意事項再本頁) -裝_ 訂 線 本纸張尺度適用中國國家標準(CNS ) A4規格(2丨〇><297公釐) 129 A7 '發明説明(126 7·89·7·95(3Η,ιη)· IR(KBr):3269,3065,3008,2952,2874,2763,1746,17.07,1607,1322,1157 /cm. [〇:]D= ·26·2β (CH3OH,c=1.01,25t:)e No.l a - 1 0 2 CD30D 1.00-2.25(17H,m),2.92(lHfs),3.64(3H,s),5.07.5.21(2H,m),7.53(lH,s),7.77(2H,d, J=8.6H2),7.90(2H,d,J=8.6). IR(KBr):3430,3277,3006,2952,2873,1720,1687,1620,1571,1438,1312,1156 /cm. [a]D= -27.3° (ΟΗ30Η,〇=0.51,26Χ:). mp 230-232X: Νο·1 a - 1 0 3 CDC13 300MHz 0.94-1.96(14H,m),2.19(lH,m),2.28(2H,t,J=7.2Hz)f3.04(lH,m),3.69(3H,s),5.11( lH,d,J=6.6Hz),5.15-5.28(2H,m),7.60(2H,d,J=8.4Hz),7.67(lH,s),7.98(2H,d,J=8. 4Hz). IR(CHC13):3381,3021,2955,2876,1735,1605,1437,1411,1325,1231,1177 /cm. [a]D=+8.6° (0ΗΟ13,ο=1.00,23Χ:)〇 (請先閱讀背面之注意事項再頁) —裝· ^^本 、v'口 經濟部中央標準局員工消費合作社印製
No.l a — 1 0 4 CDC13 300MHz 0.94-1.96(14Hlm),2.21(lH>m),2.31(2Hlt,J=6.8Hz)l2.99(lHlm),5.18-5.28(2H,m), 5.45(lH,d,J=6.6Hz),7.61(2H,d,J=8.7Hz)l7.67(lHfs),7.99(2H,d,J=8.7Hz). IR(CHC13):3382,3222,3028,3019,2957,2876, Π36,1709,1604,1412,1322,1301,1 286,1179,1162 /cm. [a]D= +10.4〇 (CHCadOOW1^)·
No.l a - 1 0 5 本紙浪尺度適用中國國家標準(CNS ) A4規格(210 X 297公釐) 130 513422 A7B7 五、發明説明(127 ) 經濟部中央標準局員工消費合作社印製 CDC13 300MHz 0.92-1.98(14H,m),2.17(lH,m),2.26(2H.d,J=7.5Hz),3.01(lH,m),3.69(3H,s),4.01( 3H,s),4.84(lHfd,J=6.3Hz),5.14.5.30(2H,m),7.71(2H,d,J=8.7Hz),7.87(2H,d,J=8. 7Hz),8.09(lH,s). IR(CHC13):3385,3284,3025,3015,2954,2877,2821,1730,1598,1459,1438,1403,1 341.1160.1052 /cm. [a]D= +3.6。(CHC13,c=1.00,26t:)e No.l a - 1 0 6 CDC13 300MHz 0.92-2.08(14H,m),2.14(lH,m),2.34(2H,d,J=7.2Hz),3.02(lH,m),4.01(3H,s),5.19( lH,d,J=6.9Hz),5.23-5.32(2H,m),7.71(2H,d,J=8.4Hz),7.88(2H,d,J=8.4Hz),8.09( lH,s). IR(CHC13):3510,3384,3268,3028,3021,3014,2957,2877,2821,2667,2821,2666,1 707.1598.1459.1404.1341.1324.1160.1052 /cm. [a】D= +11.8。(CHC13,〇=1·01,25Χ:)· mp 95-96X: No.l a — 1 0 7 CDC13 300MHz 0.92-1.97(14H,m)>1.34(3Hft,J=7.2Hz),2.18(lH,m),2.28(2H.d,J=7.4Hz),3.01(lH, m),3.68(3H,s),4.26(2H,q,J=7.2Hz),4.86(lH,d>J=6.6Hz),5.15-5.29(2H,m),7.71(2 H,d,J=8.7Hz),7.87(2H,d,J=8.7Hz),8.09(lH,s). IR(CHC13):3385,3282,3025,3026,3015,2954,2877,1729,1599,1480,1458,1438,1 403,1338,1161 /cm. [a]D=+4.4° (CHC13,c=1.00,25t:)· No.l a — 1 0 8 CDC13 300MHz 0.90-2.04(14H,m),1.34(3H,t,J=7.2Hz),2.14(lH,m),2.34(2H,d,J=7.lHz),3.01(lH, (請先閲讀背面之注意事項再本頁) 裝. 訂 線 本紙張尺度適用中國國家標準(CNS ) A4規格(210 X 297公釐) 131 513422 A7 B7 五、發明説明(128 經濟部中央標準局員工消費合作杜印製 m),4.27(2H,q,J=7.2Hz),5.20(lH,d,J=6.6Hz),5.21-5.35(2H,m),7.71(2H,d,J=8.4H z)f7.88(2H,d,J=8.4Hz),8.10(lH,s). IR<CHC13):3514,3384,3270,3025,3015,3015,2957,2877,1708,1599,1458,1403,1 324,1324,1160,1050 /cm. [a】D= +12.7。(CHC13,c=1.00,25t:)· No.l a — 1 0 9 [a]D=+8.5〇 (CHC13,c=1.00,25<C). mpl09.0-lll.0t: No.l a — 1 1 0 CDC13:CD30D(95:5) 0.92.2.06(14H,m),2.20(lH,m),2.30(2H,d,J=7.2Hz),2.99(lH,m),5.22.5.33(2H,m), 7.54.7.66(3H,m),8.07(2H,d,J=9.0Hz),8.12-8.20(2H,m),8.29(2H,d,J=9.0Hz). IR(Nujol):3270f2956,2924,2S54>1716,1548,1485,1319,1167/cm. [a]D=+17.0° (CHC13,c=1.00,25t:). mp. 166.5-168t: No.l a — 1 1 1 [a]D=+2.6° (CHC13,c=1.00,24t:)e mp 120.0-121.Ot: No.l a - 1 1 2 CDC13 300MHz 0.96.2.04(14H,m)f2.19(lH,m),2.33(2H,d,J=7.lHz),3.07(lH,m)r5.28-5.31(2H,m), 5.33(lH,d,J=6.6Hz)>7.54.7.63(3H,m),8.05(2H,d,J=8.4Hz),8.18-8.23(2Hlm)l8.41 (2H,d,J=8.4Hz). IR(CHCi3):3384,3269,3025,3015,2957,2877,1708,1598,1496,1457,14 17,1326,1 164 /cm. [a]D= +12.2° (CHC13,c=1.00,2‘lt:)· mp.163.164t: (請先閱讀背面之注意事項再Hi本頁) 裝-
、1T 線 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 132 513422 A7 B7 五、發明説明(129
No.l a — 1 1 3 [a]D= +22.1° (CHC13,c=1.05,25t:). mp.90-92t:
No.l a ~ 1 14 [a]D= +2·2β (CHC13,c=1.02,25t:)e
No.l a - 1 1 5 CDC13 300MHz 0.90-1.98(14H,m),2.15-2.22(lH,m)>2.27(2H,t,J=7.2Hz),2.95-3.04(lH,m), 3.68(3H,s),4.04(2H,s)f4.85(lH,d,J=6.6Hz)>5.10-5.27(2H,m),7.12- 7.34(7H,m),7.76-7.82(2H,m). IR(CHC13):3384,3026,2952,1727,1595,1493,1436,13 IS, 1155, l〇91,890/cm. [a]D==0· [a ]436=+4.9 ±0.4·
No.l a - 1 1 6 CDC13 300MHz 0.90-2.10(14H,m),2.10.2.18(lH,m),2.32(2H,t,J=7.2Hz),2.96-3.04(lHlm)l 4.04(2H,s)f5.14(lH,d,J=6.6Hz),5.16.5.28(2H>m),7.12.7.34(7Hfm),7.76- 7.82(2H,m). IR(CHC13):3260,3020,2950,1709,1407,1318,1154,1091,892/cm. [a]D==+9.1±0.5*(CHC13,c=1.04,23t:) 經濟部中央標隼局員工消費合作社印製
No.l a - 1 1 7 CD30D 300MHz 0.96.2.18(17H,m)f2.89-2.92(lH,m),4.05(2H,s),4.95-5.22(2Hfm),7.15- 7.42(7H,m),7.75-7.81(2H,m). IR(KBr):3429t3279,2951,2872,1563,U94,1453,1408,1313, i 155,1093,1057/c jD==· 16.3 土 0.5· (CH30H,c=l.06,25t:) 133 本纸浪尺度適用中國國家標準(CNS ) A4規格(210 X 297公釐) 513422 A7 B7 五、發明説明(130 ) 經濟部中央標準局員工消費合作社印製
No.l a — 1 1 8 CDC13 300MHz 0.98-1.70(1δΗ,m), 1.8〇.2.00(5H,m),2.20-2.40(3H,m),2.98(lH,m),4.06(2H,s),4.7 2(lH,d,J=6.3Hz),5.00-5.23(3H,m),7.16(2H,d,J=8.4Hz),7.26-7-33(5H,m),7.79(2 H, d,J=8.lHz). IR(CHC13):3376,3020,2948,2868,1716,1596,1492,1453,1407,1318,1155,1105/c m. [a]D=+2.4° (CHC13,c=l.08,24t:). No.l a — 1 1 9 CDC13 300MHz ; 0.90-2.02(14H,m)f2.20(lH,m),2.29(2H,t,J=7.2Hz),3.00(lH,m),3.68(3H,s),4.86( lH,d>J=6.9Hz),5.13-5.34(2H,m),7.00-7.09(4Hlm),7.22(lHlm),7.37-7.45(2Hfm), 7.79-7.86(2H,m). IR(CHC13):3376,3018,2946,2868,1727,1582,1486,1321,1243,1151,1093 /cm. [a]D= +4.5° (CHC13,c=l.05,23.5t:)e No.l a - 1 2 0 CD30D 300MHz I. 00.2.00(14H>m),2.13(2H,t,J=7.5Hz),2.16(lH,m),2.91(lH>m),5.05-5.33(2H,m), 7.04-7.11(4H,m),7.18-7.25(lH,m),7.38.7.48(2H,m),7.80-7.87(2Hfm). IR(KBr):3430,3278,3006,2952,2873,1583,1487,1410,1322,1298,1245,1152,109 5 /cm. [crjD= -8.8。(CH30H,c=l.05,25.Ot:)· No.l a ~ 1 2 1 CDC13 300MHz 0.90-2.10(14H,m),2.15(lH,m),2.35(2H,t,J=7.2Hz),3.0i(LH,m),5.20(lH,d,J=6.9 (請先閱讀背面之注意事項再本頁) -裝_ 訂 線 本纸張尺度適用中國國家標準(CNS )八4規格(210X 297公釐) 134 513422 A7 B7 五、發明説明(131
Hz),5.22-5.35(2H,m),7.00-7.09(4H,m),7.18.7.25(lH,m),7.37-7.45(2H,m)f7.79-7. 86(2H,m)· IR(CHC13):3260,3020,2948,2868,1708,1582,1486,1409,1321,1296,1243,1151,1 093 /cm.
[a]D= +13.Γ (CHC13,c=1.04,24.0t:)e
No.l a — 1 2 2 CDC13 300MHz 0.90-2.00(14H,m)>2.23(lH,m)l2.28(2H,t,J=7.5Hz),2.96(lH,m),3.67(3H,s),4.69( lHtd,J=6.6Hz),5.15.5.32(2H,m),6.22(lH>s)>6.98-7.40(5H,m)>7.30-7.38(2H,m),7. 68-7.74(2H,m). IR(CHC13):3416,3370,3018,2946,2868,1725,1587,1508,1437,1400,1320,1149,1 094 /cm.
[a]D= +6.2° (011013^=1.04,25.0^:)0
No.l a - 1 2 3 CDC13 300MHz 0.90.2.04(14H,m),2.18(lH,m),2.33(2H,t,J=7.2Hz),2.96(lH,m),5.04-5.35(3H,m), 6.98-7.12(3H,m),7.12-7.20(2H,m)l7.28-7.38(2H,m),7.66-7.74(2H,m). IR(CHC13):3424,3270,3028,2952,2872,1708,1587,1508,1445,1399,1320,1148,1 092 /cm.
[or】D= +20.9。(CHC13,c=1.06,23.0*C)· 經濟部中央標準局員工消費合作社印製
No.l a — 1 2 4 CDC13 300MHz 0.90-2.00(14H,m),2.18(lH,m),2.28(2H,t,J=7.2Hz),3.00(lH,m),3.14(3H,s),3.68( 3H,s),4.56(2H,s),4.84(lH,d,J=6.3Hz),5.10-5.29(2H,m),7.16-7.26(4H,m),7.26-7. 34(2H,m),7.78-7.84(2H,m)· IR(CHC13):3384,3028,2952,2874,1727,1598,1501,1435,1410,1370,1329,1172,1 135 本纸張尺度適用中國國家標準(CNS ) A4規格(210X 297公瘦) 513422 A7 B7 五、發明説明(132 ) 經濟部中央標準局員工消費合作社印裝 145.1091 /cm. [a】D=+2.7°(CHC13,c=l.O9,23.0t:)· No.l a — 1 2 5 CDC13 300MHz 0.90-2.00(14H,m),2.18(lH,m),2.28(2H,t,J=7.2Hz),2.29(3H,s),3.00(lH,m),3.68( 3H,s),4.04(2H,s),4.S0(lH,d,J=6.6Hz),5.11-5.29(2H,m),6.99-7.06(2H,m),7.12-7. 19(2H,m),7.31(2H,d,J=8.lHz),7.79(2H,d,J=8.lHz). IR(CHC13):3382,3280,3024,2950,2S74,1730,1596,1504,1435,1407,1367,1318,1 196.1155.1091 /cm. [a]D= +2.9° (CHC13,c=1.06,23.0t:)e No.l a — 1 2 6 CDC13 300MHz 0.90-2.02(14H,m),2.14(lH,m),2.29(3H,s),2.32(2H,t,J=7.2Hz),3.01(lH,m),4.03( 2H,s),5.10(lH,dfJ=6.6Hz),5.15-5.30(2H,m),6.98-7.06(2H,m)(7.11-7.18(2H,m),7. 30(2H,d,J=8.lHz),7.79(2H,d,J=8.1Hz). IR(CHC13):3374,3260,3020,2948,2868,1749,1708,1596,1504,1407,1369,1317,1 195.1155.1091 /cm. [a]D= +10.0° (CHC13,c=1.09,23.0t:)e No.l a - 1 2 7 CDC13 300iMHz 0.87.1.95(14Htm),2.18.2.32(3H,m),2.95(lH,m),3.69(3H,s),3.96(2H,s),4.79(lH, d,J=6.6Hz),4.97.5.17(2H,m)f5.54(lH,s),6.75-6.82(2H,m),6.97.7.05(2H,m),7.25-7.33(2H,m),7.75-7.81(2H,m). j j IR(CHCi3):3382,3026,2950,2874,1722,1595,151 1,U36,1407, L3 17,1257, LI 54.1 090 /cm. [ajD二-2.1a (CHCl3.c=1.00,21.5t:)e (請先閱讀背面之注意事項再本頁) 裝_ 訂 線 本紙浪尺度適用中國國家標準(CNS ) A4規格(210 X 297公釐) 136 513422 A7 B7 五、發明説明(133 請 先 閱 讀 背 δ} 5 意 事 項
No.l a - 1 2 8 CDC13 300MHz 0.85-2.02(14H,m),2.18(lH,m),2.31(2H,t,J=7.2Hz),2.96(lH,m),3.95(2H,s),5.05- 5.27(3H,m),6.73.6.82(2H,m),6.96-7.04(2H,m),7.25-7.32(2H,m),7.74-7.81(2H,m )· IR(CHC13):3262,3020,2948,286S, 1708,1596, loll, HOT, 1315,1242,1154,1091 / cm.
[a]D=+4.8〇 (CHC13,c=1.04,22t:).
No.l a — 1 2 9 CDC13 300MHz 0.89-1.98(14H,m),2.18(lH,m),2.27(2li,t,J=7.2Hz),2.99(lH,m),3.6S(3H,s),3.79( 3H,s),3.98(2H,s),4.81(lH,d,J=6.6Hz)>5.10-5.27(2H,m),6.81-6.87(2H>m)>7.03-7. 10(2H,m),7.25-7.32(2H)m),7.75-7.82(2H,m). IR(CHC13):3382,3276,3006,2950,2874,1726,1609,1509,1457,1436,1407,1315,1 244,1154,1091,1033/cm.
[a]D=+19.3〇(CHC13,C=1.05,23t:)· iMo.l a - 1 3 0 CDC13 300iMHz 經濟部中央標準局員工消費合作社印製 0.90-2.00(14H,m),2.20(lH,m),2.30(2H,t,J=7.2Hz),2.9S(lH,m),3.69(3H,s),4.81( lH,d,J=6.6Hz),5.12-5.32(2H,m),5.46(lH,brs),6.84-7.01(6H,m),7.76-7.83(2H,m) IR(CHC13):3380,3284,3024,2952,2874,1724,1588,1504,1488,1436,132 1,1296,1 149r1091/cm.
[ajD:+28.9。(CHCl3,C:1.01,23t:).
No. L a — 1 3 1 CDC13 300MHz 本紙張尺度適用中國國家標準(CNS ) Α4規格(210X 297公釐) 137 513422 A7 B7 五、發明説明(134 ) 0.92-2.10(14H,m),2.18(lH,m),2.34(2H,t,J=€.9Hz),2.96(lH,m),5.18-5.35(3H,m), 6.84-7.01(6H,m),7.75.7.83(2H,m). IR(CHC13):3270,3028,2952,2874,1708,1589,1505,1489,1456,1322,1297,1238,1 148,l〇91/cm.
[a]D=+7.7e (CHC13,C=1.09,24t:)·
No.l a — 1 3 2 CDC13 300MHz 0.91-2.02(14H,m),2.19(lH,m),2.29{2H,t,J=7.2Hz),2.99(lH,m),3.6S(3Hts),3.83( 3H,s),4.82(lH,d,J=6.6Hz),5.14-5.33(2H,m),6.90-7.04(6H,m),7.76-7.83(2H,m). IR(CHC13):3384,3006,2952,2874,1727,1589,1502,1488,1459,1438,132 1,1295,1 231,1150,1092,1033/cm. (α]Ό=+3.Γ (CHC13,C=1.01,23X:).
No.l a - 1 3 3 TLC Rf=0.21 (醋酸乙酯·· n-己烷=1 : 1(0.3%賭酸>):
No.l a - 1 3 4 CDC13 300MHz 0.97-2.10(14H,m),2.20(lH,m),2.36(2H>t(J=6.9Hz),3.04(lHtm),5.22-5.33(2H,m), 5.41(lH,d,J=6.6Hz),7.02(lH,d,J=9.0Hz),7.09-7.13(2H,m),7.26-7.32(lH,m),7.43 • 7.49(2H,m),7.93<lH,d.d,J=2.4and9.0Hz),8.46(lH,d,J=2.4Hz). 經濟部中央標準局員工消費合作社印製 IR(CHC13):3334,3270,3020f2958f 1709,1610,1587,1537,1479,1352,127 1,1252,1 167/cm.
[a]D=+20.9° (CHC13,C=0.51,22t:).
No.L a - 1 3 5 、 CDC13 300MHz 0.9G-2.02(14H,m)t2.21(lH,m),2.29C2H,t,J=7.2Hz),3.07(LH,m),3.68(3H,s),5.04( 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) -138 - 513422 A7 B7 五、發明説明(135 經濟部中央標準局員工消費合作社印製 lH,d,J=6.9Hz),5.16-5.33(2H,m),7.48-7.55(2H,m),7.64(lH,m),7.76.7.82(2H,m), 7.88-7.94(2H,m)f7.98-8.04(2H,m). IR(CHC13):3384,3282,3026,2952,2874,1727,1663,1596,1446,1396,1316,1274,1 163,1090 /cm. [a】D= +3·Γ (CHC13,c=l.03,22.Ot:)· No.l a - 1 3 6 CDC13 300MHz 0.95-2.05(14H,m),2.19(lH,m),2.34(2H,t,J=7.2Hz),3.08(lH,m),5.10-5.40(2H,m), 5.35(lH,d,J=6.8Hz),7.45-7.58(2Hfm),7.64(lH,m),7.74.7.84(2Hlm),7.84-7.95(2 H,m),7.95-8.06(2H,m). IR(CHC13):3260,3018,2950,2870,1708,1662,1595,1446,1395,1316,1274,1162,1 090 /cm. [a]D二 +12.9。(CHC13,c=1.05,21.5t:)。 No.l a - 1 3 7 CDC13 300MHz 0.97-2.04(14H,m),2.27(lH,m),2.31(2H,t,J=7.2Hz),3.07(lH,m),3.70(3H,s),5.15· 5.30(3H,m),7.48-7.68(5H,m),7.96-8.02(2H,m). IR(CHC13):3382,3030,2952>2878,1725,1446,1329,1154,1098 /cm. [a]D= -12.1° (CHCi3,c=1.03,22.0t:)e No.l a - 1 3 8 CDC13 300MHz 0.95-2.04( 2,25( lH,m),2.35(2H,t,J=7.2Hz),3.08( lH,m),5· 15-5.34(2H,m), 5.41(lH,d,J=6.6H2),7.48-7.68(5H,m),7.98-8.03(2H,m). IR(CHC13):3370,3242,3022,2950,2870,1707,1445,1408,1329.1154,1099 /cm. [c^D二,O.G〇 (CHCl3,c=l.〇6.2l.5t:) M3G5 +30.7。((:Η(:13.π1·06,21·5Γ). : : 扯衣-- (請先閱讀背面之注意事項再||||>本頁) 、11 線 本纸張尺度適用中國國家標準(CNS ) A4規格(210 X 297公釐) 139 五 、發明説明( 136 A7 B7 經濟部中央標準局員工消費合作社印製
No.i a - 1 3 9 CDC13 300MHz 0.92-2.19(14H,m),2.27-2.34(3H,m),3.26(lH,m),3.65(3H,s),4.28(2H,s),4.37(lH, d,J=7.4Hz),5.34-5.50(2H,m),7.37.7.62(9H,m). IR(CHC13):3389,3294,3028,3015,2954,2877,1730,1600,1488,1325,1151,1129 / cm. [a]D= -24.8° (CHC13,C=1.01,24t:)e No.l a — 1 4 0 CDC13 300MHz 0.92-2.22(15H,m),2.34(2H,t>J=7.lHz),3.24(lH,m),4.29(2H,s),4.81(lH,d,J=7.4H z),5.32-5.52(2H,m)f7.36.7.62(9H,m). IR(CHC13):3510,3388,3251,3031,3015^2956,2877,2668,1708,1601,1488,1318,1 151,1129 /cm. [a]D= -24.6° (CHC13,c=1.02,25t:)e No.l a - 1 4 1 CDC13 300MHz 0.92-2.19(15H,m),2.32(2H,t,J=7.2Hz),3.26(lH,m),3.65(3H,s),4.31(2H,s),4.48(l H,d,J=7.4Hz),5.33-5.49(2H,m),7.42-7.80(8H,m). IR(CHC13):3388,3285,3018,2955,2877,2225,1730,1597,1479,1320,1152,1129 / cm. [a]O= -20.Γ (CHC13),c=0.96,25t:). No.l a - 1 4 2 CDC13 300MHz 0.92.2.22(15H,m)l2.35(2H,t,J=6.8Hz),3.25(lH,m),4.32(2H,s),4.86(lH,d,J=7.4H z),5.33-5.53(2H.m),7.43-7.80(8FI,m). IR(CHC13):35 12,3388,3258,303 1,3023,30 14,2956 2377,2225,1708,1597, U79, 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) (請先閱讀背面之注意事項再本頁) 裝. 訂 綠 140 513422 經濟部中央標準局員工消費合作社印製 A7 B7五、發明説明(137) 1319,1151,1128 /cm. [a]D= ·19·3。(CHC13,c=:L09,23t:)· No.l a — 1 4 3 CDC13 300MHz 1.00-1.93(14H,m),2.17(lH,m)>2.27(2H,t,J=7.2Hz),3.07(lH,m),5.17-5.22{2H,m), 5.36(lH,d,J=6.9H2),7.77(lH,d,J=9.0Hz),8.11-8.17(2H,m),8.36(lH,d.d,J=2.1an d9.0Hz),8.51(lH,d,J=1.8Hz),8.65(lH,d,J=2.lHz). IR(CHC13):3382,3266,3026,2954,2874,1708,1632,1585,1528,145s, 1419,1345,1 153/cm. [a]D=+7.6〇 (CHC13,C=1.04I22<C). No.l a - 1 4 4 ' CDC13 300MHz 0.95-1.90(14H,m),2.17(lH,m),2.25(2H,t,J=T.5Hz),3.02(lH,m),5.09(lH,d,J=6.6 Hz)>5.15-5.21(2H,m),6.72(lHfd,J=8.4Hz),6.85(lH,s),7.54(lH,d,J=S.4Hz)f7.72( lH,d,J=9.0Hz),7.83(lH,d.d,J=1.8and9.0Hz)f8.32(lH,d,J=1.8Hz). IR(CHC13):3380,3260,3022,2948,2868,2352,1709,1636,1460,1425,1313,1291,1 265,1148,1130/cm. [a]D=+12.9〇 (CHC13,C=1.02,22.5t:). No.l a - 1 4 5 CDC13 300MHz 0.97.1.90(14H,m),2.15(lH,m)f2.27(2HtttJ=6.9Hz),3.02(lH,m)>3.0S(6Hls),5.12( lH,d,J=6.3Hz),5.19-5.25(2H,m),6.78.6.84(2H,m),7.53(lH,d,J=8.7Hz),7.76-7.83 (2H,m),8.30(lH,d,J=1.8Hz). IR(CHC13):3272,3030f2950,2874,1708,1635,1601,15 11,1457,1425,1357,1328,1 151,U24/cm. [aJD=+6.3〇 (CHCi3,C=L.04,23t:). (請先閱背面之注意事項再本頁) •裝_ 訂 線一 本纸張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 141 513422 A7 B7 五、發明説明(138) 經濟部中央標隼局員工消費合作社印製
No.l a - 1 4 6 CDC13 300MHz 0.95-2.00(14H,m),2.16(lH,m),2.29(2H,t,J=7.2Hz),3.05(lH,m),4.10(3H,s),5.13. 5.28(2H,m),5.38(lH,d,J=6.9Hz),7.67-7.74(2H,m),8.08(lH,d.d,J=1.8and9.0Hz), 8.11(lH,s),8.61(lH,d,J=1.8Hz). IR(CHC13):3260,3020,2948,2868,1708,1639,1606,1528,1470,1455,1424,1349,1 311,1238,1174,1149,H20,1079,l〇60,1022/cm. [a]D=+7.8〇 (ΟΗ013,0=1.00,23Χ:). No.l a — 1 4 7 CDC13 300MHz 0.92-1.92(14H,m),2.17(lH,m),2.25(2H,t,J=7.2Hz),3.01(lH,m),3.97(3H,s)l5.10< 5.27(5H,m),6.92(lH,s),7.29(lH,s),7.52(lH,d,J=8.7Hz),7,82(lH,d.d,J=2.1and8· 7Hz),8.33(lH,d,J=2.1Hz). IR(CHC13):3380,3264,3002,2950,2868,1708,1634,1476,1452,1426,1317,1264,1 218,1169,1147,1115,1068,1031/cm. [a】D=+5.6。(CHC13,C=1.02,23t:)· No.l a — 1 4 8 CDC13 300MHz 0.9(M.98(14H,m),2.15(lH,m),2.28(2H,t,J=6.9Hz),2.91(6Hs),3.03(lH,m),4.01(3 Hfs),5.15-5.26(3H>m),7.18(lH,s),7.38(lH,s),7.59(lH,d,J=8.7Hz),7.87(lH,d.d,J =2.1and8.7Hz),8.40(lHtd,J=2.lHz). IR(CHC13):3384,3266,295611709,1632,1602,1495,1473,1458,1430,1317,1231,1 148,1121/cm. [a】D=+11.20 (CHC13,C=1.01,23r). No.l a - 1 4 9 (請先閱讀背面之注意事項再本頁) |裝· 太 訂 線 本纸張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 142 513422 A7 B7 五、發明説明(139 ) CDC13 300MHz 0.99-1.90(14H,m),2.17(lH,m),2.28(2H,t,J=7.2Hz),3.00(lH,m),5.13-5.19(2H,m), 5.43(lH,d,J=6.0Hz),7.02(lH,d.d,J=2.4and9.0Hz),7.38.7.41(2H,m),7.58(lH,d,J ! =8.7Hz),7.96(lH,d.d,J=1.8and8.7Hz),8.45(lH,d,J=1.8Hz). IR(CHC13):3270,3020,2948,2868,1709,1601,1478,1448,1419,1315,1147,1120/c m. [a]D=-11.4。(CHC13,C=1.01,23t:). No.l a — 1 5 0 CDC13 300MHz 0.97-1.8S(14H,m),2.12.2.31(3H,m),2.38(3H,s),3.01(lH,m),5.14.5.19(2H,m),5.3 6(lH,d,J=6.6Hz),7.24(lH,d.d,J=2.4and9.0Hz)>7.59(lH,d,J=6.3Hz),7.66(lH,d,J =8.7Hz),7.72(lH,d,J=2.4Hz),8.01(lH,d.d,J=1.8and8.7Hz),S.49(lH,d,J=l.SHz). IR(CHC13):3470,3374,3260,3018,2950,2868,1709,1474,1444,1412,1370,1319,1 266,1162,1145,1118/cm. [a]D=+4.9° (CHC13,C=1.00,24t:). (請先閱讀背面之注意事項再本頁) -裝- 訂 經濟部中央標準局員工消費合作社印製
No.l a — 1 5 1 CDC13 300MHz 0.97-1.89(14H,m),2.17(lH,m),2.25(2H,t,J=7.2Hz),3.03(lH,m),3.92(3H,s),5.15- 5.20(2H,m),5.32(lH>d,J=6.6Hz),7.11(lH,d.d,J=2.4and9.3Hz),7.45(lH,d,J=2.4 Hz),7.50(lH,d,J=9.3Hz),7.62(lH,d,J=8.7H),7.97(lH,d.d,J=2.1and8.7Hz),8.50( !H,d,J=2.lHz). IR(CHC13):3260,3018,2948,1708,1483,1454,1432,1314,1287,1268,1188,1169,1 147/cm. [a]D=+4.9。(CHC13,C=1.01,23.5t:).
No.l a - 1 5 2 CDC13 300MHz 本纸張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 線 143 513422 A7 B7 五、發明説明(14Q ) 0.98-2.04(i4H,m),2.15(lH,m),2.30(2H,t,J=6.6Hz),3.04(lH,m),5.17-5.29(3H,m), 7.41(lH,d.d,J=1.5and8.1Hz),7.64-7.68(2H,m),7.92(lH,d,J=8.4Hz),8.00(lH,d.d, J=1.8and8.4Hz),8.49(lH,d,J=1.8Hz). IR(CHC13):3266,3028,2952,2872,1707,1629,1591,1456,1416,1318,1275,1150/c m.
[a]D=+3.2° (CHC13,C=1.04,23t:).
No.l a — 1 5 3 CDC13 300MHz 0.97-1.88(14H,m),2.16(lH,m),2.26(2H>t,J=/7.2Hz),3.03(lH,m),4.64.4.65(2H,m), 5.16.5.50(5H>m),6.13(lH,m),7.14(lHld.d,J=2.7and9.0Hz),7.46.7.52(2H,m),7.6 3(lH,d,J=8.7Hz),7.97(lH,d.d,J=1.8and8.7Hz),8.49(lH,d,J=1.8Hz)· IR(CHC13):3374,3260,3020,2948,2868,1708,1599,1478,1446,1414,1314,1284,1 268,1184,1148,1120/cm.
[cr]D=+5.3。(CHC13,C=1.00,23t:)·
No.l a - 1 5 4 CDC13 300MHz 0.99-2.00(15H,m),2.26(2H,t,J=7.2Hz),3.03(lH,m),4.07(3H,s),5.23-5.27(2H,m), 5.36(lH,d,J=7.2Hz),7.20(lH,s),7.36-7.48(2H,m),7.55-7.58(lH,m),7.91.7.93(lH, m),8.52(lH,s)· 經濟部中央標準局員工消費合作社印製 (請先閱讀背面之注意事項再本頁) IR(CHC13):3362,3257,3020,2948,2868,1708,1637,1602,1579,1488,1457,1437,1 413,1345,1318,1301,1276,1182,1104/cm.
[a】D= +19.4° (CHC13,C=1.01,25\:). mp.88-90t:
No.l a ~ 1 5 5 CDC13 300MHz 0.92.2.02(14H,m),2.15(lH,m),2.31(2H,t,J = 7.2Hz)(3.01(lH,m),4.10(2H,s),5.10( 本紙浪尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 144 513422 A7 B7 五、發明説明(141 經濟部中央標準局員工消費合作社印製 lH,d,J=6.6Hz),δ. 18-5.35(2H,m),7.04-7.26(5H,m),7.67-7.76(2H,m). IR(CHC13):3266,3028,2952,2952,2872,1708,1599,1574,147S, 1457,1418,1301,1 258,1147,1124,1101,1080/cm. [a]365 +33.4e(CHC13,O1.00,23t:)· No.l a — 1 δ 6 CDC13 300MHz 0.91-2.21(15H,m),2.33(2H,t,J=6.9Hz),3.01(lH,m),5.11(lH,d,J=6.6Hz),5.27-5.3 5(2H,m),6.85-6.96(5H,m),7.35(lH,d,J=2.lHz),7.42(lH,d.d,J=2.1and8.7Hz). IR(CHC13):3384,3263,2957,1708,1587,1489,1462,1416,1290,1222,1151,1123/c m. (a]D=+6.4° (CHC13,C=1.00,23t:). _No.l a — 1 5 7 CDC13 300MHz 0.97-1.91(14H,m),2.18(lH,m),2.26(2H,t,J=6.9Hz),3.04(lH,m),5.1S-5.26(3H,m), 7.52-7.56(2H,m),7.88-8.00(3H,m)>8.25(lH,m)>8.69(lH,m). IR(CHC13):3382,3268,2952,2874,1707,1457,1425,1409,13 IS, 1152/cm. [a]D=+4.4〇 (CHC13,C=1.02,22t:). No.l a — 1 5 8 CDC13 300MHz 1.02-1.97(14H,m),2.20(lH,m),2.29(2Hft,J=7.2Hz),3.06(lHfm),5.19-5.24(2H,m), 5.58(lH,d,J=6.6Hz),7.62(lH,m),T.72(lH,m)f7.86.7.91(2Hfm),7.96(lH,dfJ=7.8H z),8.04(lHld.d,J=1.5and8.lHz)f8.34(lHld,J=1.2Hz). IR(CHCi3):3490,3260,3020,2950,2870,1707,1456,1399,13 12.1 165/cm. [a】D二-8.3° (CHC13,C=1.00,23t:).
No.l a 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) (請先閱讀背面之注意事項再^!^本頁) .裝- 、^7 絲 145 513422 A7 B7 五、發明説明(142 ) 經濟部中央標準局員工消費合作社印製 CDC13 300MHz 0.92.1.88(14H,m),2.13(lH,m),2.24(2H,m),3.02(lH,m),3.90(3H,s),5.12-5.26(3H, m),7.29-7.58(4H,m),7.97(lH,d.d,J=1.8and7.5Hz),8.13(lH,d,J=7.5Hz),S.64(lH, d,J=1.8Hz). IR(CHC13):3382,3266,3018,2956,1708,1629,1594,1476,1467,1325,1245,1227 ,1158,1146/cm. [a]D=+14.6〇 (CHC13,C=1.00,22t). Νο·1 a - 1 6 0 CDC13 300MHz 0.93-l.SS(14H,m),2.18-2.24(3HJm),3.00(lH,m),5.08-5.21(3H,m),7.28-7.33(lH, m),7.47-7.51(3H,m),7.90(lH,d.d,J=1.5and7.8Hz),8.10(lH,d,J=7.8Hz),8.63-8.64 (2H,m). ’ IR(CHC13):3465,3380,3275,3020,2957,2876,1708,1627,1604,1495,1473,1457,1 328,1240,1222,1156,1149/cm. [a]D=+8.2° (CHC13,C=1.01,22=). No.l a — 1 6 1 CDC13 300MHz 0.98-1.88(14H,m),2.17(lH,m),2.24(2H,t,J=7.2Hz),3.05(lH,m),5.16-5.20(2H,m), 5.35(lH,d,J=6.6Hz),7.40(lH,m),7.55(lH,m),7.63(lH,d,J=8.lHz),7.89(lH,d.d,J = 1.5and8.lHz),8.01(lH,m),8.06(lH,d,J=8.1Hz),8.12(lH,d,J=1.5Hz). IR(CHC13):3478,3266f3028,2952,2874,1708,1454,14 17,1323,1196,1148/cm. [a]D=+21.9° (CHC13,C=1.01,23t:). No.l a - 1 6 2 CDC13 300MHz 0.96-1.98(14H,m)l2.02(lHfm)f2.25(2H,t,J=7.2Hz),3.05(lH,m)>4.10(3H,s),5.i4- 5.25(2H,m),5.41(lH,d,J=7.2Hz),7.35-7.42(lH>m),7.51-7.G4(3H,m)17.94.8.00(i --Γ--.------¾衣-- (請先閱讀背面之注意事項再本頁) 訂 •4- 本纸痕尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 146 513422 A7 B7 五、發明説明() 經濟部中央標準局員工消費合作社印製 H,m),8.16(lH,s)· IR(CHC13):3368,3274,3028,2952,2874,1708,1633,1583,1465,1452,1438,1413,1 315,1151,ll〇3,1053,l〇24/cm. [a]D= +15.1° (CHC13,0=1.01,23t:). mp.l08-ll〇X: No.l a — 1 6 3 d6-DMSO 300MHz 0.97-L84(14H,m),1.92(lH,m)>2.04(2H,t,J=7.5Hz)>2.90(lH,m),5.0S*5.23(2H,m), 7.32(lH,s),7.38-7.61(2H,m),7.62(lH,s)7.68-7.71(lH,m),7.92(lH,s),8.14-8.17(l H,m),10.7(lH,s),11.9(lH,s). IR(KBr):3350,3295,2952,2874,1707,1636,1601,1466,1431,1389,1315,1251,117 4,1146,1106/cm. [α)Ώ= -25.3° (CH30H,0=1.01,25^): mp.l59-162t: No.l a — 1 6 4 CDC13 300MHz 0.9S-L96(17H,m),2.05(lH,m),2.25(2H,t,J=7.2Hz),3.07(lH,m),4.32(2H,q,J=7.2 Hz),5.19-5.23(2H,m),5.31(lH,d,J=7.8Hz),7.38(lH,m),7.41-7.62(3H,m),7.95(lH, m),8.15(lH,s). IR(CHC13):3360,3018,2946,2870,1709,1633,1457,1445,1425,1394,1314,1176,1 152,1105/cm. [a]D= +12.7° (CHC13,C=1.02,25r). mp.l08-109t: No.l a - 1 6 5 CDC13 300MHz 0.95-1.98(15H,m),2.26(2Htt,J=7.5Hz)t3.04(lH,m),4.15(3Hrs),5.20-5.2G(2Hfm)f 5.34(1Η,ά^=6.9Ηζ),7.41-7.47(1Η,πι),7.65-7.68(2Η,πι),7.89.7.92(ΐΗ,πι),8.32(1 H,s). iR(CPiCl3):3366,3087,3022,2957,1708,1632,1538,1463, L408,1364,13*IG, 1308,1 (請先閲讀背面之注意事項再本頁) •裝· 訂 線 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 147 513422 Μ Β7 五、發明説明(144 227,1212,1205,1167/cm.
[a]D= +19.6。(CHC13,C=1.01,25t:)·
No.l a - 1 6 6 CDC13 300MHz 0.97-2.02(15H,m),2.27(2H,t,J=6.9Hz),3.07(lH,m),4.14(3H,s),5.21-5.27(2H,m), 5.47(lH,d,J=6.9Hz),7.64(lH,s),7.72(lH,d.d,J=0.6and9.0Hz),8.25(lH,s),8.47(l H,d.d,J=2.4and9.0Hz),8.94(lH,d<d,J=0.6and2.4Hz). IR(CHC13):3373,2957,1708,1639,1587,1528,1467,1428,1415,1345,1221,1184,1 155/cm.
[a]D= +14.4° (CHC13,C=0.50,25t:)
No.l a - 1 6 7 CDC13 300MHz 0.92.2.00(14H,m),2.15(lH,m),2.27(2H,t,J=7.2Hz)f3.04(lH,m),3.97(2H,s),5.15- 5.30(3H,m),7.35-7.47(2H,m),7.55-7.63(lH,m),7.80-7.96(3H,in),8.05(lH,d,J=0.3
Hz). IR(CHC13):3260f3020,2948,2868,1707,1451,1413,1319,1172,1144,1101, l〇71/c m· [a]D=+18.2° (ΟΗ013,0=1.04,22Χ:).
No.l a - 1 6 8 CDC13 300MHz 經濟部中央標隼局員工消費合作社印製 0.90-1.88(14H,m),2.16(lH,m),2.25(2H,tfJ=6.9Hz),3.00(lH,m),5.00.5.19(2H,m), 5.35(lH,d,J=6.6Hz),7.25-7.30(lH,m),7.48-7.50(2H,m),7.73(lH,d.d,J=1.5and8. 1Hz),8.08-8.14(3H,m),8.93(lH,s). IR(CHC13):3466,3380,3276,3016,2957,1708,1630,1495,1458,1324,124 lf1150/c m.
[a]D=+18.0° (CHC13,0=1.00,22^). 148 本紙張尺度適用中國國家標準(CNS ) A4規格(2丨〇'乂 297公釐) 513422 A7 B7 五、發明説明(145 ) 經濟部中央標準局員工消費合作社印製
No.l a - 1 6 9 CDC13 300MHz 0.87-1.86(14H,m),2.15(lH,m),2.25(2H,t,J=6.9Hz),2.98(lH,m),3.89(3H,s),5.00· 5.22(2H,m),5.27(lH,d,J=6.9Hz),6.88(lH,d.d,J=2.1and8.4Hz),6.94(lH,d,J=2.1 Hz),7.69(lH,d.d,J=1.5and7.8Hz),7.92-8.01(3H,m),8.83(lH,s). IR(CHC13):3465,3378,3276,3022,2957,1708,1630,1609,1569,1459,1433,1314,1 281,1229,1151/cm. [a]D=+19.3° (CHC13,C=1.01,21^:). No.l a - 1 7 0 CDC13 300MHz 0.88-2.25(17H,m),3.04(lH,m),3.84(3H,s),3.95(3H,s),5.06-5.26(3H,m),6.87-6.93 (2H,m),7.69(lH,d.d,J=1.6and8.2H2),7.93-9.05(3H,m). IR(CHC13):3026,2957,1708,1630,1601,1460,1331,1243,1224,1152/cm. [a]D=+17.2e (CHC13,C=1.00,22t:). No.l a - 1 7 1 CDC13 300MHz 0.95-2.00(14H,m),2.16-2.32(3H,m),2.66(3H,s),3.14(lH,m),3.68(3H,s),5.09(lH, d,J=6.8Hz),5.10-5.28(2H,m),7.45(lH,d.d”J=1.8&8.6Hz),7.75-7.84(2H,m). IR(CHC13):3374,3018,2946,2868,1725,1585,1513,1436,1340,1278,1153,1112 / cm. [a]D= -14.7° (ΟΗΟ13,ο=1.07,25.0Χ:).
No.l a - 1 7 2 CDC13 300MHz 0.97-2.02(14H,m),2.23(lH,m),2.28(2H,t,J=7.2Hz),2.66(3H,s),3.14(lH,m),5.12· 5.22(2H,m)f5.41(lH,dlJ=7.2Hz),7.45(lHld.d.,J=2.1&8.7Hz),7.76(lH,d,J=8.7Hz 本纸浪尺度適用中國國家標準(CNS ) A4規格(210X297公釐) ——:——,------^—— (請先閱讀背面之注意事項再本頁) 線 149 W3422 A7 B7 五、發明説明(146 ) ),7.78(lH,d,J=2.lHz). IR(CHC13):3372,3250,3022,2950,2868,1707,1514,1419,1336,1279,1154,1112 / cm.
[α]Ό= -4.1° (CHC13,c=1.08,26.0t:) m.p.l4M43t:
No.l a — 1 7 3 CDC13 300MHz
1.15-2.42(17H,m),2.91(lH,m),5.15(lH,d,J=4.2Hz),5.25-5.40(2H,m),7.85(lH,t,J =7.2Hz),8.00(lH,t,J=8.lHz),8.15-8.20(2H,m),8.67(lH,d,J=8.lHz),8.73(lH,d,J= 8.1Hz),8.83(1H,s),9.43<1H,s). IR(KBr):3422,3269,3046,2952,2871,1711,1617,1447,1333,1243,1161,1146/cm.
[a】D:41.0〇 (CH3OH,C=1.01,23t:)· *
No.l a - 1 7 4 CDC13+d6-DMSO 300MHz 1.00-1.92(14H,m),2.20(2H,t,J=6,6Hz),2.35(lH,m),2.92(lH,m),5.05-5.22(2H,m), 6.63(lH,d,J=5.4Hz),7.77-7.92(3H,m),8.31(lH,d.d,J=1.8and8.7Hz)f8.59(lH,d(J =8.7Hz),8.73(lH,d,J=8.7Hz),9.01(lH,s),9.55(lH,d,J=1.8Hz). IR(KBr):3433,3252,2952,2871,1696,1578,1423,1335,1308,1219,1185,1160,110 6/cm.
[a]D=-19.3。(DMSO,C=0.50,23t:)· 經濟部中央標準局員工消費合作社印製
No.l a ~ 1 7 5 CDC13 300MHz 0.96-1.87(14H,m),2.20,2.25(3H,m),2.95(lH,m),3.66(3H,s),‘i.7‘i(lH.d,J=6.GHZ),: 5.10-5.12(2H,m),6.88(lH,d,J=1.2Hz),7.37-7:50(3Hfm),7.56(LH,dd,J=8.7fI.5Hz)J 7.68-7.77(3H,m),8.06(lH,s),9.44(lH,dd,J=1.2Hz). IR(CHC 13):3462,3374,3026,3006,2952,2872,1724,16 10,1580, M84,1452,1358,1 本纸張又度適用中國國家標準(CMS ) A4規格(210X297公釐) 150 513422 A7 B7 五、發明説明(147 ) 經濟部中央標準局員工消費合作社印製 309,1147. [a]D=+16.4° (CHC13,c=1.05,26t:). mp.l30-132t:. No.l a - 1 7 6 CDC13+CD30D 300MHz 1.00.2.02(14H,m),2.22(lH,m),2.29(2H,t,J=6.9Hz),2.88(lH,m),5.16-5.26(2Hlm ),6.87(lH,s),7.28-7.57(4H,m),7.69(lH,d,J=8.4Hz),7.75-7.78(2H,m),7.99(lH,s). IR(KBr):3254,2944,1704,1484,1453,1358,1305,1147. [a]D=+13.0° (CH3OH,c=1.02,24t:), mp.l60-16lX: No.l a - 1 7 7 CDC13 300MHz ·: 0.96-L88(14H,m),1.88-2.26(3H,m),2.94(lH,m),3.67(3H,s),3.87(3H,s),4.67(lH, brs),5.08-5.14(2H,m),6.77(lH,d,J=1.5Hz),6.99-7.02(2H,m),7.53-7.57(lH,m),7.6 5-7.70(3H,m),8.00(lH,s),9.27(lH,brs). IR(CHC13):3426,3376,3006,2952,1724,1610,1495,1438,1357,1308,1282,1249,1 177,1147/cm. [a]D=+18.1〇 (CHC13,C=1.02,22t:). No.l a - 1 7 8 CDC13+CD30D 300MHz 0.96-1.91(14H,m),2.19(lH,m)?2.27(2H,tlJ=6.0Hz),2.85(lH,m),3.87(3H,s),5.16-5.23(2Hfm),6.99-7.02(2H,m)>7.41(lH,m),7.64-7.73(3H,m)>7.92(lH,m). IR(CHC13):3366,3261,3004,2954,2873,1705,1611,1496,1458,1438,1304,1286,1 253,1180,1149,1128/cm. [ap二+14.60 ((^13,0=1.02,22=). No.l a - 1 7 9 CDC13+CD30D 300MHz (請先閱讀背面之注意事項再本頁) 訂 本纸張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 151 513422 A7 B7 五、發明説明(148) 0.96-1.87(14H,m),2.15-2.23(3H,m),2.93<lH,m),3.85(3H,s),5.10;16(2H,m),6.9 〇.6.93(2H>m),7.50(lH,m),7.60-7.65(3H,m)>7.91(lH,d,J=0.9Hz). IR(CHC13):3369,3270,2950,2373,1719,1612,1498,1456,1440,1359,1306,1269,1 219,1146,1127/cm. [a]D=+18.1° (CH30H,C=1.00,22t:). No.l a — 1 8 0 CDC13+CD30D 300MHz 1.03-l.S6(14H,m),2.08.2.17(3H,m),2.91(lH,m),5.06-5.10(2H,m),6.76(lH,m),6.8 6-6.90(2Η,ιη),7.48(ΐΗ,πι),7.61-7.69(3Η,πι),7.89(ΐΗ,ιη). IR(CHC13):3360,3259,2954,2873,1706,1612,1497,1457,1360,1306,1272,1230,1 176,114S,1126/cm. [a]D=+20.3° (CH30H,C=1.00,22t:). No.l a — 1 8 1 CDC13 300MHz 0.97-1.96(14Hfm)f2.15(lH,m),2.29(2H,t,J=6.9Hz),3.05(lH,m),3.Sl(3H,s),5.0S( lH,d,J=6.9Hz)>5.23-5.25(2H,m),6.62(lH,s)f7.47-7.54(5H,m),7.59(lH,m),7.70(l H,m),7.97(lH,m). IR(CHC13):3380,3260,3020,2946,2868,1708,1466,1388,1328,1149/cm. [a]D=+32.9〇 (CHC13,c=1.07,22t:). (請先閱讀背面之注意事項再本頁) 訂 經濟部中央標準局員工消費合作社印製
No.l a - 1 8 2 CDC13 300MHz 0.94.1.90(14H,m),2.25(2H,t,J=7.5Hz),2.30(lH,m),2.98(lH,m),3.70(3H(s),4.83( 1H,d, J=6.GHz),5.13-5.16(2H,m),6.95( lH,d,J=1.5Hz),7.11-7.23(2H,m),7.43(1H, d,J=8.lHz),7.65(lH,d,J=8.lHz),7.79.7.93(4H,m),9.08(lH,br). IR(CHC13):3458,3372,3020,3002,2946,2868,17 19,1598,14 52, U22,132 1,1300,1 157/cm. 本纸張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 152 513422 A7 B7 五、發明説明() [a]D=-6.6〇 (CHC13,c=1.00), mpl50-15lt: No.l a - 1 8 3 CDC13 300MHz O.95-1.94(14H,m),2.26(lH,m),2.28〈2H,t,J=7.5Hz),3.00(lH,m),5.16-5.19(2H,m), 5.32(lH,d,J=7.2Hz),6.93(lH,<l,J=1.2Hz),7.13(lH,m),7.22(lH,dd,J=7.8>6.6Hz), 7.42(lH,d,J=7.8Hz),7.63(lH,d,J=7.8Hz),7.76(2H,d,J=8.4Hz),7.90(2H,d,J=8.4H z),S.95(lH,br). IR(CHC13):3458,3374,3260,3020,3002,2948,2868,1708,1598,1452,1422,130 1,1156/cm. [a]D=+17.9〇 (CHC13,c=1.01,22t:)· No.l a - 1 8 4 CDC13 200MHz 0.92-2.00(14H,m),2.20(lH,m),2.34(2H,t,J=6.8Hz)i3.05(lH,m),5.20-5.36(3H,m), 7.39-7.44(2H,m),7.61-7.66(lH,m),7.S0-7.84(lH,m),8.05(2H,d,J=8.6Hz),S.40(2 H,d,J=S.6Hz). IR(CHC13):3384,3271,3019,2958,1709,1615,1599,1551,1453,1405,1344,1326,1 243,1163/cm. [a]D=+18.5〇 (CHC13,C=L00,2lt:). (請先閱讀背面之注意事項再 裝- 頁) 訂 線 經濟部中央標準局員工消費合作社印製
No.l a — 1 8 5 ’ CDC13 300MHz 0.89-2.20(15H,m),2.26(2H,d.t,J=2.1and7.2Hz),2.99(lH,m),5.08(lH,d,J = 6.3Hz), 5.09-5.24(2H,m),6.90(lH,d,J=1.2Hz),7.32-7.48(4H,m),7.64-7.72(3H,m),8.20(l H,d,J=1.2Hz)>9.00(lH,s). IR(CHC13):3464,3375,2275,3022,2956,1707,1005,1490,1449,1356,1322,12 19,1 147,113 1/cm. [a]D=+21.6。(CHC13.01.01,23Χ:). 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 153 A7 五 、發明説明( Β7 150
No.l a ~ 1 8 6 CDC13:300MHz 1.36.2.24(14H,m),2.31(2H,t,J=7.4Hz),2.49(lH,bs)f3.37(lH>m),3.67(3H,s),5.3S- 5.50(2H,m),7.40-7.68(9H,m). IR(CHC13):3375,1727,1602,1435,1362,1221,1207,1168,1045/cm.
No.l a - 1 8 7 CDC13:300MHz 1.10-2.25(14H,m),2.36(2H,t,J=7.2Hz),2.47(lH,m),3.37(lH,m),5.3H54(2H,m), 5.62(lH,d,J=7.2Hz),7.39-7.70(9H,in). IR(CHC13):3674,3496,3376,3234,3012,2952,2880,2650,n25(sh),1709,1602,14 85,1420,1360,1167/cm.
[a]D=+32。(CHC13,c=1.69)·
No· 1 a - 1 8 8 CDC13 200MHz 0.86-L92(14H,m),2.22(3H,m),2.36(3H,s),2.95(lH,m),3.67(3H,s),3.93(3H,s),4.8 l(lH,d,J=6.2Hz),5.04-5.20(2H,m),7.02-7.05(2Hfm),7.31(lH,d,J=8.6H2),7.39(l H,d,J=7.8Hz),7.79-7.89(3H,m). IR(CHC13):3385,3286,3029,3019,3015,2954,2877,1718,1617,1598,1567,1507,1 311,1269,1153 /cm.
[ajD= ·29.4。(CHC13,c=1.01,25t:)·
No. 1 a ~ 1 8 9 [a]D=-7.7a (CHC13,c=1.00,24t:).
No. 1 ci — 1 9 0 [a]D=-17.3。(CHC13.C=l.〇〇,2‘H)- 本纸張尺度適用中國國家標準(CNS ) Α4規格(210Χ 297公釐) (請也閱讀背*面之注意事項再β 經濟部中央標準局員工消費合作社印製
-154 513422 A7 B7 五、發明説明(151 經濟部中央標準局員工消費合作社印製 Νο·1 a — 1 9 1 CDC13 300MHz 0.95-2.20(14H,m),2.30(lH,m),2.36(2H,d,J=6.9Hz),3.21(lH,m),4.25(2H,s),5.07( lH,d,J=7.8Hz),5.35-5.48(2H,m),7.25(lH,dd,J=1.8 and 8.1Hz),7.32-7.35(2H,m ),7.59(lH,d,J=8.1Hz),7.94(lH,s),8.14(lH,d,J=2.7Hz),8.23(lH,d.d,J=2.7and8.7 Hz). IR(CHC13):3386,3026,3015,2957,2877,2633,1702,1617,1573,1530,1348,1123 / cm. [a]D= ·6·Γ (CHC13,c=1.01,25t:)· No.l a - 1 9 2 CDC13 300MHz 0.92.2.20(14H,m),2.13(3H,m),3.23(lH,m),3.64(3H,s),3.94(3H,s),4.22(2H,s),4.3 6(lH,d,J=7.8Hz),5.37-5.42(2H,m),7.16-7.42(6H,m),7.53(lH,d,J=8.4Hz),7.94(l H,s). IR(CHC13):3389,3022,3013,2953,2877,1716,1616,1560,1485,1340,1326,1124 / cm. [ck】D= -15.20 (CHC13,c=1.01,25t:)e No.l a - 1 9 3 CDC13 300MHz 0.92-2.20(14H,m),2.25(lH,m),2.35(2H,t,J=7.2Hz),3.17(lH,m),4.22(2H,s),4.91( lH,d,J=7.5Hz),5.37-5.42(2H,m),7.13-7.43(6H,m),7.60(lH,d,J=8.1Hz),8.05(lH, s). IR(CHC13):3511,3387,3029,3020,3011,2957,2877,2651,1698,1614,1560,1505,1 320,1280,1252,1126 /cm. [a]D= ·0.9〇 (CHC13,c=1.00,25t:)e 批衣-- ·*· (請先閱讀背面之注意事項再本頁) 線 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 155 - 513422 A7 B7 五、發明説明(152
No.lb— 1 CDC13 300MHz 0.98-1.56(15H,m),1.85-1.9O(5H,m),2.23(lH,m),3.05(lH,m),3.66(3H,s),4.77(lH, d,J=6.0Hz),5.08-5.28(2Hlm),7.46(3H,m),7.38.7.54(2H,d,J=7.5Hz),7.72(2H,d,J= 8.4Hz),7.93(2H,d,J=8.4Hz). IR(CHC13):3384,3028,2952,2876,1719,1595,1391,1322,1155/cm.
[a ]436 +4.0^+6.0(011013,〇=1.00,23*0). mp.96-98t:
No.lb-2 ODC13 300MHz 0.98-1.52(15H,m),1.85.1.90(5H,m),2.17(lH,m),3.00(lH,m),3.67(3H,s),4.05(2H, s),4.83(lH,d,J=6.0H2),5.05-5.23(2H,m),7.14(2H,d,J=7.2Hz),7.17-7.32(5H,m),7. 78(2H,d,J=8.4H2). IR(CHC13):3384,3026,2952,2874,1719,1595,1453,1407,1320,1180/cm. [a:}D=+2.5a (CHC13,c=1.02,24t:).
No. lb — 3 CDC13 300iMHz 0.96·2.05(20Η,ιη),2.07(1Η,πι),3·07(ΐΗ,ιη),4.04(2Η,3),5.21·5.35(2Η,ιη),5.55(ΐΗ, drJ=6.9Hz)f7.14(2H>d>J=6.6Hz),7.20-7.32(5H,ra),7.78(2H,d,J=8.lH). IR(CHC13):3250,3022,2950,1699,1596,1495,1453,1405,1318,1153/cm. 經濟部中央標準局員工消費合作社印裝 [Q^D= +17.Γ (CHC13,C=l.〇l,25t:). mp.129-131t:.
No. lb — 4 CDC13 200MHz 0.90.2.L0(15H,m)tI.L9(3H,s)t1.20(3Hfs),3.il(lH,m),5.24-5.32(2H,m),5.70(lHt d,J-6.6Hz),7.38*7.68(4H,m),7.96-8.04(2H,m),8.53(lH,d,J=i.4H2). 156 本纸張尺度適用中國國家標準(CNS ) Λ4規格(210X 297公釐) 513422 A7 B7 五
發明説明(1W 經濟部中央標準局員工消費合作社印製 IR(CHC13):3384,3246,2958,1701,1632,1595,1468,1445,1322,1216,1202,1190,1 155,1122/cm. [a]D=+10.8° (σΗ013,0=0.51,23Χ:). No.lb — 5 1.02-2.10(15H,m),1.16(6H,s),3.02(lH,m),4.09(3H,s),5.23-5.28(2H,m),5.76(lH, d,J=7.2Hz),7.36-7.63(4H,m),7.97(lH,d,J=7.8Hz),8.16(lH,s). IR(CHC13):3369,2959,1702,1635,1585,1468,1454,1441,1415,1318,1222,1189,1 170,1154/cm. [a]D=+9.9° (011(:13,0=1.00,23^). No.lc— 1 CDC13 300MHz 1.10- 2.02(14H,m),2.27(2H,t,J=7.5Hz),2.50(lH,m),2.89(3H,s),3.31(lH,m),3.64( 3H,s),5.16-5.30(2H,m),7.34-7.42(3H,m),7.50-7.59(2H,m)f7.62-7.68(2H,m),7.76-7.82(2H,m). IR(CHC13):3020,2946,2868,2212,1727,1596,1495,1437,1339,1156,1135,1084 / cm. [a 】D=-16.1° (01^13,0=1.05,25.0=). m.p.100-102t: No.lc — 2 CDC13 300MHz 1.10- 2.05(14H,m),2.23(2H,t,J=7.5Hz),2.53(lH,m),2.91(3H,s),3.35(lH,m),3.62( 3H,s),5.02-5.30(2Hfm),7.50-7.60(3H,m),7.90.8.08(6Htm). IR(CHC13):3〇 16,2946,2868,1728,1437,1398,1340,1160,1086 /cm. [a]D=-32.5° (ΟΗ013,〇=1.00,25.0^:). No. lc — 3 (請先閱讀背面之注^^事項再本貢) -裝·
、1T 線 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 157 513422 A7 B7 五、發明説明(154) CD30D 300MHz 1.15.2.05(14H,m),2.13(2H,t,J=7.2Hz),2.47(lH,m),2.91(3H,s),3.27(lH,m),4.90· 5.30(2Η,πι),7.37.7.44(3Η,ιη),7.53-7.61(2Η,ιη),7.71-7.77(2Η,ιη),7.81-7.87(2Η,ιη ). IR(KBr):3412,2999,2951,2871,2217,1560,1399,1243,1159,1137,1103,1084. [qj]D=-8.6° (CH3OH,c=1.03,23t:).
No· Id — 1 CDC13 300MHz l. 00-2.16(15H,m),2.36(2H,t,J=7.2Hz),3.17(lH,m),3.33(3H,s),5.23.5.43(3H,m), 7.δ1-7.δ9(3Η,ιη),7.91.8.10(6Η,ιη),9.02(ΐΗ^Γ8). IR(CHC13):3382,3268,3028,2954,2874,1715,1442,1400,1337,1162,1120,1089/c m.
[a]D=+40.0° (CHC13,O0.53,22t:)·
No.ld- 2 CDC13 300MHz 1.03-2.30(17H,m),3.03(lH,m),4.03(2H,s),5.26(2H,m),5.84(lH,br),5.25-5.29(lH, d,J=6.6Hz),6.03(lH,br),7.14(2H,d, J=8.lHz), 7.26-7.3 l(5H,m),7.80(2H,d,J=S.l Hz). IR(CHC13):3376,3002,2946,1669,1595,1492,1454,1406,1318,1154/cm. [a]D=+4.3〇 (CHC13,c=1.00,23t:). 經濟部中央標準局員工消費合作社印製 (請先閱讀背面之注意事項再本頁)
No.ld-3 CDC13 300MHz 0.96-2.17(17H,m),2.33(2H,t,J=6.9Hz),3.01(lH,m),4.04(2H,s),5.10(lH.d,J=G.6H z)>5.21.5.26(2H,m)f7.14(2H,dIJ=8.7Hz),7.16-7.32(5H,m),7.78(2H,d,J=8.4Hz). IR(CHC13):3260,3020,2946,1711,159G,1492,1457,H07,L3 18, U54/cm. [a]D=+9.3° (CHC13,c=1.09,25t:). 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 158 513422 A7 B7 155 五、發明説明
No.Id — 4 CDC13 300MHz 0.95-2.14(15H,m),2.34(2H,t,J=7.2Hz),3.09(lH,m),3.30(3H,s),4.04(2H,s),5.19(l H,d,J=7.2Hz),5.22.5.39(2H,m),7.10-7.35(7H,m),7.81(2H,d,J=8.lHz),9.10(lH,b rs). IR(CHC13):3382,3260,3028,2952,2874,2670,1713,1595,1492,1450,1405,1338,1 160,1120,1092/cm.
[o:】D=+22.2。(CHC13,C=1.07,22t:).
No. Id ~ 5 CDC13 300MHz 1.00-2.10(14H,m),2.30-2.39(3H,m),3.15(lH,m),3.35(3H,s),5.18-5.40(3H,m),7.4
l(lH,d.t.,J=0.9and7.8Hz),7.50.7.69(3H,m),7.88-8.15(2H,m),8.60(lH,d,J=1.5H z),9.06(lH,s). IR(CHC13):3382,3268,3028,2954,2874,1714,1442,1402,1338,1188,1155,1 121,1072/cm.
[a]D=+15.3° (CHC13,C=1.00,22X:)· !
No. le — 1 CDC13 300MHz 1.19-2.45(19H,m),2.58(lH,m)I5.63(lH,d,J=3.0Hz),7.42-7.65(4Hlm),7.94-8.03(2 H,m),8.49-8.50(lH,m). 經濟部中央標準局員工消費合作社印製 IR(CHC13):3293,3024,1710,1595,1584,1467,1445, H 10,1324,1222,12 13,1206,1 190,1160/cm.
[a]D=-41.1° (CHCi3,C=1.01,23r).
No. le - 2 CDCI3 300iMHz 本纸張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 159 513422 A7 B7 經濟部中央標準局員工消費合作社印製 五、發明説明(156 ) 1.10-2.25(19H,m),2.94(lH,m),4.12<3H,s),5.53(lH,d,J=7.2Hz),7.39(lH,m),7.50· 7.62(3H,m),7.96(lH,d,J=7.5Hz)fS.13(lH,s). IR(CHC13):3367,3025,2955,1711,1634,1600,1584,1468,1454,1440,1415,1342,1 317,1222,1189,1157/cm. [a]D=+1.2° (CHC13,C=1.00,25t:). No.lf - 1 CDC13 300MHz ^ 1.08- 2.47(19H,m),2.56(lH,m),3.52(2H,t,J=6.6Hz),5.59(lH,d,J=2.4H2),7.40.7.6 6(4H,m),7.95-8.04(2H,m),8.50(lH,d,J=1.8Hz). IR(CHC13):3624,3383,3295,2950,2877,1705,1595,1584,1468,1445,1405,1347,1 337,1324,1224,1190,1160/cm. ; [a]D=-54.1〇 (CHC13,C=1.01,23t:). No.lf— 2 CDC13 300MHz 1.08- 2.24(19H,m),2.94(lH,m),3.53(2H,t,J=6.3Hz),4.13(3H,s),5.47(lH,d,J=6.6H z),7.36-7.63(4H,m),7.96(lHld,J=6.3Hz)f8.14(lH,s). IR(CHC13):3625,3368,3025,3013,2949,2877,1710,1634,1600,1584,1468,1454,1 440,1415,1342,1317,1232,1220,1189,1157/cm. [a]D=-5.6° (CHC13,C=1.00,25t:). No. lg — 1 CDC13 200MHz 1.17.2.34(15H,m)t3.22(lHfm),5.10.5.16(2H,m),5.45(lH,d,J=7.0Hz),7.35-7.66(4 H,m),7.95-8.01(2HIm),8.51(lHld,J=2.0Hz). IR(CHC13):3383,3275,2959f 1707,1595,1584,1468,1445,1425,1319,1269,1248,1 ; 190,1 149,1123/cm. MD=+64.3。(CHC13,C=1.〇l,23t:). (請先閲讀背面之注意事項再^一^本百〇 裝·
、1T 線 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 160 513422 A7 B7 五、發明説明(157 ) 經濟部中央標準局員工消費合作社印製
No.lg- 2 CDC13 300MHz 1.10-2.15(13H,m),2.36(2H,t,J=7.2Hz),3.21(lH,m),4.09(3H,s),5.10-5.22(2H,m), ' 5.43(lH,d,J=7.8Hz),7.36.7.62(4H,m),7.96(lH,d,J=7.8Hz),S.12(lH,s). | ! IR(CHC13):3366,2959,1708,1635,1600,1585,1467,1454,1440,1415,1345,1318,1 | 233,1189,1152/cm. [a]D=+103.1° (CHC13,C=1.01,23t:). No.lh— 1 CDC13 300MHz 0.90-1.60(17H,m),1.83(lH,m),2.11(lH,m),2.22(2H,t,J=7.2Hz),3.07(lH,m),5.11( lH,d,J=7.2Hz)>7.38-7.47(lHIm),7.50-7.60(lH,m),7.60-7.72(2H,m),7.88-8.12(2 H,m),8.54(lH,d,J=0.9Hz). IR(CHC13):3382,3274,2926>1707,1464,1442,1318,1266,1188,1153f1121,1105,l 071,1019/cm. ί [a]D=-2.8。(CHC13,C=1.01,23r). j No.li- 1 [a]365 +50.9〇 (CHC13,c=1.01,24t:). ; No.li- 2 CDC13 300MHz 0.98-1.70(llH,m),1.80-2.O0(5H,m),2.19(lH,m),3.03(lH,m),3.64(2H,t,J=6.6Hz), 4.05(2H,s),4.69(lH,d,J=6.6Hz)l5.15(lH,m),5.25(lH,m),7.16(2H>d,J=7.2Hz)(7.2 :, 7-7.32(5H,m),7.77(2H,d,J=8.4Hz). IR(CHC13):3376,3004,2946,2316,1596,1492,1453,1407,13 18,1 154/cm. +3.5° (CHC13,c=1.00,22t:). mp .80.5*82.0^3 I , —- I .......- Hi -·- ii 1—! ........................ 1-1- ϋ (請先閲讀背面之注意事項再尽頁) -11 綉 本纸張尺度適用中國國家標準(CNS ) Λ4規格(210X 297公釐) 161 513422 A7 B7 五、發明説明(158 )
No.lj - 1 [a】436=-7.5±0.5.(CHC13,c=1.05,22t:)·
No.lj— 2 [a]D==-9.7±0.5.(CHC13,c=1.06,22t:).
No.lj - 3 [or 】D==+15.0土 0.5 (0113011,0=1.06,24.51 )·
mp. 101- lOS'C
No.lj — 4 -- [a ]D==-28.0 土0.6 (011(313,0=1.06,241). mp. 159-16 l'C lj-δ
[a]D==-l2.5±0.5.(CHC13,c=1.04,23t:)· mp.99-10 lC
No.lj — 6 CDC13 300MHz 0.90-2.03(14H,m),2.20(lH,m),2.30(2H,t,J=7.3Hz),3.00(lH,m)3.68(3H,s),4.76(l H,dlJ=6.8Hz),5.13.5.35(2H,m),7.01-7.08(4H,m),7.19-7.26(lH,m),7.37.7.46(2H, 經濟部中央標準局員工消費合作社印製 m),7.80-7.84(2H,m). IR(CHC13):3382,3280,3080>3016,2952,2900,1727,1582, I486,1432,1322,1150/c m.
[a]D= -31.0。(CHC13,0=1.05,261).
No. lj 一 ’ 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 162 513422 A7 B7 五、發明説明(159 ) 經濟部中央標準局員工消費合作社印製 CDC13 300MHz 0.91-2.09(14H,m),2.15(lH,m),2.35(2H,t,J=7.5Hz)>3.01(lH,m),5.17(lH,d,J=6.8 Hz),5.21-5.34(2H,m),7.01.7.08(4H,m),7.15-7.27(lH,m),7.37-7.43(2H,m),7.80.7. 85(2H,m). IR(CHC13):3474,3386,3270,3024,2958,2900,2675,1711,1584,1488,1420,1323,1 | 298,1150/cm. [a】D= -13.4。(CHC13,c=1.01,26t:)· No.lj — S CDC13 300MHz 〇.95.2.14(13H,m),2.30(2H,t,J=7.5Hz),2.36(lH,m),2.S4(lH,m),2.91(lJ=4.8Hz), 3.66(3H,s),5.33-5.52(2H,m),6.82.6.87(lH,m),6.93-7.00(2H,m),7.09-7.15(4H,m), 7.2S-7.36(2H,m),7.54.7.59(lH,m). IR(CHC13):3350,3010,2950,2880,172S, 1603,15S2,14S9 1461,1438,1360,1160/c m. [α]Ώ= +75.1° (CHC13,c=L13,26t:). No.lj-9 CDC13 300MHz 0.95-2.03(14H,m)f2.20(lH,m)f2.29(2H,tfJ=7.5Hz),3.06(lH,m),3.68(3H,s),4.98( lH,d,J=7.4Hz),5.14·5.34(2H, m),7.46-7.54(2H,m),7.60-7.68(lH,m), 7.75-7.80(2 H,m),7.88-7.92(2H,m),7.99-8.03(2H,m)· IR(CHC13):3384,3280,3020,2960,2888,1727,1662,1600,1316,1273,1163/cm. [ajD= ·41.0〇 (CHC13,c=1.17,26t:). No.lj - 10 CDC13 + CD30D 300MHz 0.94-2.08(14H,m),2.21(lH,m),2.34(2Hlt,J=6.2Hz),3.0-t(LH,m).5.2i-5.35(2H,m),' 5·40(ΐΗ,ηι)·7·49·7.53(2Η,πι)·7.64.7.68(ΐΗ,πι),7.79.8.06(6Η,Γη). (請先閱讀背面之注意事項再頁) vs -口 本纸張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 163 1J422 A7 B7 五 、發明説明(16〇) IR(CHC13):3475,3370,3250,3018,2956,2976,2650,1709,1662,1595,1445,1420, 1395,1317,1274,1163/cm. [a]D= -17.1° (CHC13,c=1.13,25t:). No.lj-11 CDC13 3Ό0ΜΗζ 1.06-1.98(14H,m),2.24-2.29(3H,m),3.13(lH,m),3.66(3H,s),5.10-5.24(2H,m),5.4 0(1H, d, J=6.3Hz),7.39·7·49(3Ή, m), 7.59-7.64(3H,m),7.80-7.83(2H,m), 8.08-8.11( lH,m). IR(CHC13):3302,3012,2948,2905,1727,1661,1593,1435,1332,1312,1287,1271,1 165/cm. [a]D= +15.6。(CHC13,c=1.03,26t:).
No.lj — 1 2 CDC13 300MHz 1.0S-1.98(14H,m),2.23(lH,m),2.33(2H,t,J=7.5Hz),3.16(lH,m),5.1S-5.26(2H,m), 5.39.5.45(lH,m),7.39-7.49(3H,m),7.60-7.64(3H,m),7.80.7.S3(2H,m),8.09-8.12( lH,m). IR(CHC13):3325,3022,2956,2872,2680,1708,1662,1603,1598,1425,1340,1316,1 288,1271,1165/cin. [a]D= +9.7e (CHC13,c:0.52,25t:). 請 閲 讀 背 面 之 注 意 事 項 再 頁 裝 線 經濟部中央標準局員工消費合作社印製
No. lj - 13 CDC13 300MHz 0.95-2.00(14H,m)l2.20(lH,m),2.27(2H,t,J=6.3Hz),3.03(lH>m),3.67(3H,s),4.99( lH,d,J=6.6Hz),5.12-5.31(2H,m),7.47-7.55(2H,m),7.6〇.7.69(2H,m), 7.76-7.81(2 H,m),7.96-8.05(lH,m),8.08.8.14(lH,m),8.27-8.28(lH,m). IR(CHC13):3674,3538,3376,3276,30 12,2948,2860,1726,1GG2,1595, U40,1335,1 317,1297,1274,1 166,1 150/cm. 本纸張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 164 513422 A7 B7 五、發明説明(161 經濟部中央標準局員工消費合作社印製 [a]D=+10.2° (CHC13,c=1.00,25t:). No.lj — 14 CDC13 300MHz 0.93-2.08(14H,m),2.21(lH,m),2.32(2H,t,J=6.3Hz),3.00(lH,m),5.20-5.36(2H,m), 5.38(lH,d,J=6.2Hz),7.50-7.55(2H,m),7.63-7.71(2H,m),7.77-7.81(2H,m),7.99-8. 04(lH,m),8.10-8.18(lH,m),8.32-8.36(lH,m). IR(CHC13):3674,3480,3374,3258,3012,2950,2875,2650,1709,1662,1598,1418,1 335,1317,1274,1143/cm. [a]D=+61.0〇 (CHC13,c=1.19,25t:). No.lj - 15 : CDC13 300MHz 0.90-2.00(14H,m),2· 19(lH,m),2.30(2H,t, J=7.3Hz),3.01(lH,m),3.67(3H,s),4.82( lH,d,J=6.6Hz),5.14-5.34(2H,m),7.36-7.39(3H,m),7.53-7.57(2H,m),7.62.7.66(2 H,m),7.83-7.88(2H,m). IR(CHC13):3376,3276,3010,2948,2868,2212,1727,1597,1500,1437,1325,1161/c m. [a]D=-7.2〇 (CHC13,c=1.00,26t:). No. lj — 16 CDC13 300MHz 0.93-2.03(14H,m),2.15(lHfm),2.36(2H,t,J=7.5Hz),3.05(lH,m),5.20-5.40(3H,m), 7.36-7.39(3H,m),7.55-7.66(4H,m),7.84-7.88(2H,m). IR(CHC13):3470,3376,3260,30 12,2950,2868,2675,22 12,1708,1596,1503,1416,1 396,1322,1 160. [u jD = -22.4° (CHC13,c=1.00,26t:).
No. lj ~ 17 本纸張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) (請先閲讀背面之注意事項再 -裝 頁) 訂 線 165 513422 A7 B7 五、發明説明(162 經濟部中央標準局員工消費合作社印製 CDC13 300MHz 1.00-1.60(9H,m),1.79-1.89(5H,m),2.17(lH,bs),2.23(2H,t,J=7.2Hz),3.03(lH,m), 5.10-5.23(2H,m),5.49(lH,d,J=6.6Hz),7.40(lH,t,J=7.4Hz),7.53(lH,t,J=7.2H2),7. 60-7.68(2H,m),7.98-8.03(2H,m),8.55(lH,d,J=1.5Hz). IR(CHC13):3516,3384,3270,2666,1708,1632,1595,1584,1467,1445,1425,1374,1 345,1321,1269,1248,1218/cm. [a]D= ·7·8 0 (CHC13,c=1.01,22r)· No. lj — 18 CDC13 300MHz 0.90-2.03(14H,m),2.19(lH,m),2.30(2H,t,J=7.5Hz),3.00(lH,m),3.67(3H,sM.80( lH,d,J=6.4Hz),5.14-5.35(2H,m),6.99-7.04(2H,m),7.16-7.22(2Hlm),7.34-7.49(4 H,m),7.57-7.61(lH,m). IR(CHC13):3376,3276,3012,2948,2875,1727,1583,1488,1471,1432,1330,1311,1 150/cm. [a]D=+54.0° (¢^013,(:=0.99,251). No.lj- 19 CDC13 300iMHz 0.91-2.09(14H,m),2.15(lH,m),2.34(2H,t,J=7.5Hz),3.01(lH,m),5.16(lH,d,J=6.6 Ηζ),5·24·5.40(2Η,ιη),7.01·7.08(2Η,ιη),7.15·7.25(2Η,Γη),7.35-7.53(4Η,Γη),7.59-7. 65(lH,m). IR(CHC13):3470?3376,3260,3012,2950,2875,2640,1708,1583,1488,147 1,1430,1 335,1305,1149/cm. [a]D= -21.0。(CHC13.c=1.30,25t:).
No.lj- 2 0 CDC13 300MHz 1.17(lH,m), 1.26-L34(2H,m),l-54-2.24(l lH,m),2.31(2H,t,J = 7.4Hz),2.48( 1 H.bs), 本纸張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) (請先閲讀背面之注意事項再頁) 裝_
、1T 絲 166 513422 A7 B7 五、發明説明(163 3.37(lH,m),3.67(3H,s),5.35-5.50(2H,m),7.39-7.68(9H,m)· IR(CHC13):3377,1727,1601,1435,1362,1168/cm.
No.lj — 2 1 CDC13 300MHz l,l〇.2.25(14H,m),2.36(2H,t,J=7.2Hz),2.47(lH,m),2.89(lH,m),5.35-5.53(2H,m)l 5.63(lH,d,J=7.2Hz),7.40-7.71(9H,m). IR(CHC13):3674,3496,3374,3234,3010,2952,2870,2640,1730(sh), 1710,1605,14 85,1425,1360,1167/cm.
[a]D=-43.0° (CHC13,c=1.01,25t:)·
No.lj — 2 2 CDC13 300MHz 0,98-1.95(14H,m),2.25-2,31(3H,m),2.95(lH,m),5.19-5.30(2H,m),5.33(lH,d,J=3. 9Hz),6.58(lH,d,J=7.5H2),6.80(lH,t,J=7.5Hz),6.99-7.05(lH,m),7.44-7.53(6H,m), 7.60-7.73(9H,m)f7.94-7.73(3H,m),8.23-S.26(2H,m),10.66(lH,s). IR(CHC13):3475,3372,3260,3008,2952,2868,2722,1725,1710(sh)f 1663,1590,15 7 1,1525,1448,1437,1345,1314,116 l,1112/cm.
[a]D=+12.9° (CHC13,c=0.12,23t:).
No.lj — 2 3 CDC13 300MHz 經濟部中央標準局員工消費合作社印製 0.94-1.94(14H,m),2.23-2.30(3Hfm),2.98(lH,m),3.68(3H,s),5.09{lH,d,J = 6.2Hz), 5.15-5.28(2H,m),7.14-7.22(lH,m),7.34-7.42(2H,m),7.68-7.73(2H,m),7.89-8.03( 4H,m),8.51(lH,s). IR(CHC13):3372,3275,1724,1673,1599,1438,1320,116 1/cm.
[a]D二 +17,0 〇 (CHC13.(:=1.38,251).
No. lj - 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 167 513422 A7 B7 五、發明説明(164 CDC13+CD30D 300MHz 0·96·2.05(14Η,ιη),2,25-2.34(3H,m),2.92(lH,m),5.16-5.34(2H,m),7.14-7.22(1H, m),7.29-7.42(2H,m),7.70(2H,d,J=7.6Hz),7.92-8.05(4H,m). IR(CHC13):3616,3426,3375,3010,2950,2828,2645,1708,1672,1599,1439,1323,1 161/cm.
[a]D=+21.0° (ΟΗ3ΟΗ,ο=1.00,22^).
No.lj— 2 5 CDC13 300MHz 1.03(lH,m),1.18-2.01(13H,m),2.20(lH,bs),2.27(2H,t,J=7.4Hz),3.08(lH,m),3.66 (3H,s)>5.11(lH,d>J=6.6Hz),5.14-5.34(2H,m),7.54-7.62(3H>m),8.04-8.32(6H,m). IR(CHC13):3384,3278,1726,1605,1484,1448,1331,1161/cm.
No.lj- 2 6 CDC13+CD30D 300MHz l,03-2.10(14H,m),2.22(lH,m).2.31(2H,t,J=7.5Hz),2.98(lH,m),5.23-5.38(2Hfm), 7.55-7.66(3H,m),8.05-8.08(2H,m)f8.14-8.18(2Hfm),8.28-8.31(2H,m). IR(Nujol):3260,2720,2660,1711,1545,1460,1317,1163/cm.
[〇f】D=+15.8e (CH3OH,c=1.01,22t:)·
No.lj - 2 7 [or]D= +16.7° (CHC13,c=1.00,23t:). 經濟部中央標準局員工消費合作社印製
No.lj- 2 8 CDC13 300MHz 1.0 l(lH,m),1· 14· 1.29(2H,m),1.46-2.19(1 lH,m),2.33(2H,t,J=7.2Hz),2.41(lH,bs), 3.18-3.21(5H,m),3.68(3H,s),3.73-3.76(4H,m),4.37(lH,d,J=7.2Hz),5.35-5.45(2H, m). IR(CHC13):3392,1727,1435,1335,1148/cm. 168 本紙張又度適用中國國家標準(CNS ) A4規格(210X 297公釐) 513422 A7 B7 五、發明説明(165 [a]D= +10.7 ° (CHC13,c=1.39,26t:)·
No.lj - 2 9 CDC13 300MHz 1.00(1H,m),l.20-1.29(2H,m),l,48-2.25(12H,m),2.37(2H,t,J=7.2Hz)„3.17-3.22(5 H, m),3.74-3.79(4H,m),4.79(lH,d,J=7.8Hz),5.34-5.54(2H,m). IR(CHC13):3470,3390,3270,2675,1709,1455,1420,1315,1147/cm.
[a]D= +16.8 〇 (CHC13,c=1.42,26t:)·
No.Ik — 1 [a]D= ·25·4〇 (CHC13,c=1.08,23t:)·
No.lk- 2 CDC13 200MHz I. 07-2.28(14H,m),2.32(2H,t,J=7.4Hz),2.63(lH,m),3.63(3H,s),3.93(lH,m)>5.30-5.52(2H,m),6.35(lH,d>J=7.0Hz),7.48-7.60(3H,m),7.88-8.02(6H,m). IR(CHC13):3438,3002,2946,2868,1727,1652,1514,1485,1363,1310,1245,1154 / cm.
[a]D==-80.4° (ΟΗΟ13,ο=1.01,24.0Τ:).
No.Ik — 3 CDC13 200MHz 經濟部中央標準局員工消費合作社印製 1.10-2.26(14H,m),2.37(2H,t,J=7.2Hz)t2.60(lHfm),3.93(lH,m),5.30-5.50(2H>m), 6.33(lH,d,J=7.5Hz),7.48-7.58(3Hlm),7.88.7.99(6H,m). IR(CHC13):3446,3004,2952,2874,1709,1652,1515,1485,1305,1153 /cm.
[α ]D==-96.4。(CHC13,c=l.05,23.Ot:)·
No.lk- 4 CDC13 300MHz 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 169 2234 A7 B7 五、發明説明(166) 1.05- 2.17(14H,m),2.38(2H,t,J=7.2Hz),2.52(lH,m),3.81(lH,m),5.33-5.50(2H,m), 6.08(lH,d,J=7.6Hz),7.39-7.53(3H,m),7.57-7.62(6H,m). IR(CHC13):3420,3250,3008,2948,2870,2660,2208t1735(sh), 1705,1640,1500/cm | • i [a】D=-21.9士0.6〇 (CHC13,c=1.02,22t:)·
No.lk — 5 CDC13 300MHz 1.05- 2.14(14H,m),2.38(2H,t,J=7.2Hz),2.51(lH,m),3.81(lH,m),5.34-5.46(2H,m), 6.07(lH,d,J=7.6Hz),7.33-7.56(5H,m). IR(CHC13):3422,3250,3010,2950,2876,2664,2558,2210,1735(sh), 1705,1645,15 02,1441,1410,1307,1276/cm.
[a ]D=-63.6士 1.9。(CHC13,c=0.56,22t:)·
No.lk — 6 CDC13 300MHz 1.04.2.24(14H,m),2.36(2H,t,J=7.5Hz),2.58(lH,m),3.88(lH,m),5.30-5.43(2H,m), 6.21(lH,d,J=7.2Hz),7.41-7.49(3H,m),7.73-7.77(2H,m)· IR(CHC13):3447,3011,2955,1708,1653,1603,1578,1515,1486,1457,1312,1211,1 164/cm.
[a]D=-60.3° (CHC13,C=1.00,23t:). 經濟部中央標準局員工消費合作社印製
No. Ik— 7 CDC13 300MHz 1.04.2.22(14HJm),2.36(2H>t,J=7.2Hz),2.57(lHfm),3.87(lH,m),5.30-5.44(2H,m)l 6.17(lHld,J=8.7Hz)>6.99-7.40(7H,m),7.73(2H,dtJ=7.5Hz). ; IR(CHC13):3449,3013,2955,1739,1708,1651,1609,1588,1522,1487,1243,1227,1 ! 169/cm.
[¢^1)=-60^((^000.92,231). 本紙張尺度適用中國國家森準(CNS ) A4規格(210X 297公釐) -170 - 513422 A7 B7 五、發明説明(167 )
No.lk — 8 CDC13 300MHz 1.04-2.25(14H,m),2.34(2H,t,J=7.5Hz),2.56(lH,m),3.87(lH,m),5.30-5.44(2H,m), 6.19(lH,d,J=7.5Hz),6.83-6.94(6H,m),7.69(2H,d,J=8.7Hz). IR(CHC13):3599,3455,3012,2955,1711,1644,1604,1577,1524,1507,1492,1290,1 236,1197,1170/cm. [a]D=-47.7° (CHC13,C=1.01,22X:)· No.lk — 9 CDC13 300MHz L04.2.20(14H,m),2.31(3H,s),2.36(2H,t,J=7.2Hz),2.56(lH,m),3.86(lH,m),5.30-5.43(2H,m),6.16(lH,d,J=7.2Hz),7.00-7.11(6H,m),7.74(2H,d,J=8.7Hz). .IR(CHC13):3450,3010,2955,1750,1709,1651,1609,1596,1523,1489,1370,1247,1 227,1183/cm. [ct]D=-54.r (CHC13,C=L01,22t:).
No.lk — 10 CDC13 300MHz 1.04-2.22(14H,m),2.35(2H,t,J=7.2Hz),2.56(lH,m),3.82(3H,s),3.86(lH,m),5.30-5.43(2H,m),6.17(lH,d,J=6.9Hz),6.89-7.01(6H,m),7.70(2H,d,J=8.7Hz). IR(CHC13):3023,2955,1742,1708,1649,1613,1602,1577,1522,1507,1490,1227,1 210,1170/cm. [〇f]D=-58.r (CHC13,C=1.01,22t:)· 請 先閱 讀 背 δ之注 意 事 項再 ¥ 頁 裝 訂 線 經濟部中央標準局員工消費合作社印製
No. lm — 1 CDC13 300MHz 1.06-2.25(14H,m),2.32(2H,t,J=7.4Hz),2.61(lH,m),3.63(3H,s),3.91(lH,ni),5.33· 5.47(2H,m),6.24(lH,d,J=6.9Hz),7.35-7.38(3H,m),7.53-7.60(4H,m),7.75-7.78(2 本纸張尺度適用中國國家標隼(CNS ) A4規格(210X297公釐) 171 513422 A7 B7 五、發明説明(168 經濟部中央標準局員工消費合作社印製 H, m), IR(CHC13):3438,3008,2946,2875,2212,1732,1650,1605,1519,1496/cm. [a]D= +76° (CHC13,0=1.39,24^) No.lm — 2 CDC13 300MHz I. 05-2.20(14H,m),2.36(2H,t,J=6.2Hz),2.59(lH,m),3.89(lH,m),5.29-5.48(2H,m), 6.26(lH,d,J=7.0Hz),7.26.7.38(3H,m),7.52-7.60(4H,m),7.73-7.77(2H,m)e IR(CHC13):3444,3012,2952,2874,2664,2214,1718(sh), 1708,1649,1605,1520,14 98/cm. [a]D= +81·4β (CHC13,c=1.01,23t:) No.lm — 3 CDC13 300MHz 1.06-2.23(14H,m),2.32(2H,t,J=7.0Hz),2.62(lH,m),3.63(3H,s),3.93(lH,m),5.30· 5.50(2H,m),6·28(1Η,d,J=7.0Hz),7.38-7.51(3H, m), 7.58-7.67(4H,m), 7.83-7.88(2 H, m)〇 IR(CHC13):3438,3008,2948,2875,1783(w),1727,1650,1608,1580(w),1523,1501, 1482/cm. [a]D= +59° (CHC13,c=1.49,25t:) No.lm — 4 CDC13 300MHz I. 08-2.25(14H,m),2.36(2H,t,J=7.4Hz),2.59(lH,m)f3.91(lH,m),5.28-5.48(3H,m), 6.29(lH,d,J=7.4Hz),7.38.7.50(3H,m),7.61-7.67(4H,m),7.81-7.86(2H,m). IR(CHC13):3436,3010,2948,2868,1727,1715(sh), 1649,, 1615(w), 1524,1502,1482, 1372/cm. [〇MD= +720 (CHC13,c=0.98,25t:) (請先閱讀背面之注意事項再 •裝- 頁) 訂 線 本紙張尺度適用中國國家標準(CMS ) A4規格(210X297公釐) 172 513422 A7 B7 五、發明説明(169
No.lm — 5 CDC13 300MHz 1.09- 2.20(14H,m),2.32(2H,t,J=7.2Hz),2.63(lH,m),3.63(3H,s),3.92(lH,m),5.3l. 5.51(2H,m),6.35(lH,d,J=7.0Hz),7.51-7.60(3H,m),7.92.7.97(6H,m). IR(CHC13):3436,3008,2946,2875,1727,1652,1608(w), 1515,1484/cm.
[a]D= +82。(CHC13,c=0.99,25t:)
No.lm — 6 CDC13 300MHz 1.09- 2.23(14H,m),2.37(2H,t,J=7.2Hz),2.60(lH,m),3.92(lH,m),5.30-5.49(2H,m), 6.32(lH,d,J=7.4Hz),7.51-7.55(3Hfm),7.85-7.98(6H,m). IR(CHC13):3436,3010,2950,2875,2670,1727,1715(sh),1650,1605(w), 1515,1484/ cm.
[a]D= +84° (011013^=1.54,25=)
No.lm— 7 CDC13 300MHz 1.03-2.18(14H,m),2.32(2H,t,J=7.4Hz)l2.59(lH,m),3.64(3H,s),3.89(lH,ni),5.29- 5.49(2H,m),6.16(lH>d,J=7.8Hz),6.98-7.06(4H,m)>7.14-7.20(lH,m),7.34.7.41(2 Η,Γη),7.73-7.78(2Η,ιη). IR(CHC13):3438,3008,2946t2868,1727,1648,1610,1586,1519,1485/cm.
[a】D= +54。(CHC13,c=1.29,25t:)· 經濟部中央標準局員工消費合作社印製
No.lm —8 . CDC13 300MHz 1.06.2.21(14H,m),2.36(2H,t,J=7.5Hz),2.58(lH,m),3.88(lH,m)l5.31-5.46(2Hfm), 6.17(lH,dlJ=6.9Hz)f6.99.7.05(4H,m),7.15.7*21(lH,m),7.36-7.41(2H,m),7.72-7. 75(2H,m). IR(CHC13):3436,3010,2948,2868,2675,1730(sh), 1709,1647,1608,1586,1520,14 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 173 五 、發明説明( 170 A7 B7 85/cm.
[a】D= +56。(CHC13,c=0.97,25t:)
No.lm — 9 CDC13 300MHz 1.05-2.18(14H,m),2.29-2.34(5H,m),2.59(lH,m),3.64(3H,s),3.89(lH,m),5.32-5.4 6(2H,m),6.16(lH,d,J=7.5H2)(7.00-7.11(6H>m),7.74-7.77(2H,m). IR(CHC13):3440,3010,2946,2868,1729,1649,1595,1519,1488/cm.
[a】D= +47。(CHC13,c=0.82,25X:)·
No.lm— 10 CDC13 300MHz 1.04- 2.20(14H,m),2.31-2.39(5H,m),2.57(lHfm),3.87(lHfm),5.28-5.47(2H,m),6.1 7(1H,d,J=7.0Hz),6.99-7.12(6H,m),7.72.7.76(2H,m). IR(CHC13):3674,3572f3438,3010,2948f2868,2626,1748,1710,1648,1615,1595,1 520,1489/cm.
[a】D= +5Γ (CHC13,c=0.91,25t:)
No.lm— 11 CDC13 300MHz 經濟部中央標準局員工消費合作社印製 (請先閲讀背面之注意事項再頁) 1.04- 2.16(14H,m),2.31(2H,t,J=7.2Hz),2.59(lH,m),3.63(3H,s),3.89(lH,m),5.29· 5.49(2Hfm),6.24(lH,d,J=7.4Hz),6.54(lH,s),6.83.6.93(6H,m),7.69.7.73(2H,m). IR(CHC13):3674,3588,3438,3296,3010,2946,2868,1725,1646,1603,1520,1504,1 489/cm.
[ajD= +51。(CHC13,c=〇.91,25t:)
No.lm- 1 2 CDC13 300MHz
1.04.2.21(14H,m),2.33(2H,t,J=8.0Hz),2.56(lH,m)>3.87(lH,m),5.28-5.48(2H,m)I 本紙張尺度適用中國國家標準(CNS ) A4規格(21〇χ297公釐) 174 513422 A7 B7 五、發明説明(171 經濟部中央標準局員工消費合作社印製 6.23(lH,d,J=8.0Hz),6.75(lH,m),6.87-6.94(6H,m),7.66-7.71(2H,m),9.63(lH,bs). IR(CHC13):3674,3582,3436,3275,3010,2950,2868,2675,1727,1710(sh), 1643,16 03,1522,1504,1490/cm. i [a]D= +30° (CHC13,c=0.97,25t:) | No.lm — 13 CDC13 300MHz 1.01-2.18(14H,m),2.31(2H,t,J=7.4Hz),2.58(lH,m),3.63(3H,s),3.82(3H,s), 3.89(1 H, m),5.29-5.48(2H,m),6.14(lH,d,J=7.0Hz),6.88-7.02(6H,m),7.70-7.74(2H,m). IR(CHC13):3442,3402,3004,2946,2868,1727,1648,1600,1518,1499/cm. [ct】D=+42。(CHC13,c=1.82,26t:) No.lm — 14 CDC13 300MHz I. 05-2.21(14H,m),2.35(2H,t,J=7.2Hz),2.55(lH,m),3.82(3H,s),3.88(lH,m),5.27-5.46(2H,m)f6.16(lH,d,J=7.2Hz),6.88-7.02(6H,m),7.68-7.73(2H?m). IR(CHC13):3438,3012,2948,2870,2650,1730(sh), 1709,1647,1615(sh), 1601,1519, 1492/cm. [a]D=+64e (CHC13,c=0.70,25t:) No.lm — 15 CDC13 300MHz 1.05-2.20(14H,m),2.29-2.36(5Hfm),2.62(lH,m)>3.63(3H,s)>3.92(lH,m),5.30-5.5 0(2H,m),6.25(lH,d,J=7.2Hz),7.16-7.21(2H,m),7.59.7.64(4H,m)>7.83-7.87(2H,m )· IR(CHC13):3446f3010,2946,2868,1745(sh), 1728,1650,1615,1525,1507,1486/cm.
[a]D=+65.0〇 (CHC13,c=l.〇2,23t:) 本纸張尺度適中國國家標準(CNS ) A4規格(210X297公釐) (請先閱讀背面之注意事項再 頁) 175 513422 A7 B7 五、發明説明(172 經濟部中央標準局員工消費合作社印製
No.lm— 16 CDC13 300MHz l. 08-2.21(14H,m),2.34-2.40(5H,m),2.59(lH,m),3.90(lH,m),5.29-5.48(2H,m),6.2 9(lH,d,J=7.0Hz),7.18(2H,d,J=8.6Hz),7.58-7.64(4H,m),7.83(2H,d,J=8.2Hz). IR(CHC13):3438,3012,2948,2870,2622,1749,1710,1649,1610,1526,1508,1487/c m. [o:】D=+66e (CHC13,c=1.21,24t:) No.lm — 17 CDC13 300MHz 1.06-2.19(14H,m),2.32(2H,t,J=7.2Hz),2.62(lH,m),3.63(3H,s),3.93(lH,m),5.30· 5.50(2H,m),6.32(lH,d,J=7.6Hz),6.41(lH,s),6.94(2H,d,J=9.0Hz),7.47(2H,d,J=9. 0Hz),7.58(2H,d,J=8.6Hz),7.81(2H,d,J=8.6Hz)· IR(CHC13):3580,3434,3284,3010,2946,2868,1726,1646,1606,1528,1490/cm. [〇r]D=+62.4e (ΟΗΟ13,=1·01,23ΐ:) No. lm - 18 CDC13+CD30D 300MHz l.ll-2.18(14H,m),2.32(2H,t,J=7.4Hz),2.59(lH,m),3.88(lH,m),5.30-5.49(2H,m), 6.55(lH,d,J=7.0Hz),6.92(2H,d,J=8.6Hz),7.47(2H,d,J=8.6Hz),7.59(2H,d,J=8.6H z)f7.79(2H,d,J=8.2Hz). IR(Nujol):3398,3175,2725,1696,1635,1601,1531,1510/cm. [ct]D=+99.5e (CH3OH,c=L011,25t:) No.lm— 19 CDC13 300MHz 1.05-2.20(14H, m),2.32(2H, t, J=7.4Hz),2.61(iH,m), 3.63(3H,s), 3.86(3H,s), 3.94(1 H,m),5.30-5.50(2H,m),6.24(lH,d,J=7.0Hz),6.99(2H,d,J=8.6Hz),7.53-7.63(4H,m ),7.82(2H,d,J=8.6Hz). --J-------批衣一— (請先閱讀背Vg之注^一思事項再頁) 訂 線 本纸張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 176 513422 A7 B7 五、發明説明(173 經濟部中央標準局員工消費合作社印製 IR(CHC13):3440,3006,2946,2875,1726,1649,1606,1527,1510,1489/cm. [a]D=+68° (CHC13,c=0.88,26=) No.lm — 20 CDC13 300MHz 1.09-2.20(14H,m),2.35(2H,t,J=7.3Hz),2.58(lH,m),3.85(3H,s),3.89(lH,m),5.28- 5.48(2H,m),6.3D(lH,d,J=7.2Hz),6.98(2H,d,J=8.8Hz),7.51.7.61(4H,m),7-Sl(2H, d,J=8.4Hz),8.34(lH,bs). IR(CHC13):3446,3012,2952,2881,2640,1730(sh), 1707,1647,1606,1527,1510,14 89/cm. [a]D=+83e (CHC13,c=1.00,25r). No.lm— 2 1 CDC13 300MHz 1.05.2.14(14H,m),2.37(2H,t,J=7.2Hz),2.51(lH,m),3.81(lH,m),5.34-5.46(2H,m), 6.11(lH,d,J=7.5Hz),7.33-7.48(3H,m),7.53-7.55(2H,m). IR(CHC13):3420,3250,3008,2948,2870,2660,2210,1735(sh), 1705,1645,1503,14 41,1409/cm. [a】D=+59.2± 1.0。 (CHC13,c=1.023,22t:)· No.lm — 2 2 CDC13 300MHz 1.05-2.17(14H,m),2.37(2H,t,J=7.2Hz),2.52(lH,m),3.82(lH,m),5.32-5.47(2H,m), 6.20(lH,d,J=7.6Hz),7.38-7.53(3H,m),7.58-7.61(6H,m),9.11(lH,bs). IR(CHC13):3420l3250l3010,2984,2870,2675f2208f1730(sh), 1705,1640,1500,14 06/cm. [a!D=+57.4〇 (CHCl3,c=1.83,23t:). No. 1 m ~ 2 3 (請先閱讀背面之注意事項再本頁) 本纸張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 177 513422 A7 B7 五、發明説明(174 CDC13 300MHz 1.05-2.18(14H,m),2.31<2H,t,J=7.5Hz),2.60(lH,m),3.63(3H,s),3.90(lH,m),5.32· 5.47(2H,m),6.22(lH,d,J=6.9Hz),7.40-7.49(3H,m),7.76-7.79(2H,m). IR(CHC13):3438,3008,2946,2868,1727,1651,1603,15S5,1512,1484/cm. [a】D=+52〇 (CHC13,c=1.49,25t:)· No.lm— 2 4 CDC13 300MHz 1.05.2.21(14H,m),2.36(2H,t,J=7.2Hz),2.57(lH,m),3.S9(lH>m),5.2S-5.47(2H,m), 6.22(lH,d,J=7.0Hz),7.39-7.55(3H,m),7.73-7.79(2H,m). IR(CHC13):3676,3572,3436,3010,2948,2875,1730(sh), 1709,1650,1600,1580,15 14,1484/cm. : [a]D=+57° (CHC13,c=0.97,26t:)· No.lm— 2 δ CDC13 300MHz 1.04-2.1S(14H,m),2.28-2.35(5H,m),2.59(lH,m),3.62(3H,s),3.88(lH?m),5.29-5.4 9(2H,m),6.20(lH,d,J=7.2Hz),7.15(2H,d,J=9.0Hz),7.S0(2H,d,J=8.8Hz). IR(CHC13):3436,3010,2946,2868,1752,1727,1653,1602,15 19,1491/cm. [a]D=+53° (CHC13,c=1.63,25r). (請先閱讀背面之注意事項再 -裝- 頁)
、1T 線 經濟部中央標準局員工消費合作社印製
No.lm - 2 6 CDC13 300MHz 1.05-2.19(14H,m),2.32.2.38(5H,m),2.56(lH,m),3.88(lH,m),5.29-5.47(2H,m),6.2 5(lH,d,J=7.4Hz),7.15(2Hld,J=9.0Hz),7.78(2H,d,J=8.6Hz). IR(ChTCi3):3434,3016,3006,2948,2880,2622,1752,1730(sh), 17 10,1651,1G05.15 20,1492/cm. (a]D=+58° (CHCl3,c=3.68,24t:) 本紙張尺度適用中國國家標準(CNS ) Α4規格(210X 297公釐) 178 5 2 42 3 ) Μ Β7 五、發明説明(175) 經濟部中央標準局員工消費合作社印製
No.lm— 2 7 CDC13 300MHz 1.05- 2.16(14H,m),2.30(2H,t,J=7.5Hz),2.57(lH,m),3.62(3H,s),3.87(lH,m),5.27·丨 5.47(2H,m),6.32(lH,d,J=7.4Hz),6.85(2H,d,J=8.6Hz),7.62(2H,d,J=8.6Hz),8.35( ! lH,s). IR(CHC13):3580,3450,3216,3010,2946,2868,1726,1640,1608,1584,1528,1496/0 m. [a]D=+56.2° (CHC13,c=0.713,23t:) No.lm— 2 8 CDC13 200MHz 1.10-2.25(14H,m),2.32(2H,t,J=7.2Hz),2.55(lH,bs),3.82.3.93(lH,m),5.27-5.47(2 H,m),6.25(lH,d,J=7.4Hz),6.86(2H,d,J=8.6Hz),7.62(2Hfd,J=S.6Hz). IR(CHC13):3438,3242,2675,1730(sh),1708,1639,1607,1585/cm. No.lm— 2 9 CDC13 300MHz 1.05- 2.18(14H,m),2.31(2H,t,J=7.4Hz),2.58(lH,m),3.64(3H,s),3.85(3H,s),3.89(1 H,m),5.29-5.48(2H,m),6.14(lH,d,J=6.6Hz),6.92(2H,d,J=9.0Hz),7.74(2H,d,J=9· 0Hz). IR(CHC13):3445,3008,2946,2868,1727,1646,1606,1578,1523,1493/cm. [o:]D=+53〇 (CHC13,c=2.03,24t:)
No. 1 m — 30 CDC13 300MHz 1.04-2.21(14Η,Γη),2.36(2Η,1,α=7.3Ηζ),2.δ6(ΐΗ,πι),,3.8δ(3Η,5),3.88(ΐΗ,πι),5.27-5.46(2H,m),6.15(lH,d,J=7.2Hz)l6.92(2H,d,J=8.6Hz),7.73(2H,d,J=8.6Hz). IR(CHCl3):3440,3010,2950,2870,2645f1727f ni0(sh),1646,1606,1575,1524, U 94/cm. 本纸張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) (請先閱讀背面之注意事項再 -裝- 頁) 訂 線 179 513422 A7 B7 五、發明説明(176) 經濟部中央標準局員工消費合作社印製 [a]D=+62° ((:11013^=1.10,241). No.lm— 31 CDC13+CD30D 300MHz 1.16-2.20(14H,m),2.31(2H,t,J=7.2Hz),2.59(lH,m),3.85(lH,m),5.31-5.51(2H,m), 7.13- 7.21(lH,m),7.31-7.42(2H,m),7.68-7.93(6H,m). IR(Nujol):3344,3175,2715,2675,1699,1631,1566/cm. [a]D=+67° (CH3OH,c=1.01,24t:)· No.lm- 3 2 CDC13 200MHz 1.09-2.23(14H,m),2.33(2H,t,J=7.1Hz),2.57(m,bs),3.40-3.93(9H,m),4.41(lH,bs), 5.29.5.48(2H,m),6.44(lH,d,J=7.4Hz),7.43(2H,d,J=8.2Hz),7.80(2H,d,J=7.8Hz). IR(CHC13):3434,3354,1726,1720(sh),1660(sh),1626/cm. No.lm — 33 CDC13 200MHz 1.14- 2.25(14H,m),2.37(2H,t,J=7.3Hz),2.64(lH,bs),3.93-4.01(lH,m),5.30-5.51(2 H,m),6.47(lH,d,J=7.4Hz),7.63-7.74(2H,m),7.79(2H,s),7.89-7.93(lH,m),8.00(lH, dd,J=2.3,1.0Hz),8.30(lH,d,J=1.0Hz),8.65-8.73(2H,m). IR(CHC13):3450,2675,1728,1707,1649,1528,1509/cm. [a 】D=+82.8± L2。((^0)13^=1.01,23=). No.2a-l
No.2a-2 CDC13 300MHz 0.99(lH,d,J=10.2Hz),1.15 and 1.24(each 3H,each s), 1.50-2.50(14H,m),4.30(1 本纸張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) ---:---r-----裝-- (請先閱讀背面之注意事項再本頁) 訂 線 180 513422 A7 B7 五、發明説明(177 ) H,m),5.35-5.52(2H,m),6.32(lH,dfJ=8.7Hz),7.36.7.49(3H,m),7.58-7.62(2H,m),7. 66 and 7.80(each 2H,each d,J=8.7Hz). , IR(CHC13):3116,3014,2925,2870,2663,1708,1651,1610,1524,1504,1484,1472 / cm.
[a]D= +64.Γ (MeOH,c=1.02,25t:).
No.2a-3 [a]D=+76.6°
No.2a-4 CDC13 300MHz 0.99(lH,d,J=10.2Hz), 1.15 and 1.25(each 3H,each s),1.64-2.51(14H,m),4.31(1 H,m),5.36-5.53(2H,m),6.33(lH,d,J=8.4z),7.50-7.56(3H,m),7.85-7.98(6H,m). IR(CHC13):3515,3452,3014,2925,2870,1740,1708,1654,1517, I486,1470 /cm. [a]D= +79.5。(MeOH,c=1.18, 22t:)·
No.2a-5 CD30D 300MHz 經濟部中央標準局員工消費合作社印製 0.98(1H,d,J=9.9Hz), 1.18 and 1.25(each 3H,each s),1.56-1.71(3H,m),1.98-2.4 0(llH,m),4.17(lH,m),5.41-5.52(2H,m)>7.52.7.61(3H>m)f7.91-8.01(6H,ra). IR(KBr):3416,3063,2983,2921,2869,1704,1643,1566,1518,1488,1408 /cm. [o:]D= +62·0β (MeOH,c=1.00, 25t:).
No.2a-6 [a]D=+64.1° (MeOH,c=1.01,25t:).
No.2a-7 [a jD=+65.3e (1^011/=0.99,25=). 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 181 513422 A7 B7 五、發明説明(178 經濟部中央標準局員工消費合作社印製
No.2a.8 [a】D=+74.0〇 (MeOH,c=1.01,25t:). No.2a-9 [a]D=+71.〇° (MeOH,c=1.10,25t:)· No.2a-10 [a]D=+74.7° (MeOH,c=1.00,25t:). No.2a-ll [ck]D=+72.1〇 (MeOH,c=1.00,25t:)· No.2a-12 [a]D二+53.10 (CHC13,c=1.01,26t:)· m.p.155.0-156.Ot: No.2a-13 CDC13 300MHz 0.98(lH,d,J=10.2Hz),1.18 and 1.25<each 3H,each s),l.63-2.40(14H,m),4.30(1 H,ra),5.46.5.58(2H,m),6.44(lH,dfJ=8.4Hz);7.49 and 7.77(each 2H,each d,J=8. 7Hz),7.54(lH,s). IR(CHC13):3689,3378,3028,3014,2924,1713,1652,1602,1522,1496 /cm. [a]D= +78.3° (MeOH,c=0.84,25t:). m.p.205.0-206.Ot: No.2a-14 [a lD=+72.5° (MeOH,(:=1.07,251).
No.2a-15 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) (請先閲讀背面之注意事項再^^4頁) -絮· 、^ 線 182 513422 A7 B7 五、發明説明(179 CDC13 300MHz 0.99(lH,d,J=9.9Hz),1.14 and 1.24(each 3H,each s), 1.55-2.44(14H,m),4.27(1 H,m),5.30-5.50(2H,m),6.29(lH,d,J=9.0Hz),7.11 and 7.20(each 1H,each d,J=l 6.2Hz),7.29-7.55(5H,m),7.57 and 7.72(each 2H,each d,J=8.7Hz). IR(CHC13):3453,3083,3022,3013,2925,2870,1708,1650,1607,1560,1522,1496 / cm.
[a]D= +72.3° (MeOH,c=1.00,27t:). m.p.ll5.0-117.0t:
No.2a-16 CDC13 300MHz 0.92(lH,d,J=10.2Hz),l.ll and 1.23(each 3H,each s),1.50-2.48(14H,m),3.62(3 H,s),4·29(1Η,m),5·30·5,50(2Η,m),6.20(lH,d,J=8.7Hz),6.59 and 6.68(each 1H, each,d,J=12.3Hz),7.23(5H,s),7.29 and 7.59(each 2H,each d,J=8.1Hz). IR(CHC13):3453,3024,3016,2924,2870,1730,1651,1607,1520,1495 /cm.
[a]D= +56.8° (MeOH,c=1.04,24t:)·
No.2a-17 CDC13 300MHz 0.97(lH,d,J=10.2Hz),1.11 and 1.23(each 3H,each s),1.50-2.38(14H,m),4.26(1 H,m),5.30-5.50(2H,m)f6.23(lH,d,J=8.4Hz),6.59 and 6.70(each lH,each d,J=l 2.3Hz),7.23(5H,s),7.30 and 7.57(each 2H,each d,J=8.7Hz). 經濟部中央標準局員工消費合作社印製 IR(CHC13):3452,3081,3019,3014,2925,2870,2665,1708,1650,1607,1521,1495 / cm.
[c〇D= +61.6。(MeOH,c=1.00,27t:)·
No.2a-15 CDC13 300MHz 0.97(lHfd,J = 10.2Hz), 1.11 and 1.23(each 3H,each,s), 1.50-2.50(14H,m),3.61(3 本纸張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 183 513422 A7 B7 五、發明説明(180 經濟部中央標準局員工消費合作社印製 H,s),4.31(lH,m),5.35-5.51(2H,m),6.33(lH,d,J=8.4Hz),7.48-7.64(4H,m),7.79-7. 83(2H,m),7.91(lH,dt,J=1.5 and 7.8Hz),8.01(lH,dt,J=1.5 and 7.8Ηζ),8·13(1Η, t,J=1.5Hz). IR(CHC13):3450,3026,3013,2925,2870,1730,1659,1600,1510 /cm. [a]D= +56.0° (MeOH,c=1.01,25t:). No.2a-19 CDC13 300MHz 〇.95(lH,d,J=9.9Hz),1.14 and 1.21(each 3H,each s),1.53-2.60(14H,m),4.25(1 Hfm),5.35-5.64(2H,m),7.21(lH,d,J=7.8Hz)l7.49-7.68(4H,m),7.76-7.84(3H,m),8. 25(lH,m),8.43(lH,m). IR(CHC13):3382,3196,3025,3015,2925,2870,1725,1652,1599,1577,1521 /cm· [a]D= +55.9。(MeOH,c=1.00,25t:)·, No.2a-20 CDC13 300MHz 0.98(lH,d,J=10.2Hz),1.13 and 1.24(each 3H,each s), 1.50-2.50(14H,m),3.62(3 H,s),4.31(lH,m),5.35-5.51(2H,m),6.24(lH,d,J=8.4Hz),7.40-7.52(3H,m),7.71-7. 76(2H,m). IR(CHC13):3453,3025,3013f2925,2870,1730,1753,1579,1514,1486 /cm. No.2a-21 CDC13 300MHz 0.98(lH,d,J=l〇.2Hz), 1.13 and 1.23(each 3H,each s),1.52-2.50(14H,m),4.28(1 H,m),5.34-5.51(2H,m),6.27(lH,d,J=8.7Hz),7.41-7.53(3H,m),7.71-7.74(2H,m). IR(CHC13):3452,3063,3027,3014,2925,2871,1708,1652,1578,1515,1486 /cm. [a】D= +62.0。(MeOH,c=1.01,27t:)· 本紙展尺度適用中國國家標準(CNS ) Μ規格(210X 297公釐) (請先閱讀背面之注意事項再本頁) -裝· 線 184 513422 A7 B7 五、發明説明(181 經濟部中央標準局員工消費合作社印製
No.2a-22 d6-DMS0 300MHz 〇.86(lH,d,J=9.9Hz),l.lO and 1.16<each 3H,each s),1.42-1.52(3H,m),1.85-2.4 6(llH,m),3.9S(lH,m),5.32-5.43(2H,m),7.41(3H,m),7.88(2H,d,J=6.6Hz),8.19(l H,d,J=€.6Hz). IR(KBr):3367,3060,2984,2922,2868,1634,1563,1529,1487/cm. [a]D=+47.7° (MeOH,c=l.QO,25t:). No.2a-23 [a】D=+62.7e (MeOH,c=1.01,27t:)· No.2a-24 CDC13 300MHz 0.99(lH,d,J=10.2Hz),1.14 and 1.25(each 3H,each s), 1.52-2.50(14H,m),4.31(1 H,m),5.36-5.52(2H,m),6.34(lH,d,J=8.4Hz)>7.47-7.52(2H,m)>7.59.7.64(lH>m),7. 78-7.83(6H,m). IR(CHC13):3449,3027,3013,2925,2869,1708,1656,1599,1518,1493 /cm. [a]D= +63.1° (MeOH,c=1.00,25t:). No.2a-25 [a]D=+35.1e (MeOH,c=1.00,25t:). No.2a-26 [a]D=+35.5° (MeOH,c=1.02,25t:). No.2a-27 CDC13 300MHz 0.97(lH,d,J=10.2Hz),1.12 and 1.23(each 3H,each s), 1.52-2.50( 14H,m),3.63(3 H,s),4.29(lH,m)f5.36-5.51(2H,m),6.18(lH,d,J=8.4Hz),7.01 and 7.7i(each 2H, (請先閱讀背面之注意事項再本頁) 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 185 J^422 經濟部中央標準局員工消費合作社印製 A7 B7 i、發明説明(182) each d,J=8.7Hz,)f6.98-7.05<2H,m)>7.16(lH,t,J=7.5Hz),7.34-7.41(2H,in). IR(CHC13):3455,3024,3016,2924,2870,1730,1651,1588,1520,1487 /cm. [a】D=+56.4* (MeOH,c=1.01,25t:)·
No.2a-28 CDC13 300MHz 0.98(lH,d,J=10.2Hz),1.12 and 1.23(each 3H,each s), 1.52-2.50(14H,m),4.26(l H,m),5.34-5.51(2H,m),6.20(lH,d,J=9.0Hz),7.01 and 7.70(each 2H,each d,J=9. 0Hz,),6.98-7.15(2H,m),7.17(lHft,J=7.5Hz),7.34-7.40(2H,m). IR(CHC13):3454,3031,3018,2925,2870,1708,1650,1588,1523,1487/cm. {a]D= +56.2。(MeOH,c=1.00,25t:).
No.2a.29 [a]D=+53.0° (Me〇H,c=1.03,25t:).
No.2a-30 CDC13 300MHz 0.97(lH,d,J=10.2Hz),1.10 and 1.23(each 3H,each s),l.52.2.50(14H,m),4.25(1 H,m),5.30.5.50(2H,m),6.23(lH,d,J=8.7Hz),6.36(lH,s),7.26-7.39(10H,m),7.60 a nd 7.68(each 2H,each d,J=8.4Hz,). IR(CHC13):3451,3088,3064,3029,3014,2925,2869,1707,1652,1522,1495 /cm. [a]D=+54.2° (MeOH,c=1.00,25t:).
No.2a-31 CDC13 300MHz 0.98(lH,d,J=10.2Hz),1.14 and 1.24(each 3H,each s), 1.50-2.50( 14H,m),3.63(3 H,s),4.31(lH,m),5.30.5.50(2H,m)I6.26(lH,d,J=8.4Hz),6.90(lH,t,J = 7.4Hz),7.13( lH,d,J=8.7Hz),7.29(2H,t,J=8.0Hz)t7.67-7.75(5H,m),7.32(lH,s). IR(Nujol):3380,3244,1723,1638,1601,1578,1535,1495 /cm. 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) (請先閱讀背面之注意事項再B本頁) 、v5 186 513422 A7 B7 五、發明説明(183) 經濟部中央標準局員工消費合作社印製 [a]D=+73.6〇 (MeOH,c=0.50,26t:). 111^.133.0-134.0^ No.2a-32 [立】D=+56.1° (MeOH,c=1.02,26t). No.2a-33 CDC13 300MHz 0.95(lH,d,J=10.2Hz),l.l〇 and 1.21(each,3H,each s), 1.50-2.50(14H,m),4.25(1 H,m),5.13(2H,s),5.30-5.70(3H,m),6.41(lH,d,J=8.2Hz),6.89(lHfs),7.09(lH,s)f7. 17 and 7.72(each 2H,each d,J=8.2Hz),7.62(lH,s). IR(CHC13):3450,3125,3031,3013,2925,2870,2467,1917,1708,1654,1615,1575,1 523,1497 /cm. [a]D=+55.2〇 (MeOH,c=1.01,26t:). No.2a-34 [a]D=+72.9〇 (MeOH,c=1.03,25t:). No.2a-35 CDC13 300MHz 0.98(lH,d,J=10.2Hz),1.13 and 1.24(each 3H,each s), 1.52-2.48(14H,m)f4.28(1 Hfm),5.35-5.51(2H,m),6.28(lH,d,J=8.7Hz),7.34.7.37(3H,m),7.52-7.55(2H,m),7. 58 and 7.71(each 2H,each d,J=8.7Hz). IR(CHCi3):3515,3452,3030,3012,2925,2870,1739,1708,1652,1607,1555,1521,1 497 /cm. [Q:jD=+74.3〇 (MeOH,c=1.01,25t:). No.2a-36 [a !D=+23.4e (Me〇H,c=1.07,25t:). (請先閱讀背面之注意事項再本頁) -裝· 訂 線 本紙張又度適用中國國家標準(CNS ) A4規格(210X297公釐) 187 I5 423 A7B7 五、發明説明(184) 經濟部中央標準局員工消費合作社印製
No.2a-37 CDC13 300MHz 0.83(lH,d,J=10.5Hz),0.95 and 1.18(each 3H,each s),1.44-2.46(14H,m),3.92(1 H,m),5.34-5.52(3H,m),7.26-7.54(9Hfm),7.62(lH,s). IR(CHC13):3432,3310,3189,3023,3014,2924,2870,1704,1610,1594,1523,1487 / cm. [a]D=+25.3° (ΜβΟΗ/=1·00,26^:). No.2a-38 [a]D=+70.9e (MeOH,c=1.02,25t:)· No.2a-39 [a】D=+70.6° (ΜβΟΗ,=1·01,25Χ:)· No.2a-40 [a]D=+74.7° (MeOH,c=1.00,25t:)· No.2a-41 [〇;】D=+72.r (MeOH,c=1.01,24C). No.2a-42 [a】D=+69.2〇 (MeOH,c=1.00,25t:)· No.2a-43 [a】D=+70.8° (MeOH,c=1.00,25t:)· No.2a-44 [a]D=+60.4° (MeOH,c=U)0,26t:). (請先閲讀背面之注意事項再本頁) -裝· 、訂 線 本紙張尺度適用中國國家標準(CNS ) Α4規格(210Χ 297公釐) 188 513422 A7 B7 五、發明説明(185) 經濟部中央標準局員工消費合作社印製
No.2a-45 CDC13 300MHz 〇.97(lH,d,J=9.9Hz),1.13 and 1.23{each 3H,each s),1.55-2.52(14H,m),4.29(1 H,m),5.34-5.54(2H,m),6.33(lH,d,J=9.0Hz),7.10(lH,t,J=7.4Hz),7.34(2H,t,J=7.4 Hz),7.52(2H,m),7.68 and 7.75(each 2H,each d,J=S.4Hz),7.S0(lH,s),8.10(lH,s ),10.09(lH,s)· IR(CHC13):3393,3195,3093,3033,3013,2925,2870,1698,1656,159S, 1537,1498 / cm. [a]D=+59.4e (MeOH,c=1.01,24t:). No.2a-46 : [a]D=+63.5° (MeOH,c=1.00,25t:). No.2a-47 CDC13 300MHz 0.97(lH,d,J=9.9Hz),1.12 and 1.23(each 3H,each s), 1.54-2.4S(14H,m),4.29(l H,m),5.35-5.52(2H,m),6.32(lH,d,J=3.7Hz),7.26(lH,m),7.41(2H,t,J=7.8Hz),7.6 4(2H,d,J=7.5Hz),7.73 and 7.77(each 2H,each d,J=S.4Hz),7.95(lH,s),9.20(lH, s),10.38(lH,s)· IR(CHC13):3450,3339,3003,2992>2925,2870f 1706,1653,1596,1523,1495/cm. [〇r】D=+63.3〇 (MeOH,c=l.00,25T:). No.2a-48 [a]D=+63.8〇 (ΜβΟΗ,ο=1.00,24Χ:). No.2a.‘19 CDC13 300MHz 1.00( 1 H,d,J= 10.5Hz), 1.17 and 1.26(each 3H,each s), 1.55-2.52( l4H,m),4.34( 1 (請先閱讀背面之注意事項再本頁) •裝. 訂 線 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 189 513422 A7 B7 五、發明説明(186 ) H,m),5.36-5.54(2H,m),6.35(lH,d,J=9.0Hz),7.50-7.62(3H,m),7.90 and 8.33(eac h 2H,each d,J=8.4Hz),8.21(2Hfm). IR<CHC13):3451,3029,3022,3016,2925,2870,1708,1655,1542,1508,1498,1471,1 459 /cm.
[a】D=+63.5〇 (MeOH,c二 1.02,25t:). m.p.135.0-137.Ot:
No.2a-50 [a]D=+68.9e (MeOH,c=1.01,24t:).
No.2a-51 d6-DMSO 300MHz : 0.87(lH,d,J=9.9Hz),1.10 and 1.17(each 3H,each s), 1.40-1.60(3H,m), 1.90-2.4 0(11H,m),3.98(lH,m),5.35-5.46(2H,m),7.64(lH,s),7.65 and 7.91(each 2H,eac h d,J=8.7Hz),8.06(lH,d,J=6.0Hz),9.32<lH,bs). IR(KBr):3385,2962,1734,1707,1632,1529,1498 /cm.
[o:]D=+68.4e (MeOH,c=l,01,24t:).
No.2a-52 [a]D=+76.2〇 (MeOH,c=1.01,24t:).
No.2a-53 經濟部中央標準局員工消費合作社印製 (請先閱讀背面之注意事項再本頁) [ajD=+73.9° (MeOH,c=1.02,24t:).
No.2a-54 .
[a]D=+G8.1° (MeOH,c=1.00,24t:).
No/2a-55 [ajD = + G7.8° (MeOH,c=1.00,m). 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 190 513422 A7 B7 五、發明説明(187 ) 經濟部中央標準局員工消費合作社印製
No.2a-56 [a]D=+65.4° (MeOH,c=1.03,25^C). No.2a-57 [a]D=+63.4〇 (MeOH,c=1.01,24t:). No.2a-58 [a]D=+66.6° (MeOH,c=1.01,24t:). No.2a*59[a ]D=+65.5〇 (MeOHpl.OOjW). No.2a-60 [a]D=+60.9° (MeOH,c=1.02,25t:)· No.2a-61 CDC13 300MHz 0.97(lH,d,J=10.0Hz),1.10 and 1.22(each 3H,each s), 1.50-2.50(14H,m),4.26(1 H?m),5.30-5.54(2H>m),6.28(lH,d,J=S.6Hz),6.60 and 6.82(each lH,each d,J=l 2.4Hz,),7.12(2H,d,J=6.0Hz),7.25 and 7.62(each 2H,each dfJ=8.6Hz),8.47(2H, d,J=6.0Hz).IR(CHC13):3452,3027,3019,3013,2925,2870,2480,1708,1651,1606,1520,1494 / cm. [a]D=+61.6° (MeOH,c=1.01,25t:). No.2a-62 [a ]D=十72.0〇 (MeOH.c^O.iKUSC). ^---.-----裝--(請先閱讀背面之注-ή思事項再本百〇 訂 線 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 191 513422 A7 B7 五、發明説明(188 ) 經濟部中央標準局員工消費合作社印製
No.2a-63 CDC13 300MHz 0.99(lH,d,J=10.2Hz),1.14 and 1.24(each 3H,each s), 1.50-2.50(14H,m),4.29(1 H,m),5.36-5.55(2H,m),6.35(lH>d,J=9.1Hz),7.04 and 7.27(each lH,each d,J=l 6.5Hz),7.37(2H,d,J=6.6Hz),7.56 and 7.76(each 2H,each d,J=8.4Hz),8.57(2H, d,J=6.6Hz). IR(CHC13):3452,3024,3018,3014,2925,2870,2470,1933,1708,1652,1605,1521,1 496 /cm. [a]D=+69.2〇 (MeOH,c=1.01,25t:). No.2a-64 [a]D=+56.9° (MeOH,c=1.24,25t:). No.2a-65 CDC13 300MHz 0.9S(lH,d,J=10.5Hz), 1.12 and 1.23(each 3H,each s), 1.54-2.46(14H,m),4.27(1 H,m),5.23(2H,s),5.34-5.52(2H,m),6.26(lH,d,J=8.4Hz),7.32.7.45(5H>m),7.64 an d 7.71(each 2H,each d,J=8.4Hz),8.15(lH,s). IR(CHC13):3452,3088,3065,3032,3013,2925,2870,1708,1653,1611,1559,1522,1 496 /cm. [ci]D=+61·。。(MeOH,c=0.91,25t:). No.2a-66 [a]D=+76.0〇 (iMeOH,c=1.01,25t:). No.2a-67 CDC13 300MHz 0.98(lH,d,J=10.4Hz), 1.14 and 1.24(each 3H,each s)f 1.54-2.4.28( 1 H,m),5.32-5.53(2H,m),6.27(lH,d,J=8.6Hz),6(92-7.31(each lH.each d,J=16.4H (請先閱讀背面之注意事項再本頁) 本紙張尺度適用中國國家標準(CNS ) A4現格(210X 297公釐) 192 513422 A7 B7 五、發明説明( z),7.02(lH,dd,J=5.S and 3.6Hz),7.12(lH,d,J=3.6Hz),7.24<lH,d,J=5.8Hz),7.51 and 7.70(each 2H,each d,J=8.4Hz). IR(CHC13):3453,3029,3013,2925,2870,1739,1650,1604,1524,1515,1494 /cm. [a]D=+76.2〇 (MeOH,c=1.00,24t:). m.p. 104.0-106.0^3
No.2a-68 [a]D=+57.7〇 (MeOH,c=1.01,25t:).
No.2a-69 CDC13 300MHz 0.99(lH,d,J=10.2Hz),1.14 and 1.24<each 3H,each s), 1.54-2.4S(14H>m),4.28(1 H,m),5.34-5.53(2H,m),6.29(lH,d,J=9.t)Hz),6,54-6.74(each lH,each d,J=12.0H z),7.02(lH,dd,J=4.8 and 3.3Hz),6.97(lH,dd,J=3.3 and 1.2Hz),7.13(lH,dd,J= 4.8 and 1.2Hz),7.44 and 7.70(each 2H,each d,J=8.7Hz). IR(CHC13):3453,3025,3010,2925,2870,1708,1650,1607,1559,1523,1493 /cm. [a]D=+58.4。(MeOH,c=1.00,25t:).
No.2a-70 [cr]D=+48.6° (MeOH,c=1.00,25t:). 經濟部中央標準局員工消費合作社印製
No.2a-71 CDC13 300MHz
0.98(lH,d,J=10.2Hz),1.12 and 1.23(each 3H,each s), 1.52-2.46(14H,m),2.31(3 H,s),4.26(lH,m),5.33-5.52(2H,m),6.20(lHId,J=9.3Hz),7.02-7.11(6H,m),7.70(2H d,J=9.0Hz). IR(CHC13):3460,3031,3022,30 11,2925,2870,1750,1708,1650,1608,1597,1523,1 490 /cm.
[a (MeOH,c=l.01,25^:). 193 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 513422 A7 B7 五、發明説明(190 經濟部中央標準局員工消費合作社印製
No.2a-72 [a]D=+51.2° (MeOH,c=1.02,25t:). No.2a-73 CDC13 300MHz 〇.97(lH,d,J=9.9Hz),l.ll and 1.23(each 3H,each s), 1.54-2.48(14H,m),4.27(1 H,m),5.32.5.52(2H,m),6.24(lH,d,J=9.0Hz),6.83-6.94(6H,m),7.65(2H,d,J=9.0Hz ). IR(CHC13):3598,3451,3199,3033,3012,2925,2870,1708,1642,1604,1524,1507,1 491 /cm. [a]D=+52.2° (MeOH,c=1.01,25t:). No.2a-74 [a]D=+51.5e (MeOH,c=0.92,25t:). No.2a-75 CDC13 300MHz 0.97(lH,d,J=10.2Hz),l.ll and 1.23<each 3H,each s), 1.55-2.46(14H,m),3.82(3 H,s),4.25(lHIm),5.32.5.52(2H,m),6.19(lHidfJ=8.7Hz),6.89-7.01(6H,m),7.65-7. 68(2H,m). IR(CHC13):3450,3025,3008,2925,2870,2837,1741,1649,1612,152 1,1505,1490 1 cm. [a]D=+51.1° (MeOH,c=1.00,25t:). No.2a-76 [a]D=+G0.4〇 (MeOH,c二0.98,251). J
No.2a-77 本紙張尺度適用中國國家標率(CNS )八4規格(210X 297公釐) (請先閱讀背面之注意事項再本頁) -裝· 訂 線 194 513422 A7 B7 五、發明説明(191 經濟部中央標準局員工消費合作社印製 CDC13 300MHz 〇.99(lH,d,J=10.5Hz),1.15 and 1.24(each 3H,each s), 1.54-2.48(14H,m),2.34(3 H,s),4.29(lH,m),5.32-5.54(2H,m),6.32(lH,d,J=8.4Hz),7.19 and 7.60<each 2H, each d,J=8.4Hz),7.63 and 7.79(each 2H,each d,J=S.4Hz). IR(CHC13):3452,3027,3012,2925,2870,1751,1709,1651,1611,1560,1527,1509,1 489 /cm. [a]D=+61.2° (MeOH,c=1.00,25t:). No.2a-78 [a]D=+67.4° (MeOH,c=1.01,25t:)· No.2a-79 CDC13 300MHz ’ 0.99(lH,d,J=10.2Hz),1.15 and 1.24(each 3H,each s), 1.54-2.54(14H,m),4.31(1 H,m),5.32-5.54(2H,m),6.36(lH,d,J=8.2Hz),6.93 and 7.48(each,2H.each d,J=8. 6Hz),7.59 and 7.75(each 2H,each d,J=8.4Hz). IR(CHC13):3593,3448,3192,3030,3010,2925,2870,1708,1644,1608,1591,1559,1 530,1516,1491 /cm. [a]D=+65.8° (MeOH,c二 1.01,25t:)· No.2a*80 [a]D=+66.9° (MeOH,c=1.01,25t:).
No.2a-81 CDC13 300MHz 0.99(lH,dtJ=10.5Hz),1.15 and 1.24(each 3H,each s), 1.54-2.48( 14H,m),3.80(3 H,s),4.29(lH,m),5.34-5.52(2H,m)f6.20(lH,d,J=8.7Hz),6.99 and 7.55(each 2H, each d,J=9.0Hz),7.61 and 7.77(each 2H,each d,J=S.7Hz). IR(CHC13):3450,3009,2925,2870,2838,1740,1708,1650,1608,1557,1528,15 12, L 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) (請先閲讀背面之注意事項再本頁) 铸 195 513422 A7 B7 五、發明説明(192 經濟部中央標準局員工消費合作社印製 491 /cm. [a】D=+66.2° (MeOH,c=1.01,25t:). No.2a-82 [a】D=+57.7〇 (MeOH,c=1.02,24^C). No.2a-83 CDC13 300MHz 〇.97(lH,d,J=10.2Hz),1.12 and 1.23(each 3H,each s),1.54-2.48(14H,m),2.33(3 H,s),4.26(lH,m),5.32.5.52(2H,m),6.25(lH,d,J=8.7Hz),7.16 and 7.75(each 2H, each d,J=8.7Hz). IR(CHC13):3452,3030,3022,3012,2925,2870,1754,1709,1654,1604,1585,1522,1 493 /cm. [a]D=+57.4° (MeOH,c=1.01,24t:). No.2a-84 [a]D=+57.8° (MeOH,c=1.01,24t:). No.2a-85 CDC13 300MHz 〇.95(lH,dfJ=10.2Hz),1.12 and 1.22(each 3H,each s), 1.54-2.48(14H,m),4.25(1 H,m),5.32-5.52(2H,m),6.28(lH,d,J=S.7Hz),6.87 and 7.57(each 2H,each d,J二9. 0Hz). IR(CHC13):3590,3450,3166,3019,3012,2925,287 1,1708,1637,1608,1583,1531,1 498 /cm. [c〇D=+56.0° (MeOH,c=1.01,24t:)· No.2a-86 [a!D=+59.3〇 (MeOH,c=l.01,22t:). (請先閲讀背面之注意事項再頁)
、T 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 196 513422 A7 B7 五、發明説明(193
No.2a-87 CDC13 300MHz 0.9S(lH,d,J=10.0Hz),1.13 and 1.23(each 3H,each s),1.54-2.48(14H,m),3.85(3 H,s),4.25(lH,m),5.32-5.53(2H,m),6.19(lH,d,J=8.8Hz),6.93 and 7.69(each 2H, each d,J=9.0Hz). IR(CHC13):3450,3030,3017,3012,2925,2870,2840,1740,1708,1647,1606,1575,1 525,1496 /cm.
[a]D=+58.2〇 (MeOH,c=0.99,22t:).
No.2a-88 [a]D=+50.9° (i\IeOH,c=1.02,25eC).
No.2a-S9 CDC13 300MHz 0.99(lH,d,J=10.2Hz),1.18 and 1.26(each 3H,each s), 1.56*2.48(14H,m),4.29(1 H,m),5.36-5.54(2H,m),7.03(lH,d,J=8.7Hz),7.21(lH,s),7.43(2H,m),7.74(lH,ddd, J=1.8,6.9 and 8.7Hz),8.22(lH,dd,J=1.8 and 8.1Hz). IR(CHC13):3443,3087,3023,3014,2925,2870,1708,1685,1658,1630,1517,1466 / cm.
[a]D=+57.1〇 (MeOH,c=lX)l,22t:). m.p.117.0-118.Ot: 經濟部中央標準局員工消費合作社印製
No.2a-90 [a]D=+54.1〇 (MeOH,c=1.01,22t:).
No.2a-91 CDC13 300MHz 0.97(lH,d,J=10.2Hz),L13 and 1.23(each 3H,each s), 1.52-2.46( 14H,m),4.24( 1 本纸張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 197 513422 A7 B7 五、發明説明(194 H,m),5.34-5.52(2H,m),6.49-6.53(2H,m),7.11(lH,dd,J=0.9 and 3.6Ηζ),7·44(ΐΗ, dd,J=0.9 and 1·8Ηζ). IR<CHC13):3437,3033,3022,3014/2925,2870,1739,1/708,1655,1595,1520,1472 / cm. 經濟部中央標準局員工消費合作社印製 [a]D=+55.0° (MeOH,c=1.00,22t:). No.2a-92 [a]D=+50.3° (MeOH,c=1.0O,22t:). No.2a-93 CDC13 300MHz 0.95(lH,d,J=10.5Hz),1.12 and 1.23{each; 3H,each s), 1.52-2.46(14H,m),4.25(1 H,m),5.34-5.52(2H,m),6.12(lH,d>J=8.7Hz),7.07(lHldd,J=3.9 and 5.lHz),7.45-7.48(2H,m). IH(CHC13):3450,3023,3011,2925,2870,1739,1708,1645,1531,1501,1471 /cm. [a]D=+49.1° (MeOH,c=1.02,24t:)· No.2a-94 [a】D=+51.5〇 (MeOH,c=1.00,24t:). No.2a-95 CDC13 300MHz 0.96(lH,d,J=10.5Hz),l.ll and 1.23(each 3H,each s), 1.δ2-2.46(14Η,ιη),4.2δ(1H,m),5.34.5.56(2H,m),6.14(lH,d,J=8.7Hz),7.34(2H,d,J=2.0Hz),7.85(lH,tfJ=2.0 Hz). IR(CHC13):3452,3 114,3030,3013 2925,2870,1708,1649,1535,1498,147 1 /cm. [a ]D=+55.5〇 (MeOH,c= 1.00,251). m.p.87.0-88.0t: (請先閲讀背面之注意事項再本頁) -裝· 訂 線 本纸張尺度適用中國國家標準(CNS ) Α4規格(210Χ297公釐) 198 513422 A7 B7 五、發明説明(195
No.2a-96 CD30D 300MHz 〇.94(lH,d,J=10.2Hz),1.13 and 1.22<each 3Hfeach s), 1.50-1.76(3H,m), 1.94-2. 39(llH,m),4.11(lH,m),5.39.5.49(2H,m),7.43-7.51(2H,m),8.05(lH,m). IR(KBr):3369,30S4,2985,2921,2868,1630,1566,1538,1503 /cm. [a]D=+38.8〇 (MeOH,c=1.01,22t:). No.2a-97 CD30D 300MHz0.93(lH,d,J=9.9Hz),1.13 and 1.22(each 3H,each s),1.48-1.5S(3H,m),1.96-2.3 6(llH,m),4.10(lH,m),5.35.5.50{2H>m),7.42.7.51(2H,m),8.06(lH>m). IR(KBr):3447,3087,2987,2922,2868,1629,1545,1501 /cm. [or]D=+52.9e (MeOH,c=1.01,24t:).
No.2a-9S [a]D=+53.2° (MeOH,c=1.02,23t:)· 請 閱 讀 背 5 意 事 項 再 頁 玎 經濟部中央標準局員工消費合作社印製
No.2a-99 CDC13 300MHz〇.97(lH,cl,J=10.2Hz),1.12 and 1.22(each 3H,each s),1.26-2.45(24H,m),4.25(2 H,m),5.34-5.52(2H,m),6.18(lH,d,J=8.7Hz),6.91 and 7.66(each 2H,each d,J=9· 0Hz). IR(CHC13):3455,3029,3019,2939,2862,1738,1709,1645,1605,1523,1494 /cm. [a]D=+51.4° (MeOH,c=l.00,23t:). No.2a-100 [a]D=+49.3〇 (MeOH,c=1.00f24<t:).
No.2a-101 本紙張尺度適用中國國家標準(CNS ) A4規格(2!〇χ 297公釐) 199 513422 A7 B7 五、發明説明(1% ) 經濟部中央標準局員工消費合作社印製 [a】D=+51.3e (MeOH,c=1.00,24t:)· No.2a-102 [a]D=+48.8e (MeOH,c=1.01,23t:). No.2a-103 CDC13 300MHz 0.94(lH,d,J=10.2Hz),1.12 and 1.22(each 3H,each s),1.52-2.46(14H,m),2.48(3 H,d,J=0.3Hz),4.20(lH,m)f5.32-5.54(2H,m),6.46(lH,bs),7.12(lH,d,J=9.0Hz). IR(CHC13):3415,3144,3029,3011,2926,2871,1708,1671,1598,1538,14564 /cm. [a】D=+49.6° No.2a-104 [a]D=+77.0e (MeOH,c=1.02,23t:)· No.2a-105 CDC13 300MHz 0.93(lH,d,J=9.9Hz),1.09 and 1.21(each 3H,each s), 1.51-2.44(14H,m),3.90(6 H,s),4.20(lH,m),5.38.5.50(2H,m),5,87(lH,d,J=9.0Hz),6.25 and 7.54(each 1H, each d,J=15.6Hz),6.84(lH,d,J=8.lH2),7.03(lH,d,J=1.8Hz),7.09(lH,dd,J=1.8 a nd 8.1Hz). IR(CHC13):3439,3028,3012,2937,2871,2841,1739,1708,1661,1620,1600,1513 / cm. [a]D=+77.3e (MeOH,c=1.01,23t:)· No.2a-106 [a 】D=+67.0。(MeOH,c=1.00,25r). No.2a-107 (請先閱讀背面之注意事項再 -裝· 頁) 訂 線 本紙浪尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 200 513422 A7 B7 五、發明説明(197) 經濟部中央標準局員工消費合作社印製
[a]D=+66.6° (MeOH,c=1.01,24t:). m.p.l68.〇.170.0t: No.2a-108 [a]D=+61.8e (M^OH,c=LOO,22t:). No.2a-109 CDC13 300MHz 0.96(lH,d,J=10.2Hz),1.10 and 1.22(each 3H,each s), 1.5l-2.45(14H,m),4.25(l H,m),5.33-5.49(2H,m),6.2l(lH,d,J=8.7Hz),7.25 and 7.60(each 2H,each d,J=8. 7Hz),7.33-7.41(5H,s). IR(CHC13):3453,3062,3028,3014,2925,2870,1739,1708,1651,1594,1557,1515,1 481 /cm. [a]D=+61.0° (MeOH,c=1.01,22t:). No.2a.110 CD30D 300MHz 0.94(1H,d,J=9.9Hz), 1.13 and 1.22(each 3H,each s),1.54-2.37(14H,m),4.12(1 H,m),5.38-5.49(2H,m),7.25 and 7.68(each 2H,each d,J=8.7Hz),7.4l(5H,s). IR(KBr):3435f3058,2986,2920,2866,1635,1595,1562,1521,1482,1439,1411 /cm [〇f]D=+47.3° (MeOHfc=1.01,23t:). No.2a-lll (a]D=+65.6° (MeOH>c=1.01,24<C). No.2a-112 CDC13 300MHz 0.97(lH,d,J=10.2Hz), 1.12 and 1.23(each 3H,each s), L5 l-2.46(14H,m),4.27(I (請先閱讀背面之注意事項再頁) 、v'iv 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 201 513422 A7 B7 五、發明説明(198 經濟部中央標準局員工消費合作社印製 H,m),5.35.5.50(2H,m),6.22(lH,d,J=8.4Hz),7.40 and 7.66<each 2H,each d,J=9. OHz). IR(CHC13):3439,3028,3012,2937,2871,2841,1739,1708,1661,1620,1600,1513 / cm. [a]D=+65.6〇 (MeOH,c=1.01,22t:). No.2a-113 {a]D=+59.6° (ΜθΟΗ,ο=1.00,24^:). · No.2a-114 CDC13 300MHz 0.98(lH,d,J=10.2Hz), 1.12 and 1.24(each 3H,each s),1.52-2.46(14H,m),4.29(1 H,m),5.35-5.51(2H,m),6.28(lH,d,J=8.4Hz),7.70 and 7.83(each 2H,each d,J=S. 4Hz). IR(CHC13):3439,3028,3012,2937,2871,2841,1739,1708,1661,1620,1600,1513 / cm. [a]D=+60.6。(MeOH,c=1.01,22t:). No.2a-115 [a]D=+59.7° (MeOH,c=0.99,24t:). No.2a-116 CDC13 300MHz 0.97(lH,d,J=10.2Hz),1.12 and 1.23(each 3H,each s), 1.52-2.46( 14H,m),2.39(3 H,s)r4.27(lH,m),5.33-5.51(2H,m),6.24(lH,d,J=9.0Hz),7.23 and 7.62(each 2H, each d,J=8.4Hz). IR(CHC13):3439,3028,3012,2937,287 1,284 1,1739,1708,166 1,1620,1600,15 13/c m. (a]D=+59.7〇 (MeOH,c=0.99,24t:). (請先閱讀背面之注意事項再頁) -裝·
、1T 線 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 202 513422 A7 B7 五 、發明説明(199
No.2a-117 [a]D=+56.7e (MeOH,c=1.00,23t:)· No.2a-118 CDC13 300MHz 0.96(lH,d,J=10.2Hz),l.ll and 1.23(each 3H,each s),1.53-2.44(14H,m),4.23(1 H,m),5.34-5.51(2H,m),6.02(2H,s),6.13(lH,d,J=8.7H2),6.83(lH,dd,J=1.2 and 7. 8Hz),7.22-7.25(2H,m). IR(CHC13):3453,3031,3020,3012,2924,2870,1740,1708,1650,1619,1605,1519,1 504,1480 /cm. [a ]D=+57.2e (1^011^=1.02,231). No.2a-119 CDC13 300MHz 0.96(lH,d,J=10.5Hz),1.07 and 1.23(each 3H,each s),1.51-2.44(14H,m),2.32(3 H,s),4.26(lH,m),5.37-5.52(2H,m),6.40(lH,d,J=9.0Hz),7.09(lH,m),7.30(lH,m), 7.46(lH,m),7.66(lH,m). IR(CHC13):3443,3028,3012,2925,2870,1766,1747,1709,1657,1607,1516,1479 / cm. [a ]D=+53.2。 (請先閲讀背面之注意事項再—本頁) -裝· 訂 線 經濟部中央標準局員工消費合作社印製
No.2a-I20 CDC13 300MHz 0.98(lH,d,J=10.2Hz),1.14 and 1.24(each 3H,each s),1.53-2.44(14H,m),4.30(1 H,m)l5.35-5.52(2H>m),6.42(lH,d,J=8.7Hz),6.85(lH,m),6.99(lH,dd,J=1.2 and 8.4Hz),7.27(lH,m),7.39(lH,m). IR(CHC13):3463,3033,3021,3014,2992,2924,2870,1708,1643,1597,1523,1488 / cm. 本纸張又度適用中國國家標準(CNS ) A4規格(210X 297公釐) 203 513422 A7 B7 五、發明説明( 200 [a]D=+46.3〇 (MeOH,c=1.01,21t:). No.2a-121 CDC13 300MHz Ό·98(1Η,d,J=10.2Hz),1.14 and 1.23(each 3H,each s),1.47-2.47(14H,m),3.95(3 H,s),4.31(lH,m),5.32.5.50(2H,in),6.98(lH,dd,J=0.9 and 8.4Hz),7.09(lH,ddd,J =0.9,7.7 and 8.4Hz),7.45(lH,m),8.19(lH,dd,J=2.1 and 8.lHz),8.32(lH,d,J=9. OHz). IR(CHC13):3400,3078,3028,3020,3007,2924,2870,2842,1736,170s, 1640,1600,1 536,1483,1470 /cm. [a]D=+38.1〇 (MeOH,c=1.02,23t:). No.2a-122 [a]D=+42.3〇 (MeOH,c=0.99,23t:). No.2a-123 [a]D=+38.7° (MeOH,c=1.00,2lt:). No.2a-124 [a]D=+45.03 (MeOH,c=1.01,2lt:). m.p.ll9.0-120.0t: No.2a-125 [ajD=+49.8° (MeOH,c=1.01,22t:)· —^---^-----裝-- (請先閱讀背面之注意事項再本頁) 訂 線 經濟部中央標準局員工消費合作社印製
No.2a-126 CDC13 300MHz 0.97(lH,d,J=10.2Hz), 1.11 and 1.23(each 3H,each s)f I.52-2.47(14H,m),4.2G(l H,m),5.34.5.50(2H,m),6.22{lHfd,J=8.7Hz),7.55-7.61(4H,m). 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 204 一 ο n - 513422 A7 B7 五、發明説明(201 ) IR(CHC13):3400,3078,3028,3020,3007,2924,2870,2842,1736,1708,1640,1600,1 536,1483,1470 /cm.
[a]D=+63.0〇 (MeOH,0=1.01,23^).
No.2a-127 CDC13 300MHz 0.91(lH,d,J=10.2Hz), 1.10 and 1.20(each 3H,each s), 1.50-2.42(14H,m),4.23(1 H,m),5.31<5.51(2H,m),6.45(lH,d,J=8.4Hz),7.01(lH>t,J=7.4Hz>,7.22-7.27(2H,m ),7.33-7.40(4H,m),7.53(2H,d,J=9.0Hz),8.30 and 8.48(each lH.each s). IR(CHC13):3452,3028,3022,3015,2925,2870,1708,1654,1590,1514,1478 /cm. [a]D=+59.5° (MeOH,c=l.01,23=).
No.2a-128 d6-DMSO 300MHz 0.84(lH,d,J=9.9Hz), 1.06 and 1.19{each 3H,each s), 1.37-2.37(14H,m),3.79(1 H, m),5.35-5.51(2H,m),6.08(lH,d,J=8.7Hz),6.85-6.90(lH,m),7.18-7.23(2H,m),7. 35-7.38(2H,m),8.42(lH,s),12.00(lH,s). IR(Nujol):3395,3345,2925,2866r2623,2506,1697,165S(1638,1597,1557 /cm. [o:]D二+26.0。(MeOH,c=1.01,23t:). m.p. 164.0 -166.0^2 經濟部中央標準局員工消費合作社印製
No.2a-129 CDC13 300MHz I. 01(lH,d,J = 10.0Hz), 1.17 and 1.25(each 3H,each s),l.54-2.52(14H,m),4.34(1 HIm),5.36-5.57(2H,m),6.42(lH,d,J=8.6Hz)f7.51.7.60(2H,m),7.77(lH,dd,J=1.8 and 8.6Hz),7.85-7.96(3H,m),8.24(lH,bs). IR(CHC13):345 1,3060,3028,3010,2925,2870,1708,1652,1629,1600,1517,1502 / cm.
[ajD = + 68.6° (MeOH,c=1.00,22t:). 本纸張尺度適用中國國家標準(CNS ) A4規格(210X297公董) 205 513422 A7 B7 五、發明説明(202 ) 經濟部中央標準局員工消費合作社印製
No.2a-130 CDC13 300MHz l. 02(lH,d,J=10.2Hz),1.04 and 1.26(each 3H,each s),1.54-2.52(14H,m)f4.41(l H,m),5.41-5.58(2H,m)f6.14(lH,d,J=9.〇Hz),7.43.7.59<4H,m),7.85-7.92(2H,in)>8. 27(lH,dd,J=1.8 and 7.2Hz). IR〈CHC13):3436,3032,3010,2924,2870,2664,1708,1652,1512,1498 /cm· [a]D=+93.9〇 (MeOH,c=1.00,22t:) 111^.94.0-96.0^ No.2a-131 [a]D=+50.2a (MeOH,c=0.95,2lt:). No.2a-132 [a]D=+10.9〇 (MeOHpOWJlC)· No.2a-133 [a]D=+60.4〇 (MeOH,c=LOO,2lt:). ; No.2a-134 [a】D=+33.5° (MeOH,c=1.01,23t:). No.2a-135 [¢^0=+52^(1^01^=1.01,231).m. p. 180.0 -182.0*C
No.2a-136 [a]D=+35.3〇 (MeOH,c=1.02,23t:). m.p.79.0-80.OC 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 206 -one. (請先閱讀背面之注意事項再iHF本頁) -裝. 訂 線 513422 A7 B7 五、發明説明(2〇3 ) 經濟部中央標準局員工消費合作社印製
No.2a-137 CDC13 300MHz 0.97(lH,d,J=10.2Hz),l.ll and 1.22(each 3H,each s),1.43(3H,t,J=6.9Hz),1.52 •2.44(14H,m),4.03(2H,q,J=6.9Hz),4.26(lH,m),5.33-5.50(2H,m),6.19(lH,d,J=8· 7Hz),6.88-7.00(611,111),7.65-7.68(211,111). IR<CHC13):3455,3031,3024,3014,2988,2925,2870,1741,1708,1649,1602,1521,1 504,1490 /cm. (a]D=+52.0〇 (MeOH,c=1.01,23t:). No.2a-138 CDC13 300MHz 0.97(lH,d,J=10.2Hz),l.ll and 1.22(each 3H,each s), 1.35(6H,d,J=6.〇Hz), 1-53 -2.46(14H,m),4.25(lH,m),4.51(lH,m),5.33-5.50(2H,m),6.12(lH,d,J=9.0Hz),6.8 7-6.99(6H,m)f7.65-7.68(2H,m). IR(CHC13):3454,3031,3014,2980,2925,2870,1741,170S, 1649,1602,1522,1490 / cm. [a】D=+50.0° (MeOH,c=l.05,22=). No.2a-139 CDC13 300MHz l. 00(lH,d,J=10.2Hz)>1.16 and 1.24(each 3H,each s), 1.59-2.52(14H,m),4.31(1 H,m),5.40.5.53(2H,m),6.36(lH,d,J=8.7Hz),6.70(lH,d,J=1.5Hz),7.12(lH,m),7.3 0(lH,m),7.47(lH,dd,J=0.6 and 8.lHz),7.61(lH,d,J=8.4Hz). IR(CHCi3):3449,3243,3029t3022f3013,2925,2871,1707,1631,1542,1505 /cm. [a]D=+63.4〇 (MeOH,c=1.00,23t:). m. p.178.0-179.Ot:
No.2a* 140 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 207 (請先閱讀背面之注意事項再本頁) 訂 線 513422 A7 B7 五、發明説明(204 經濟部中央標準局員工消費合作社印製 CDC13 300MHz 〇.97(lH,d,J=10.2Hz),1.18 and 1.23(each 3H,each s),l.57-2.50(14H,m),4.35(1 H,m),5.32-5.55(2H,m),6.42(lH,d,J=8.7Hz),6.70(lH,d,J=1.5Hz),7.21-7.24(2H m),7.46(lH,m),7.76(lH,m),7.86(lH,d,J=3.0Hz),10.20(lH,s). IR(CHC13):3465,3010,2924,1739,1604,1546,1504 /cm. 〇]D=+39.4e (MeOH,c=1.01,22t:)· m.p.167.0-168.OX:. No.2a-141 CDC13 300MHz 0.99(lH,d,J=10.2Hz),1.14 and 1.24(each 3H,each s),1.55-2.44(14H,m),3.84(3 H,s),4.27(lH,m),5.34-5.52(2H,m),6.28(lH,d,J=9.0Hz),6.91 and 7.47(each 2H, each d,J=9.0Hz),6.98 and 7.14(each lH,each d,J=16.5Hz)f7.54 and 7.70(ea ch 2H,eachd,J=8.7Hz). IR(CHC13):3453,3025,3015,2925,2870,2839,1740,1708,1649,1602,1510,1493,1 470 /cm. [a]D=+73.4° (MeOH,c=1.02,22t:). m.p.l55.0-157.0t: No.2a-142 CDC13 300MHz 0.97(lH,d,J=l〇.2Hz),l.ll and 1.23(each 3H,each s), 1.52-2.45(14H,m),3.79(3 H,s),4.27(lH,m),5.34-5.50(2H,m),6.24(lH,d,J=9.0Hz),6.49 and 6.62(each 1H, each d,J=12.3Hz),6.77 and 7.16(each 2H,each d,J=8.7Hz),7.32 and 7.59(ea ch 2H,eachd,J=8.lHz). IR(CHC13):3453,3025,3014,2925,2870,2839,1739,1708,1649,1606,1510, 1494 /cm. [a]D=+60.7e (ΜβΟΗ,ο=0.99,22Χ:). 本紙張尺度適用中國國家榡準(CNS ) A4規格(210X 297公釐) (請先閱讀背面之注意事項再iHF本頁) 裝_
、1T 線 208 513422 A7 B7 五、發明説明(205
No.2a-143 [a]D=+57.3° (MeOH,c=1.01,23t:)·
No.2a-144
[a]D=+12.20 (MeOH,c=1.00,23t:). m.p.114.0-116.O^C
No.2a-145 CDC13 300MHz 0.95(lH,d,J=10.2Hz),1.10 and 1.21(each 3H,each s),1.52-2.44(14H,m),4.25(l H,m),5.33-5.49(2H,m),6.37(lH,d,J=8.7Hz),7.45-7.47(3H,m),7.62-7.66(2H,m),7· 69 and 7.80(each 2H,each d,J=7.5Hz,). IR(CHC13):3449,3058,3027,3012,2925,2870,1708,1655,1513,1481,1043 /cm. [a]D=+61.0〇 (MeOH,c=1.01,23t:).
No.2a-146 CDC13 300iMHz 0.95(lH,d,J=10.5Hz),1.09 and 1.21(each 3H,each s), 1.50-2.41(14H,m),4.25(1 H,m),5.33-5.49(2H,m),6.33(lH,d,J=8.4Hz),7.49.7.61(3H,m),7.91.7.92(2HIm),7. 82 and 7.97(each 2H,each d,J=S.7Hzf). IR(CHC13):3447,3029,3023,3015,2925,2870,1708,1660,1514,1484,1321,1161 / cm. 經濟部中央標準局員工消費合作社印製 [ct】D=+62.0e (MeOH,c=1.00,22t:).
No.2a-147 CDC13 300MHz 0.97(lH,dfJ=10.2Hz)(1.12 and 1.23(each 3H,each s), 1.52-2.46( 14H,m),2.5 1(3 H,s),4.26(lH,m),5.34.5.51(2Hfm),6.23(lH,d,J=8.4Hz),7.26 and 7.G4(each 2H, each d,J=8.4Hz). 本纸張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 209 513422 A7 B7 五、發明説明(2Q6 經濟部中央標準局員工消費合作社印製 IR(CHC13):3453,3027,3015,2925,2870,2665,1708,1648,1596,1516,1484 /cm. [a]D=+67.7d (MeOH,c=0.82,22t:). No.2a-148 [a]D=+72.5〇 <Me0H,c=1.01,25t:). No.2a-149 ^ [a]D=+67.8a (MeOH,c=0.98,25t:)· No.2a-150 CDC13 300MHz 0.94(lH,d,J=10.2Hz),1.10 and 1.23(each 3H,each s), 1.52-2.50(14H,m),4.22(1 H,m),5.36-5.55(2H,m),6.48(lH,d,J=8.4Hz),8.35(lH,s),8.90(lH,s). IR(CHC13):3443,3374,3091,3024,3012,2925,2871,1709,1652,1525,1494 /cm. [a]D二+58.1° (MeOH,c=1.01,23X:)·-m.p.120.0-122.Ot: No.2a-151 [a]D=+40.6° (MeOH,c=1.01,23t:)· No.2a-152 CDC13 300i\IHz 0.96(lH,d,J=10.5Hz),1.10 and 1.24(each 3H,each s),1.50-2.50(14H,m),2.71(3 H,s),4.26(lH,m),5.37-5.51(2H,m),6.02(lH,d,J=9.0Hz),8.73(lH,s). IR(CHC13):3463,3435,3087,3025,3014,2925,2870,1708,1649,1523,1503 /cm. [ajD二+54.1° (MeOH,c=1.02,22t:). No.2a-153 CDC13 300MHz (請先閱讀背面之注意事項再本頁) _裝- 訂 線 本纸張又度適用中國國家標準(CNS ) A4規格(210X 297公釐) 210 513422 A7 B7 五、發明説明(2〇7 ) 0.95(lH,d,J=9.9Hz),1.11 and 1.23<each 3H,each s),1.50-2.50(14H,m),2.50(3 H,s),4.26(lH,m),5.36-5.51(2H,m),6.01(lH,d,J=8.4Hz),6.88(lH,d,J=5.lHz),7.26 (lH,d,J=5.1Hz). IR(CHC13):3469,3431,3025,3013,2925,2871,2664,1708,1639,1544,1505 /cm. [a]D=+35.8〇 (MeOH,c=1.03,22t:)·
No.2a-154 CDC13 300MHz 0.95(lH,d,J=9.9Hz),1.10 and 1.22(each 3H,each s),1.52.2.46(14H,m),2.51(3 H,d,J=1.2Hz),4.26(lH,m),5.34-5.50(2H,m),6.00(lH,d,J=8.4Hz),6.73(lH,dd,J=5. 1 and3.6Hz),7.29{lH,d,J=3.6Hz). IR(CHC13):3450,3431,3026,3011,2925,2869,1739,1708,1639,1547,1508 /cm. [a]D=+50.5〇 (MeOH,C=1.01,22r).
No.2a-155 CDC13 300MHz 0.99(lH,d,J=10.2Hz),1.19 and 1.25(each 3H,each s),l.53-2.48(14H,m),4.31(1 H,m),5.36.5.51(2H,m),6.79(lH,d,J=9.3Hz),7.29(lH,m),7.41(lH,m),7.48(lH,s), 7.51(lHtm),7.66(lH,d,J=8.1Hz). IR(CHC13):3436,3029,3024,3015,2925,2871,2670,1708,1659,1598,1510 /cm. [a]D=+69.1〇 (MeOH,c=1.01,22r). 經濟部中央標準局員工消費合作社印製 (請先閲讀背面之注意事項再本頁)
No.2a-156 CDC13:CD3OD=10:l 300MHz 0.99(lH,d,J=9.9Hz),l.ll and 1.21(each 3Hteach s), 1.56-2.58(14Hfm),4.22(1
• I H,m),5.35-5.59(2H,m),6.83(lH,d,J=8.4Hz)t7.48(lH,d,J=8.4Hz),7.61(lHtdd,J=l. j 5 and S.4Hz),8.09(lH,d,J=1.5Hz),8.12(lH,s). IR(KBr):3422,3 115,2985,2922,2869,2609,1708,1636,1578,1529,1470 /cm. [a]D=+62.8〇 (MeOH,c=1.01,22t:). 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 211 513422 A7 B7 五、發明説明(208
No.2a-157 [a】D=+40.0° (!^0£[,。=0.95,22^:). No.2a-158 CDC13 300MHz 1.00(lH,d,J=10.5Hz),1.17 and 1.24(each 3H,each s), 1.54-2.50(14H,m),4.34(l H,m),5.36-5.52(2H,m),7.80(lH,d,J=9.0Hz),9.30(lH,s). IR(CHC13):3410,3122,3030,3012,2925,2871,2668,1709,1667,1538,1466 /cm. [a】D=+44.9e (]\^〇艮。=0.99,22=)· No.2a-159 __ CDC13 300iMHz 0.97(lH,d,J=10.2Hz),1.13 and 1.22(each 3H,each s),1.55-2.43(14H,m),3.03(6 H,s),4.23(lH,m)>5.32.5.51(2H,m),6.16(lH,d,J=8.7Hz),6.87 and 7.63(each 2H, each d,J=8.7Hz). IR(CHC13):3457,3028,3006,2924,2870,2654,1739,1709,1637,1608,1608,1534,1 501 /cm.[a]D=+64.8° (MeOH,c=1.01,22t:). (請先閱讀背面之注意事項再本頁) 裝_ 訂 經濟部中央襟準局員工消費合作社印製
No.2a-160 d6-DMSO 300MHz 0.83(lH,d,J=9.9Hz),1.02 and 1.19(each 3H,each s), 1.38-1.6l(3H,m)t 1.90-2.3 2(llHfm)f3.90(lHfm),5.41-5.44(2H,m)f7.32(lH,dd,J=0.9 and 7.2Hz)t7.45-7.60 (2H,m),7.77(lH,dd,J=0.9 and 7.8Hz),8.03(lH,d,J=6.9Hz),12.40(lH,s). IR(Nujol):33 15,2924,2856,2656,2535, Π37,1703,1637,1598,153 1,1541 /cm. | [a]D=+78.5e (MeOH,0=1.01,24^). | m.p.161.0-162.Ot: 線 本紙張尺度適用中國國家標準(CNS ) A4規格(2丨〇乂297公釐) 212 513422 A7 B7 五、發明説明(2〇9 ) 經濟部中央標準局員工消費合作社印製
No.2a.161 [a]D=+65.3e (MeOH,c=1.00,22t:)· No.2a-162 CDC13 300MHz 0.99(lH,d,J=10.2Hz),L13 and 1.25(each 3H,each s),l.53-2.45(14H,m),4.30(1 H,m),5.36-5.51(2H,m),6.32(lH,d,J=8.4Hz),7.88 and 8.28(each 2H,each d,J=9. 0Hz). IR(CHC13):3448,3029,3016,2925,2870,1708,1664,1602,1527,1484,1347 /cm. [a]D=+72.7° (MeOH,c=1.02,22X:). No.2a-163 CDC13 300MHz 0.96(1H,d,J=10.2Hz),1.11 and 1.23(each 3H,each s),1.55-2.51(14H,m),4.26(1 H,m),5.36-5.57(2H,m),6.68(lH,d>J=7.8Hz)>7.41(lH,dd,J=4.8 and 8.1Hz),8.20( lH,d,J=8.lHz),8.66(lH,d,J=4.8Hz),9.00(lH,s). IR(CHC13):3448,3026,3013,2925,2870,2534f 1709,1658,1590,1515,1471 /cm. [a]D=+71.3〇 (MeOH,c=1.01,22t:). No.2a-164 [a]D=+40.8° (MeOH,c=0.98,22<C). No.2a-165 CDC13 300MHz 0.96(lH,d,J=10.5Hz),l.ll and 1.24(each 3H,each s), 1.55-2.52(14H,m),4.24(1 H,m),5.37-5.57(2H,m),6.63(lH,d,J=7.8Hz),7.59 and 8.63(each 2H each d,J= 6.0Hz). IR(CHC13):3447,3346,3028,3016,2925,2870,2538,1941,1708,1662,1556,1516 / cm. 請先, 閱 讀 背 面參 之 注 意 事 項 t 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 213 Ο 1 Ο - 513422 A7 B7
五、發明説明(21Q 經濟部中央標準局員工消費合作社印製 [a]D=+75.4e (MeOH,c=1.01,22t:). No.2a-166 CDC13 300MHz 0.97(lH,d,J=10.2Hz),l.ll and 1.22(each 3H,each s),1.51-2.44(14H,m),2.95(6 H, s),4.25(lH,m),5.33_5.50(2H,m),6.19(lH,d,J=8.7Hz),6.77 and 6.97(each 2H, each d,J=8.4Hz),6.94 and 7.65(each 2H,each d,J=9.〇Hz). IR(CHC13):3453,3024,3016,2924,2871,2806,1739,1708,1647,1612,1604,1515,1 490 /cm. [ct】D=+53.r (MeOH,c=1.02,23t:)· m.p.104.0-105.5t: No.2a-167 CDC13 300MHz I. 01(lH,d,J=9.9Hz),1.19 and 1.26(each 3H,each s),1.56-2.53(14H,m),4.37(l H, m),5.35-5.55(2Hfm),6.47(lH,d,J=8.4Hz),7.61-7.71(2H,m)>7.79(2H,s),7.89-7. 97(2H,m),8.27(lH,d,J=2.1Hz),8.66-8.73(2H,m). IR(CHC13):3450,3024,3014,2925,2870,2667,1707,1650,1531,1509 /cm· [a]D=+70.5〇 (MeOH,c=1.00,22t:). No.2a-168 CDC13 300MHz I. 02(lH,d,J=10.2Hz)f1.20 and 1.26(each 3H,each s),1.56-2.50(14H,in),4.38(l H,m),5.36-5.56(2H,m),6.51(lH,d,J=8.4Hz)l7.61.7.93(7H,in)f8.74(lHtd,J=8.4Hz ),9.15(lH,s). IR(CHC13):3517,3451,3060,3028,3011,2925,2870,2664,1709,1651,1519,1498/c m. [a]D=+54.4〇 (ΜβΟΗ,ο=1.00,23Τ:). (請先閲讀背面之注意事項再本頁) 訂 線 本纸張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 214 513422 A7 B7 五、發明説明(211) 經濟部中央標準局員工消費合作社印製
No.2a-169 CDC13 300MHz 〇.96(lH,d,J=10.5Hz),l.D9 and 1.21(each 3H,each s),1.50-2.44(14H,m),3.85(3 H,s),4.24(lH,m),5.32-5.48(2H,m),6.19(lH,d,J=8.4Hz),6.94 and 7.45(each 2H, each d,J=9.0Hz),7.11 and 7.45{each 2H,each d,J=8.7Hz). IR(CHC13):3516,3453,3029,3009,2925,2870,2840,2665,1708,1650,1593,1515,1 493,1482 /cm· [a]D=+57.8° (MeOH,c=1.00,23r). No.2a-170 CDC13 300MHz 0.98(lH,d,J=10.2Hz),1.15 and 1.24(each 3H,each s), 1.52-2.50(14H,m)>4.28(l Η,ιη),δ.33-5.54(2Η,ιη)>6.25(1Η,(Ι^=8.2Ηζ),7.38-7.44(2Η,ιη),7.74(1Η,5),7.81-7. 86(2H,m). IR(CHC13):3517,3448,3427,3024,3013,2925,2870,2669,1708,1650,1562,1535,1 500 /cm. [a】D=+61.6〇 (MeOH,c=1.00,23t:)· No.2a-171 CDC13 300MHz 0.96(lH,d,J=10.2Hz,l.ll and 1.22(each 3H,each s),1.52-2.42(14H,m),2.48(3 H,s),4.21(lH,m),5.31-5.52(2H,m),6.06(lH,d,J=8.2Hz),6.97 and 7.59(each 1H, each d,J=1.2Hz). IR<CHCi3):3452,3113,3028,3007,2925,2870,2669,1708,1645,1554,1509 /cm. [o:]D=+52.4〇 (MeOHlc=1.00,23<C).
No.2a-172 CDC13 300MHz .96(lH,d,J=10.2Hz),l.09 and 1.28(each 3H,each s),1.50-2.40(UH,m),2.69(3 0 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) (請先閱讀背面之注意事項再本頁) -裝· 訂 線 215 513422 A7 B7 五、發明説明(212 經濟部中央標準局員工消費合作社印製 H,s),4.24(lHfm),5.35.5.51<2H,m)>5.96(lHfd,J=8.7Hz),7-.03 and 7.0T(each 1H, each d,J=5.4Hz). IR(CHC13):3451,3031,3013,2925,2870,2666,1708,1647,1542,1497 /cm. [o:】D=+51.2° (MeOH,c=1.00,23t:). No.2a-173 CDC13 300MHz 〇.95(lH,d,J=10.2Hz),l.l〇 and 1.23{each 3H,each s),l.〇0-2.45(14H,m)f4.22(l H,m),5.35-5.49(2H,m),6.05(lH,d,J=8.4Hz),7.26 and T.75(each lH,each d,J=l. 5Hz). IR(CHC13):3451,3011,3029,3011,2925,2870,1708,1652,1538,1500 /cm. [a]D=+50.6e (MeOH,c=1.01,23t:)· No.2a-174 CDC13 300MHz 0.96(lH,d,J=10.2Hz),1.13 and 1.23(each 3H,each s),1.52-2.50(14H,m),4.29(l H,m),5.35-5.51(2H,m),7.02(lH,d,J=8.4Hz),7.32 and 8.16(each lH.each d,J=3. 9Hz). IR(CHC13):3417,3115,3023,3014,2925,2870,1708,1645,1530 /cm. [a]D=+48.8〇 (MeOH,c=1.02,23t:). No.2a-175 CDC13 300MHz 0.97(lH,d,J=10-2Hz), 1.14 and 1.23(each 3Hfeach s), 1.50-2.52(14H,m),2.52(3 H>s)t4.29(lH,m),5.34.5.51(2H,m),7.78(lH,d,J=9.0Hz)I7.24 and 7.52(each 1H, each d,J=5.4Hz). IR(CHCi3):3329,3093,3023,30 15,2924,287 1,1708,1640,1526 /cm. (a ]D=+45.0〇 (MeOH,c=i.OL,23t:). (請先閱讀背面之注意事項再HP本頁) -裝· 、訂 線 本紙張又度適用中國國家標準(CNS ) A4規格(210X 297公釐) 216 五 、發明説明(213) A7 B7 經濟部中央標準局員工消費合作社印製
No.2a.176 CDC13 300MHz 0.95(lH,d,J=10.5Hz),1.09 and 1.23(each 3H,each s), 1.52-2.46(14H,m),2.40(3 H,d,J=0.9H2),4.24(lH,m),5.35-5.51<2H,m),6.05(lH,d,J=8.7Hz),6.95(lH,m),7.5 7(lH,d,J=3.3Hz). IR(CHC13):3517,3444,3103,3024,3013,2926,2870,1739,1708,1649,1636,1507/c m. {a]D=+54.8° (MeOH,c=1.01,23t:)· m.p.97.0-99.Ot: No.2a-177 CDC13 300MHz 0.97(lH,d,J=10.2Hz),1.11 and 1.23(each 3H,each s),1.52-2.45(14H,m),3.93(3 H,s),4.27(lH,m),5.34-5.50(2H,m),6,35(lH,d,J=3.3Hz),7.80(lH,d,J=S.7Hz),8.10 (lH,d,J=3.3Hz). IR(CHC13):3395,3121,3031,3019,3012,2925,2871,1739,1709,1640,1557,1533 / cm. [a】D=+22.8〇 (MeOH,c=1.01,23t:). m.p.109.0-112.Ot: No.2a-178 CDC13 300MHz 0.96(lH,d,J=10.5Hz),1.10 and 1.23(each 3H,each s),l.51-2.45(14H,m),4.24(1 H,m),5.35-5.50(2H,m),6.09(lH,d,J=8.4Hz),7.17-7.31(6H,m),7.95(lH,d,J=1.5Hz ). IR(CHC13):3510,345 1,3062,303 1,3022,30 11,2925,2870,2662,1708,165 1,1582,1 5351497,1477/cm. [a)D=+47.9〇 (MeOH,0=1.01,25^). (請先閱讀背面之注意事項再本頁)
、*IT 線 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 217 0 17 - 513422 A7 B7 五、發明説明(214 經濟部中央標準局員工消費合作社印製
No.2a-179 CDC13 300MHz 0·96(1Η,d,J=10.2Hz),1.14 and 1.24(each 3H,each s),l.52-2.48(14H,m),4.30(1 H,m),5.36-5.52(2H,m),6.73(lH,d,J=9.0H2),6.26 and 7.37(«ach lH,each d,J=6. 0Hz). IR(CHC13):3509,3429,3115,3094,3025,3014,2925,2871,2666,1708,1649,1529,1 510 /cm. [a]D=+51.0° (MeOH,c=l.02,25X:). No.2a-180 CDC13 300MHz 〇.95(lH,d,J=10.2Hz),1.14 and 1.24(each 3H,each s), 1.52-2.46(14H,m),3.89(3 H,s),4.21(lH,m),5.35-5.50(2H,m),6.05(lH,d,J=8.4Hz),6.46 and 7.04(each 1H, each d,J=1.8Hz). IR(CHC13):3516,3450,3114,3031,3010,2925,2871,1708,1648,1546,1511,1477 / cm. [a ]D=+49.1° (Me011^=1.01,251). No.2a-181 CDC13 300MHz 0.97(lHfdfJ=10.2Hz),1.14 and 1.23(each 3H,each s), 1.52-2.48(14H,m),2.42(3 Hfs),4.31(lH,m),5.34-5.52(2H,m),8.07(lHtd,J=9.3Hz),7.27 and 8.17(each 1H, each d,J=3.3Hz). IR(CHC13):3510,3301,3112,3023,3007,2924,2871,2663,1708,1636,1534 /cm. [a]D=+41.0° (ΜθΟΗ,ο=0.96,25Τ:).
No.2a-132 CDC13 300MHz 0.96(lH,d,J=10.2H2),l.ll and 1.23(each 3H,each s), 1.53-2.46( 14 H,m),2.5 1(3 本紙張·尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) (請先閲讀背面之注意事項再本頁) 訂 線 218 513422 A7 B7 五、發明説明(215 ) H,s),4.21(lH,m),5.35-5.51(2H,m),6.05(lH,d,J=8.lHz),7.26 and 7.78(each 1H, each d,J=1.8Hz). IR(CHC13):3509,3450,3109,3024,3012,2925,2870,2666,1708,1650,1535,1 498,1471 /cm. [a]D=+52.9° (MeOH,c=0.95,25t:). No.2a-183 CDC13 300MHz 0.96(lH,d,J=10.5Hz),1.12 and 1.22(each 3H,each s), 1.52-2.46(14H,m),4.25(1 H, m),5.33-5.51(2H>m),6.17(lH,d,J=8.7Hz),7.01-7.05(3H,m).7.14 and 7.62(eac h 2H,each d,J=8.7Hz),7.27-7.34(2H,m). IR(CHC13):3428,3026,3015,2925,2870,2666,1739,1708,1643,1613,1594,1526,1 499 /cm. [a]D=+64.8〇 (MeOH,c=1.02,23t:). No.2a-184 CDC13 300MHz I. 01(lH,d,J=10.2Hz), 1.18 and 1.26(each 3H,each s), 1.55-2.50(14H,m),4.35(1 H,m),5.35-5.55{2H,m),6.42(lH,d,J=8.7Hz),7.46-7.52<2H,m).7.73(lH,dd,J=1.8 and 8.4Hz),7.83.7.89(2H,m),8.21(lH,m),8.59(lH,d,J=1.5Hz). IR(CHC13):3451,3031,3014,2925,2870,2660,1739,1708,1650,1604,1513,1463 / cm. [a]D=+58.3〇 (MeOH,c=1.00,23t:)· (請先閱讀背面之注意事項再本頁) 訂 線 經濟部中央標準局員工消費合作社印製
No.2a-185 CDC13 300MHz 1.00(lH,dtJ=10.2Hz),1.18 and 1.25(each 3H,each s), 1.55-2.50(14H,m),4.34(1 | ! H,m),5.35-5.54(2Hfm),6.36(lH(d,J=8.7Hz),7.37(lH,t,J=7.4Hz),7.50(lH,m),7.5 | 7-7.59(2H,m),7.79(lH,dd,J=1.8 and 8.1 Hz),7.99( 1 H,d,J=7.8Hz),8.39( 1 H,d,J = 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 219 513422 A7 B7 五、發明説明(216 經濟部中央標準局員工消費合作社印製 1·8Ηζ). IR(CHC13):3451,3030,3<)20,2870,2665,1708,1652,1632,ie〇3,1586,1514,1469,l 448 /cm. [a】D=+59.4。(MeOH,c=1.01,24t). No.2a-186 CDC13 300MHz 1.00(lH,d,J=10.5Hz),1.17 and 1.25(each 3H,each s), 1.54-2.50(14H,m),4.33(1 H,m),5.35-5.54(2H,m),6.37(lH,d,J=8.7Hz),7.37(lH,t,J=7.4Hz),7.51(lH,t,J=7.8 Hz),7.56(lH,m),7.70(lH,dd,J=1.2 and 8.4Hz),7.97(3H,m). IR(CHC13):3451,3030,3014,2924,2870,2671,1739,1708,1652,1577,1517,1488,1 471 /cm. ; [a]D=+72.2° (MeOH,c=1.00,24t:). No.2a-187 CDC13 300MHz 1.00(lH,d,J=9.8Hz),l,18 and 1.25(each 3H,each s), 1.54*2.53(14H,m),4.07(3 H,s),4.37(lH,m),5.30-5.54(2H>m),7.34(lH,m),7.47(lH,s),7.47.7.60(2H,m),7.93( lH,d,J=7.8Hz),8.43(lH,s),8.49(lH,d,J=9.0Hz). IR(CH€13):3397,3074,3027,3020,3009,2924,1738, Π08,1647,1633,1534,1465,1 453 /cm. [a】D=+43.7° (MeOH,c=1.01,25t:)· No.2a-188 CDC13 300MHz 0.97(lH,d,J=10.2Hz),l.ll and 1.23(each 3H,each s), 1.53-2.50( L4H,m).4.23( 1 H,m)l5.37.5.50(2Htm)f6.10(lHtd,J=9.0Hz),6.20(lH,m),6.51(iH,m),6.97(lH,m), 10.81(lH,bs). IR(CHC13):3450,3236,3 112,3029,3015,2925,287 L,2645,170 1,16 16,1558,15 L6 (請先閲讀背面之注意事項再^!本頁) 裝- 訂 綉 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 220 513422 A7 B7 五、發明説明(217) 經濟部中央標準局員工消費合作社印製 /cm. [a]D=+50.69 (MeOH,c=1.01,24t:). No.2a-189 CDC13 300ιΜΗζ 〇.94(lH,d,J=9.9Hz),l.ll and 1.23(each 3H,each s), 1.50*2.46(14H,m),3.93(3 H,s),4.18(lH,m),5.35-5.52(2H,m),6.03(lH,d,J=9.3Hz),6.09(lH,m),6.48(lH,m), 6.73(lH,m). IR(CHC13):3452,3102,3028,3007,2925,2871,2666,1739,170S, 1650,1536,1499,1 471 /cm. [a]D=+49.8°(MeOH,c=1.01,23t:)· ιη.ρ.101.δ-103.5ΐ: No.2a-190 CDC13 300MHz 0.94(lH,d,J=10.2Hz),l.ll and 1.21(each 3H,each s), 1.54-2.47(14H,m),4.23(1 H,m),5.33.5.52(2H,m),6.06(lH,d,J=9.0Hz)>6.34(lH,m),6.75(lH,m),6.36(lH,m), 9.71(lH,bs). IR(CHC13):3470,3215,3030,3020,3010,2925,2871,2664,1709,1613,1564,1510 /cm. [or]D=+43.3a (MeOH,c=1.01,24t:)· No.2a-191 CDC13 300MHz 0.96(lH,d,J=10.2Hz),l.ll and 1.22(each 3H,each s),1.55.2.44(14H,m),3.66(3 H,s),4.20(lHfm)(5.35-5.51(2H,m),5.93(lH,d,J=8.4Hz),6.27(lH>dd,J = 1.3 and 2. 7Hz),6.56(lHft,J=2.7Hz),7.19(lH,t,J=1.8Hz). IR(CHC13):3452,3031,30 18,3006,2925,287 1,2662,1736,17 10,1634,1609,1556,1 498 /cm. (請先閱讀背面之注意事項再本頁) 裝· 絲 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 221 _ O O 1 - 513422 A7 B7 五、發明説明(218 ) 經濟部中央標準局負工消費合作社印製 [a】D=+43.1° (MeOH,c=1.01,23t:). No.2a-192 CDC13 300MHz 0.96(lH,d,J=10.5Hz),l.ll and 1.21(each 3H,each s), 1.43(3H,t,J=7.5Hz), 1.54 .2.44(14H,m),3.93(2H,q,J=7.5Hz),4.21(lH,m),5.33-5.51(2H,m)f5.94(lH,d,J=8. 4Hz),6.27{lH,dd,J=1.8 and 2.7Hz),6.62(lH,t,J=2.7Hz),7.26(lH,t,J=1.8Hz). IR(CHC13):3630,3452,3032,3018,3006,2925,2871,2661,1735,1710,1633,1610,1 555,1497 /cm. [a]D=+40.1° (MeOH,c=1.00,23t:). No.2a-193 : CDC13 300MHz 0.95(lH,d,J=10.2Hz),1.10 and 1.22(each 3H,each s), 1.53-2.49(14H,m),2.58(3 H,s),4.21(lH,m)l5.35-5.54(2H,m),6.15(lH,d,J=8.lHz)>6.52(lH,dd,J=l.S and 3. 6Hz),7.29(lH,t,J=3.6Hz),7.94(lH,t,J=1.8Hz). IR(CHC13):3516,3450,3410,3152,3027,3015,2925,2871,2670,1732,1648,1574,1 509 /cm. [a]D=+45.0° (MeOH,c=1.01,25t:). No.2a-194 CDC13 300MHz 0.99(lH,d,J=10.2Hz),l.ll and 1.24(each 3H,each s),1.52-2.53(14H,m),4.34(1 H,m),5.33-5.57(2H,m)f6.2 l(lH,d,J=8.6Hz),7.35-7.50(2H,m),7.83(1H,s),7.86( 1H, m).8.31(lH,m). IR(CHC13):3443,3067,30 13,2925,2870,2665,1708,165 1,15 15,1493 /cm. [a]D=+55.7° (MeOH,(:=1.01,231).
No.2a-195 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) (請先閱讀背面之注意事項再本頁) 、tr 線 222 513422 A7 B7 五、發明説明(219 CDC13 300MHz (請先閲讀背面之注意事項 l. 01(lH,d,J=10.0Hz),1.06 and 1.26(each 3H,each s), 1.50-2.64(14H,m),2.68(3 H,s),4.40(lH,m),5.36-5.61(2H,m),6.02(lH,d,J=9.4Hz),7.3〇.7.42(2H,m),7.73.7. 86(2H,m). IR(CHC13):3510,3434,3062,3029,3014,2924,2871,2669,1708,1650,1563,1539,1 500 /cm.
[a]D=+72.4° (MeOH,c=1.00,23r). m. p.111.0*112.Ot:
No.2a-196 CDC13 300MHz 0.42 and 1.04(each 3H,each s),0.80(lH,d,J=10.0Hz),l.ll-2.48(14H,m),2.24(3 H,s),4.02(lH,m),5.23.5.44(2H,m),5.53(lH,d,J=S.8Hz),7.27.7.31(2H,m),7.42-7. 4S(3H,m),7.93(lH,s). IR(CHC13):3419,3114,3025,3006,2924,2871,2662,1737,1709,1636,1540,1519 / cm.
[a]D二+43.7° (MeOH,c=1.01,23t:).
No.2a-197 CDC13 300MHz 經濟部中央標準局員工消費合作社印製 0.95(lH,d,J:10.0Hz),1.09 and 1.23(each 3H,each s),l.54-2.46(18H,m),2.77(4 H,bs),4.21(lH,m),5.32-5.54(2H,m),6.02(lH,d,J=8.6Hz),7.43(lH,s)· IR(CHC13):3445,3101,3024,3014,2928,2865,2661,1739,1708 1646,1550,1507 / cm.
[cr]D=+51.9〇 (MeOH,c=1.01,23t:).
No.2a-198 CDC13 300MHz 0.96(lH,d,J=10.2Hz),l.ll and 1.22(each 3H,each s), 1.50-2.44( 14H,m),4.24( 1 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 223 513422 A7 B7 五、發明説明(22〇 ) 經濟部中央標準局員工消費合作社印製 H,m),4.42(2H,s),5.35-5.49(2H,m),6.25(lH,d,J=8.lHz),7.33(lH,m),7.43(lH,dd,J = 1.5and 7.5Hz),7.49(lH,d,J=8.lHz),7.60-7.63(lH,m),7.68(lH,dd,J=1.8 and 7. 8Hz),8.02(lH,d,J=1.8Hz),8.19(lH,dd,J=1.5 and 8.1Hz). IR(CHC13):3448,3030,3012,2925,2870,1739,1708,1671,15SS, 1559,1514,1472 / cm. [a]D=+56.9e (MeOH,c=l.01,24t:). No.2a-199 CDC13 300MHz 0.96(lH,d,J=10.2Hz),l.ll and 1.22(each 3H,each s), 1.5l-2.46(14H,m),3.40(l H,m),3.76(lH,m),4.24(lH,m),5.33-5.51(3H,m),6.25(lH,m),7.16(lH,m),7.24-7.3 3(2H,m),7.46(lH,d,J=7.5Hz),7.52-7.60(?H,m),7.85(lH,dd,J=1.8 and 4.5Hz). IR(CHC13):3583,3447,3062,3028,3013,2924,2871,2663,170s, 1651,1600,1557,1 514,1471 /cm. [a ]D=+54.8〇 (MeOH,c=1.00,23^C). No.2a-200 CDC13 300MHz 0.96(lH,d,J=10.2Hz),1.12 and 1.23(each 3H,each s), 1.5l-2.46(14H,m),4.25(l H,m)f5.34-5.51(2H,m),6.25(lHfd,J=8.4Hz),7.02 and 7.10(each,lH,each d,J=l 2.3Hz),7.23-7.33(4H,m),7.50(lH,m),7.64(lH,dd,J=1.8 and 7.8Hz),7.82(lH,d,J = 1.8Hz). IR(CHC13):3450,3060,3025,3014,2925,2871,2662,1708,1653,1596,1542,1513,1 473 /cm. [_=+62.5〇 (MeOH,c=1.00,2‘ir). No.2a-201 ! I CDC13 300MHz ,! 0.95(19,(1^=9.91^2),1.15 and 1.22(each 3H,each s), 1.55-2.60( 14H,m),4.26( 1 (請先閱讀背面之注意事項再本頁) 本纸張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 224 513422 A7 B7 五、發明説明(mi 經濟部中央標準局負工消費合作社印製 H,m),5.35-5.63(2H,m),7.14(lH,d,J=9.9Hz),7.34 and 7.40(each,lH,each d,J=l 2.9Hz),7.62-7.73(4H,m),8.25-8.30(2H,m),8.72(lH,d,J=1.5Hz). IR(CHC13):3443,3389,3297,3061,3030,3016,2925 2870,1726,1708 1652,1603, 1521,1483,1472,1309 /cm. [a]D=+61.r (Μ«ΟΗ^=1.01,23ΐ:)· No.2a-202 CDC13 300MHz 〇.96(lH,d,J=10.2Hz),1.09 and 1.22(each 3H,each s),1.52-2.43(14H,m),2.63(3 H,s),4.25(lH>m),5.33-5.49(2H,m),6.19(lH,d,J=8.4Hz),7.10 and 7.58(each,2H, each d,cJ=9.0Hz),7.21(lH,m),7.30-7.32(2H,m),7.46(lH,d,J=7.5Hz). IR(CHC13):3511,3453,3062,3032,3014,2925 2870,1739,170S, 1650,1595,1556,1 516,1482,1471 /cm. [〇:]D=+60.2° (MeOH,c=1.01,25t:). No.2a-203 CDC13 300MHz 0.96(lH,d,J=10.5Hz),1.09 and 1.23(each 3H,each s), 1.52.2.43(14H,m),4.23(l H,m),5.35-5.51(2H,111),5.93(lH,d,J=8.7Hz),6.56(lH,dd,J=0.9 and l.SHz),7.43( lH,t,J=1.8Hz),7.92(lH,dd,J=0.9 and 1.8Hz).' IR(CHC13):3517,3450,3134,3031,3008,2925,2870,2667,1708,1656,1588,1570,1 514 /cm. [a]D=+46.7e (MeOH,c=0.92,25t:)· No.2b-l [a!D= +25.6° (MeOH,c=1.01,23t:). No.2b-2 [u 1D= +38·9° (MeOH.cd.Ol^H). j (請先閲讀背面之注意事項再本頁)
、1T 線 本纸張尺度適用中國國家標準(CNS ) Λ4規格(210X 297公釐) 225 513422 A7 __B7 五、發明説明(222 ) d2c-1 [a】D= +60.5° (MeOH,c=1.01,22^C). No.2c-2 [a]D= +55,8° (MeOH,c=0.92,22t:). No.2c-3 [a]D= +54,7。(MeOH,c=1.01,22t:)· No.2d-l [a]D= -6.2° (MeOH,c=1.00,2lt:). No.2d-2 [a]D=+15.8 (MeOH,c=0.34,22^C).
No.2d.-3 [α]Ό=+31.6β (MeOH,c= 1.01,22X3). No.2e-1 [a -9.4° (MeOH,0=1.00,221).
No.2e-2 經濟部中央標準局員工消費合作社印製 [a]D= -1.8° (MeOH,c=1.02,23t:). No.2e-3 [a]D= -6.7° (ΜβΟΗ,ο=1.01,23ΧΙ). No.2f-l 本纸張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 513422 A7 B7 五、發明説明(223 [a]D= +6.8e (MeOH,c=1.01,23t:)·
No.2f-2 [a]D= -2.6° (MeOH,c=1.00,22t:).
No.2f-3 [a]D= -3.5° (MeOH,c=1.01,22t:).
No.2g-l [a]D= +54,6° (MeOH,c=1.01,24t:)·
No.3a-2 . CDC13 300MHz 0.98-2.15(14H,m),2.31(2H,t,J=7.2Hz),2.35-2.40(lH,m),3.10-3.20(lH,m), 5.00(lH,d,J=6.9Hz)>5.30-5.48(2H,m),6.75(lH,d,J=10.2Hz),7.38-7.52(6H,m). IR(CDC13):3266,3028,2954,2874,1709,1620,1448,1412,1318,1141,970,892/cm.
[a]D=+20.3 土 0.6* (CHC13,c=1.05,24t:)·
No.3a-3 CDC13 300MHz 0.95-2.00(14H,m),2.20-2.29(3H,m),3.00-3.08(lH,m),3.66(3H,s),5.00(lH,d, 經濟部中央標準局員工消費合作社印製 J=6.6Hz〉,5.13-5.29(2H,m),7·38·7.52(3H,m),7.59-7.65(2H,m),7.69· 7.75(2H,m),7.92-7.98(2H,m). IR(CHC13):3376,3018,2946,2868,1727,1594,1436,1395,1322,1157,1095,S90 /cm.
[a ]D=+2.3 土 0.4· (CHC13,c二 1.03,22C). mp.65-66.5^3
No.3a-4 本纸張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 227 513422 A7 B7 五、發明説明() 經濟部中央標準局員工消費合作社印製 CDC13 300MHz 0.93-2.05(14H,m),2.15-2.22(lH,m),2.31(2H,t,J=7.2Hz),3.Ol-3.10(lH,m), 5.18-5.31(3H,m),7.38-7.52(3H,m),7,58-7.66(2H,m),7.69·7·76(2Η,ιη),7.92· 7.98(2H,m) IR(CHC13):3374,3260,3020,2948,2868,1708,1594,1479,1396,1319,1156,1095,1 052,891/cm. [a]D=+13.1±0.5.(CHC13,c=1.16,24t:)· No.3a-6 CD30D 300MHz 1.04· 1.95(14H,m),2.07(2H,t,J=7.8Hz),2·14.2·22(1Η, m), 2.94-3.00(lH,m), 5.04. 5.25(2H,m),7.36-7.52(3H,m),7.66-7.71(2H,m),7.78-7.85(2H,m),7.91- 7.97(2H,m). IR(KBr):3421,3278,2951,2872,1562,1481,1409,1317,1156,1097,1057,895/cm. [cc]D=-15.3±0.5· (CHC13,〇=1.06,23^:)· mp.105-112^ No.3a.ll CDC13 300MHz 0.90-2.04(14H,m),2.08.2.19(lH,m)l2.35(2H,t,J=7.2Hz),2.95-3.04(lH,m), 5.17- 5.32(3H,m),7.56-7.63(2H,m),7.83.7.95(2H,m). IR(CHC13):3260,3020,2948,286811707,1569,1456,1383,1325,126S, 1160,1088, 1053,1006,892/cm. [a jD=+8.3土0.5· (CHC13,c=1.00,22t:).
No.3a* 16 CDC13 300MHz 0.80-1.90(14H,m),1.98-2.04(lH,m),2.27(2H,tfJ=7.2Hz),2.88(6H,s),2.90- 2.98(lH,m),4.88-5.00(2HIm),5.13(lH,dtJ=7.2Hz)I7.18(lH,d,J=7.5Hz),7.48- 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) (請先閱讀背面之注意事項再尽頁) 訂 線 228 513422 A7 B7 五、發明説明(225 7.60(2H,m),8.25-8.33(2H,m),8.53(lH,d,J=8.7Hz). IR(CHC13):3272,3020,2946,2866,2782,1708,1573,1455,1407,1311,1229,1160, 1142,1070,942,891/cm.
[a]D=-19.7土0·6· (CHC13,c=.1.08,23.5t:).
No.3a-31 CDC13 300MHz 0.80-l.S5(14H,m),2.02-2.08(lH,m),2.20(2H,t,J=7.2Hz),2.85-2.95(lH,m), 3.68(3H,s),4.80-4.92(2H,m),4.96(lH,d,J=6.9Hz),7.50-7.70(3H,m),7.92. 7.98(lH,m),8.07(lH,dlJ=8.4Hz),8.29(lH,dd,J=1.5&7.5Hz),8.65 (lH,d,J=8.7Hz). IR(CHC13):3374,3016,2946,2868,1727f1506,1435,1318,1160,1133,1105,1051, 984,890/cm.
[a ]D=-39.3土0.8· (CHC13,c=1.07,22t:).
No.3a-32 CDC13 300MHz 0.80-L90(14H,m),1.95-2.05(lH,m),2.27(2H,t,J=7.2Hz),2.90-2.96(lH,m)f 4.85· 5.00(2H,m),5.23(lH,d,J=6.6Hz)>7.50-7.72(3H,m)l7.95(lH,d,J=8.lHz)l 8.07(lH,d,J=8.4Hz),8.29{lH,dd,J=1.2&7.5Hz),8.66(lH,d,J=9.0Hz). IR(CHC13):3270,3020,2948,2868,1708,1455,1412,1317,1159,1132,1104,1079,1 051,983,891/cm.
[a]D=-29.2±0.6.(CHC13,c=1.08,22t:)· 經濟部中央標準局員工消費合作社印製
No.3a-33 CD30D 300MHz 0.94-1.84(14Hfm),L96-2.08(3H,m),2.77-2.84(lH,m)f4.67-4.84(2H,m),7.55-7.75(3H,m),8.02(lH,d,J=7.8Hz),8.12-8.26(2H,m),8.74(lH,d,J=8.7Hz). IR(KBr):3432,3298,295 1,2872,1564,14 12,1315,1 159,1134,1 107,1082,1058, 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 229 513422 A7 B7 五、發明説明(226 986/cm. [a ]D=-79.9土 1·2· (CH30H,c=1.00,23t:)· No.3a-34 CDC13 300MHz 0.97-1.91(14H,m),2.13-2.20(lH,m),2.42(2H,t,J=7.2Hz),3.00-3.07(lH,m), 5.06-5.24(2H,m),5.33(lH,dfJ=6.9Hz),7.57-7.68(2H,m),7.82-8.00(4H,m), 8.45(lH,d,J=1.2Hz) IR(CHC13):3260,3020,2948,1708,1408,1319,1154,1129,1073,953,893/cm. [a ]D=+20.7土 0.6· (01^13^=1.07,22=). No.3a-35 CD30D 300MHz 1.03.2.20(m,17H),2.97(m,lH),5.02(m,2H),7.64(m,2H),8.00(m,4H),8.43(S,lH). IR(KBr):3360,3285,1562,1407,1316,1153,1130,1075/cm. [a]D=^0 [α]365=+20·9 土 0.6-(CH30H,c=1.04,23t:)· (請先閱讀背面之注意事項再本頁) 裝· 丁 、-'口 經濟部中央標準局員工消費合作社印製
No.3d-l CDC13 300MHz 0.93-2.55(m,17H),3.02(m,lH),5.24(m,2H),6.48(m,lH),7.35-7.60(m,3H)f7.85- 8.00(m,2H) IR(Nujol): 3275,1548,1160,1094,758,719,689,591,557/cm. [a 】D=+19.0土0.6。(¢:11301^=1.010,26.51). 元素分析(〇20 14 26 1^〇45*1/2〇3.1.0142〇七1^1:) 計算値:C, 57.94:H, 6.82;N, 3.38:Ca. 4.83; H 2 O, 4.3 5 實測値:C,5 7.8 0 ; H. 6.68 ; N, 3.68 ;Ca, 5.06; H 2 〇,4.5 0 線 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 230 513422 A7 B7 五、發明説明( 227 )
No.3d-6 [cr】D=-20.7土0.6· (CHC13,c=1.00,24t:)· No.3d-7 [a]D=-3.2±0.4.(CHC13:c=1.03,22t:).
mp.65-67*C ,
No.3d-8 [α]〇=·14·5 土 0.5*(CHC13,c=1.07,24t:)· No.3d-9
[a】D=+12.2 土 0.5.(CH30H,c=1.00,23X:)· mp.H9-125,C
No.3d-10 [a 】D=+39.7土0·8· (CHC13,c=1.07,22t:)· No.3d-ll [a】D=+29.2 土 0.7*(011(:13,。=1.06,221)· No.3d-12 經濟部中央標準局員工消費合作社印製 [a】D=+76.4土 1·Γ ((:Η30Η,〇=1·03·24^:)· No.3d-14 [a】D=-20.6士0.6· (¢311(:13,0=1.07,221). No.3d-15 [a 1365=-28.0土0.7· (0^3011^=1.03,24.5^). 本紙浪尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 231 513422 A7 B7 五、發明説明( 228 ) 經濟部中央標準局員工消費合作社印製
No.3d-16 [a 】D=-8.7 ± 0.5· <CHC13,c=1.06,22t:). No.3d-17 CDC13 300MHz 0.80-2.15(m,24H),2.32(t,J=7Hz,2H),2.68<t,J=7Hz,2H),3.02(m,lH),2.15 (m,24H),2.32(t,J=7Hz,2H),2.68(t,J=7Hz,2H),3.02(m,lH),5.22(m,2H),5.38(d,J: 7Hz,lH),7.30(A2B2q-Apart,J=SHz,2H),7.81(A2B2qBpart,J=8Hz,2H),9.86 (br.s,lH). {a]D=^0 [α]365=·9.7士0.5〇 (CHC13,c=1.03,22t:)· No.3d-24 [a 】D=+19.2± 0.6· ((^013/=1.05,23^:). No.3d-26 CD30D 300MHz 0.9〇.2.20(20H,m),2.88(lH,m),3.07(2H,q,J=7.0Hz),5.00-5.40(2H,m)>7.20- 7.60(4Hfm),7.95(lH,m). IR(KBr):3415,3254,1698,1564,1314,1154/cm. No.3d-28 CD30D 300MHz 0.90-2.20(20H,m),2.73(2H,q,J=7.0Hz),2.93(lH,m),5.00.5.30(2H,m),7.40- 7.50(2H,m),7.60-7.77(2H,m). IR(KBr):3435,3280,1562,1323,1304,115 1/cm. No.3d-30 (請先閱讀背面之注意事項再本頁) 訂 線 本纸張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 232 513422 A7 B7 五、發明説明(229) 元紊分析 C20H25BrN〇4SNa Calc.C50.21;H5.27;Brl6.70;N2.93;S6.70;Na4.81 found.C50.22;H5.40;Brl5.57;N2.88;S6.41;Na5.10 IR(KBr):3425r3280,3085,1697,1570,1410,1321,1165,1155/cm.
No.3e-l CD30D 300MHz 0.71(lHfd,J=10.2Hz),1.04(3Hfs)l1.12(3H,s),1.35-2.28(14H,m), 2.42(3H,s),3.17-3.25(lH,m),5.18-5.39(2H,m)t7.37(2H,d,J=8.4Hz),7.75(2Htd,J=8.4Hz). IR(CHC13):3400,3289,2986,2924,2870,1559,1424,1322,1305,1160,1095,1075,1 030/cm.
[a 】D=+25.9土0.7· (¢^301^=1.00,23=). 經濟部中央標準局員工消費合作社印製 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 233 513422 A7 B7 五、發明説明(230 鼷於上述實施例得到之化合物,K如下實驗例所示之 方法進行活體内及活體外試驗。 奮驗例1 PGDa受容體之結合實驗 試驗材料及試驗方法 ⑴人血小板膜區分之調製 從健康正常人(成人男性及女性)之靜脈之裝有3.8 %檸檬酸納之塑膠製注射器採取到的血液置入塑膠製試驗 管内,輕輕傾倒混合後,於室溫Μ 1800 rpin,10分鐘離心 分離,採取上清之多血小板血漿[PRP(Platelet rich Plasma)]。將此PRP進一步附諸室溫2300 rpm,22分鐘之 離心分離,得到血小板。所得到之血小板使用hofliogenizer (Ultra-Turrax)而經同質化後,K4t!,2000 rpm,10 分 鐘離心分離進行3次,得到血小板膜區分。膜區分蛋白定 量後,成為2nig/ml,供應結合實驗而於-80TC下冷凍保存 (請先閱讀背面之注意事項再本貢) 訂 經濟部中央標準局員工消費合作社印m ⑵PGD,受容體之結合實驗 於結合反應液(50 bM TrB/HCl,pH 7.4,5 mM MgCla> 0.2®1中加入人血小板膜區分(O.ling)及5 nM[3H] PGDa(115 Ci/mffl〇l),於41C下反應90分鐘。反應後使用玻璃纖維濾 紙過濾,以冷生理食鹽水洗淨數次,测定殘餘在濾紙之放 射活性。特異性結合量係從全結合量減去非特異性結合量 (10 PGD2#在下之結合量)之值。各化合物之結合阻 礙活性係Μ在化合物非存在下之結合量作為100%,求取 各化合物存在下之結合量(%)而作成取代曲線,算出50% 線 本纸張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 234 513422 A7 B7 五、發明説明(231 ) 抑制濃度(I CeD值)。結果表示於下。 化合物编號結合活性UM>化合物编號結合活性UM) 3a - 4 0.6 2a-4 0.54 la-115 8.6 2a -17 0.12 la-28 0.045 2a - 21 5.2 la - 47 0.0086 2a-28 0.046 la-100 0.56 2a-95 1.6 la-176 0.047 2a-109 0.003 la-2 0.13 1 a-162 0.027 (請先閲讀背面之注意事項再 -- 本頁) 經濟部中央標準局員工消費合作社印製 實驗例2 使用人血小板之PGDa受容體的拮抗活性 Μ預先添加有1/9之檸樺酸一右旋糖液的注射器從健 康正常人採取末梢血液,以180g離心10分鐘後,採取上清 (PRP : Platelet roch plasma)。Μ洗淨緩衝液將所得到 之PRP離心洗淨3次後,Mmicrocell計數器計數血小板數 目。將調製成最終濃度5X 10e®/ml之血小板浮游液加溫 至37它後,M3-異丁基-1甲基黃瞟呤(0.5bM)前處理5分 鐘,添加稀釋成各種濃度之化合物,10分鐘後,添加0.1 〜2·0ίΐΜ之PGDa而引起反應。15分鐘後加入鹽酸Μ停止反 應,Μ超音波homogenizer破壊血小板,離心後Μ放射分 析定量其上清中之CAMP。藥物之PGDa受容體拮抗活性係Κ 各濃度求取對於藉PGDa添加而增加之CAMP的抑制率,算出顯 示50%阻礙之藥物濃度而進行評價。結果表示於下。 訂 本紙浪尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 235 513422 A7 B7 五、發明説明(232 化合物编號 人血小板cAMP上昇阻礙IC^UM) 3a-16 0.37 la-121 2.11 la-28 0.30 la - 47 2.09 2a - 2 0.77 2a-4 0.94 2a-35 1.52 2a-75 0.71 (請先閲讀背面之注意事項本頁) 經濟部中央標準局員工消費合作社印製 實驗例3 鼻塞模型之實驗 使用天竺鼠之鼻腔抵抗之測定及抗鼻塞作用之評價方 法表示於Μ下。以超音波嗅霧器將1%卵白清蛋白(OVA)溶 液煙霧化,使此令Hartley条雄性天竺鼠每隔一遇Μ 2次 各吸入10分鐘而作用之,其7日後,暴露抗原而引起反應 。戊巴比妥(30 ag/kg,i.p.)麻醉下切開天竺鼠的氣管而 分別於鼻腔俩與肺侧裝載揷管,於肺側連接一可Μ每分鐘 60次、1次4ml之空氣的人工呼吸器。Μ加拉明(gallamine) (2 mg/kg,i.v.)使天竺鼠之自發呼吸停止後,從鼻腔侧 之插管使用人工呼吸器將每分70次、1次4ml之空氣送至鼻 吻側,介由裝載於側枝之轉換器Μ測定此送氣中必要的空 氣壓,作爲彝腔抵抗的指標。抗原的暴露係藉由於人工呼 吸器與鼻腔揷管之間使3% 0VA溶液的煙霧劑產生3分鐘 來進行的。被檢藥物乃於抗原暴露的10分鐘前靜脈注射。 成績係連績测定0至30分鐘間之鼻腔抵抗,其分鐘間之 AUC〔縱軸為鼻腔抵抗(caHa〇>、横軸為時間(0-30分鐘)〕 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 236 513422 A7 B7 五、發明説明(233 當為指檫,表示成對於媒液之抑制率。結果表示於Μ下 化合物纗號 抑制率(%> lng/Kg(i.v J 備 考 3ag/Kg(i.v.) 10ag(Kg(p.ο.) l〇eg(Kg(p.ο.) 製劑例1 經濟部中央標準局員工消費合作社印製 la - 28 44 la-98 69 la-100 50 la-115 66 la-116 48 la-120 58 la-2 82 la-162 80 la-176 60 la-267 62 2a - 4 60 2a-21 52 2a-28 54 2a-95 77 2a-96 77 2a-109 73 2a-110 66 2a-194 79 (請先閱讀背面之注意事項本頁) 錠劑之製造 依常用的方法製造一含有40 ng之有效成分的錠劑 40 mg錠的組成表示於下。 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 237 513422 A7 B7 234 五、發明説明( ( + )-(Z)-7-[(lR,2S,3S,4S)-3 -苯磺醯胺雙環[2,2,1]庚-2 - 基]-5-庚烯酸鈣二水和物 40.0 mg 羥丙基纖維素 3.6 mg 硬脂酸鎂 0.4 mg 玉蜀黍澱粉 18.0 mg 乳糖 58.0 mg 合計 120.0 mg 製劑例2 顆粒劑之製造 (+)-(Z)-7-[(lR,2S,3S,4S)-3 -苯磺醯胺雙環[2,2,1]庚-2- 經濟部中央標準局員工消費合作社印製 基]-5-庚烯酸鈣二水和物 100. .0 mg 羥丙基纖維素 30. ,0 mg 羧甲基纖維素鈣 30. ,0 mg 滑石粉 10. ,0 mg 聚氧伸乙基(160)聚氧伸丙基(30> 乙二醇188 20. 0 ag 結晶纖維素 70. 0 mg 玉蜀黍澱粉 300. 0 mg 乳糖 440. 0 mg 合計 1000.0 mg 238 本紙張尺度適用中國國家標準(CNS ) Α4規格(210X 297公釐) 513422 補充說明書 (一) 申請案號數:第八五一〇七四二五號 (二) 申請案名稱:雙環之環系胺基衍生物及含有該衍生物之?〇〇2拮 抗劑組成物 (三) 申請人姓名:曰商•鹽野義製藥股份有限公司 地址:日本 代理人姓名:憚軼群技師(M100046301,台代字第487號) 康偉言技師(A104293682,台代字第1501號) 地址:台北市松山區105南京東路三段2 4 8號七樓 (四) 補充之依據·· 87.09.11·台專(玖)02021字第131515號函 收文日期:中華民國87年09月14曰
(五) 補充要點··依原已揭示之内容,補充具有r<DY f^Y結構 經濟部中央標準局員工消費合作社印製 之化合物的物理化學數據,及使用人體血小板 之PGD2受容體的拮抗活性(IC50)。 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 513422 (六)補充内容:
COOH
COOH
S
經濟部中央標準局員工消費合作社印製 Ή-NMR及其他數據 1 1.20-2.40 (13H, m)r 3.01 (1H, m), 4.07 (1H, d, J =: 4.0 Hz), 4.41 (1H, tf J = 5.0 Hz), 5.16 (2H, m), 5.64 (1H, d, J = 6.0 Hz), 7.5δ (3H, m), 7.88 (2H, m). IR(film): 3206, 1706, 1157 cm*1 2 0.87 and 1.24 (each 3H, each s), L51 (1H, d, J = 10.5 Hz), L60-2.61 (14¾ m), 4.24 (1H, m), 5.32-5.45 (2H, m), 6.12 (1H, d, J = 9.0 Hz), 7.37-7.48 (2H, m), 7.85-7.88 (2H, m), 8.33 (1H, d, J = 7.8 Hz). IR (CHCla): 3429, 3067, 3023, 3014, 2923, 2871, 1708, 1652, 1556, 1516, 1494(:1^4:^25-23.0° (c=1.00%,CH3OH) 3 1.11 and 1.24 (each 3H, each s), 1.50 (1H, d, J = 10.8 Hz), 1.59^2.60 (14H, m), 4.20 (1H, m), 5.32-5.45 (2H, m), e.09 (1H, d, J = 8.4 Hz), 7.16 (1H, ddd, J = 2.4, 9.0 and 10.2 Hz), 7.77 (1H, dd, J = 4.8 and 9.0 Hz), 7.93 (1H, s), 8.09 (1H, dd, J = 2.4 and 0.2 Hz). IR (CHCls): 3429, 3095, 3030, 3015, 2923, 2871, 1708, 1653, 1603, 1566, 1517, 1432 cm*1 [α]〇23-22.4° (c=1.〇1%,CH3OH) 一 2- 本紙張尺度適用中國國家標準(CNS ) a4規格(210X297公釐) 513422 0.86 and 1.23 (each 3Hr each s), 1.49^2.58 (15H, m), 4.24 (1H, m), 5.25-5.40 (2H, m), 6.18 (1H, d, J = 9·0Ηζ), 7.03 (1H, dd, J = 2.4 and 8.7 Hz), 7.66 (1H, d, J = 8.7 Hz), 7.77 (1H, s), 8.06 (1H, d, J = 2.4 Hz). IR(CHC13): 3425, 3237, 3029, 3021, 3017, 2924, 2871,1707, 1637, 1519, 1457, 1437 cm*1 [α]〇25-18.7° (c=1.00%, CH3OH) 5 0.91 (1H, d, J = 10.2 Hz), 1.13 and 1.25 (each 3H, each s), 1.60-1.88 (3H, m)F 2.01- 2.50 (10H, m), 2.79 (1H, t, J = 11.6Hz), 4.54 (1H, m), 5.31- 5.50 (2H, m), 6.10 (1H, d, J = 8.4 Hz), 7.37-7.48 (2H, m), 7.85-7.88 (2H, m), 8.33 <1H, d, J = 7.5 Hz). IIUCHCla): 3429, 3065, 3023, 3015, 2923, 2872, 1708, 1651, 1556, 1516, 1493 cm'1 [α]ϋ25+26.5° (c=1.01%f CHsOH) 6 0.91 (1H, d, J = 10.2 Hz), 1.12 and 1.25 (each 3H, each s), 1.60-1.90 (3H, m), 2.01-2.50 (10H, m), 2.78 (1H, t, J = 12.2 Hz), 4.52 (1H, m), 5.30-5.50 (2H, m), 6.08 (1H, d, J = 8.4 Hz), 7.16 (1H, dt, J = 2.7 and 8.7 Hz), 7.77 (1H, dd, J = 4.5 and 8.7 Hz), 7.91 (1H, s), 8.09 (1H, dd, J = 2.7 and 9.9 Hz). IR(CHCls): 3430, 3095, 3024, 3015, 2923, 2872, 1708,1652, 1603, 1565, 1517, 1433 cm1 [a]D25+25.8° (c=1.00%, CH3OH) 7 0.88 (1H, d, J = 9.9 Hz), 1.11 and 1.26 (each 3H, each s), 1.50-1.90 (3H, m), 2.00-2.23 (8H, m), 2.40-2.50 (2H, m), 2.83 (1H, t, J = 12.0 Hz), 4.55 (1H, m), 5.24-5.44 (2H, m), 6.11 (1H, d, J = 9.0 Hz), 7.02 (1H, dd, J = 2.4 and 8.4 Hz), 7.67 (1H, d, J = 8.4 Hz), 7.75 (1H, s), 8.12 (1H, d, J = 2.4 Hz). IR(CHCl3): 3425, 3222, 3028, 3022, 3015, 2923, 2872, 1707, 1637, 1601, 1519, 1456, 1437 0^((^25+19.3° (c=1.00%, CH3OH) 請 先 閲 讀 背 φ 之 注 意 事 項 再 .装 訂 經濟部中夬榡準局員工消費合作衽印製 使用人體血小板之PGD2受容體的拮抗活性(IC5。) 化合物編號 β Μ 化合物編號 β Μ 1 *(7.1%) 5 0.37 2 0.77 6 0.037 3 0.58 7 0.23 4 0.29 10 Μ Μ時69抑制率 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 513422 補足說明 3
5
4 O-NMR and other data 1 1.20-2.40 (13H, m), 3.01 (1H, m), 4.07 (1H, d, J = 4.0 Hz), 4.41 (1H, t, J = 5.0 Hz), 5.16 (2H, m), 5.64 (1H, d, J = 6.0 Hz), 7.55 (3H, m), 7.88 (2H, m). IR(film): 3206, 1706, 1157 cm·1 2 0.87 and 1.24 (each 3H, each s), 1.51 (1H, d, J = 10.5 Hz), 1.60-2.61 (14H, m), 4.24 (1H, m), 5.32-5.45 (2H, m), 6.12 (1H, d, J = 9.0 Hz), 7.37-7.48 (2H, m), 7.85-7.88 (2H, m), 8.33 (1H,d, J = 7.8 Hz)· IR (CHC13): 3429, 3067, 3023, 3014, 2923, 2871, 1708, 1652, 1556, 1516, 1494 0^4^25-23.0° (c=1.00%,CH3OH) 3 1.11 and 1.24 (each 3H, each s), 1.50 (1H, d, J = 10.8 Hz), 1.59-2.60 (14H, m), 4.20 (1H, m), 5.32-5.45 (2H, m), 6.09 (1H, d, J = 8.4 Hz), 7.16 (1H, ddd, J = 2.4, 9.0 and 10.2 Hz), 7.77 (1H, dd, J = 4.8 and 9.0 Hz), 7.93 (lH, s), 8.09 (1H, dd, J = 2.4 and 0.2 Hz). IR (CHCls): 3429, 3095, 3030, 3015, 2923, 2871, 1708, 1653, 1603, 1566, 1517, 1432 cm*1 [a]D25.22.4° (c=1.01%,CH3OH) 513422 4 0.86 and 1.23 (each 3H, each s), 1.49-2.58 (15H, m), 4.24 (1H, m), 5.25-5.40 (2H, m), 6.18 (1H, d, J = 9.0Hz), 7.03 (1H, dd, J = 2.4 and 8.7 Hz), 7.66 (1H, d, J = 8.7 Hz), 7.77 (1H, s), 8.06 (1H, d, J = 2.4 Hz). IR(CHC13): 3425, 3237, 3029, 3021, 3017, 2924, 2871, 1707, 1637, 1519, 1457, 1437 0111^^10^-18.7° (c=1.00%, CHsOH) 5
0.91 (1H, d, J = 10.2 Hz), 1.13 and 1.25 (each 3H, each s), 1.60-1.88 (3H, m), 2.01- 2.50 (10H, m), 2.79 (1H, t, J = 11.6Hz), 4.54 (1H, m), 5.31- 5.50 (2H, m), 6.10 (1H, d, J = 8.4 Hz), 7.37-7.48 (2H, m), 7.85-7.88 (2H, m), 8.33 (1H, d, J = 7.5 Hz). IR(CHC13): 3429, 3065, 3023, 3015, 2923, 2872, 1708, 1651, 1556, 1516, 1493 cm*1 [^]d25+26.5〇 '(c=1.01°/〇, CHsOH). 6 0.91 (1H, d, J = 10.2 Hz), 1.12 and 1.25 (each 3H, each s), 1.60-1.90 (3H, m), 2.01-2.50 (10H, m), 2.78 (1H, t, J = 12.2 Hz), 4.52 (1H, m), 5.30-5.50 (2H, m), 6.08 (1H, d, J = 8.4 Hz), 7.16 (1H, dt, J = 2.7 and 8.7 Hz), 7.77 (1H, dd, J = 4.5 and 8.7 Hz), 7.91 (1H, s), 8.09 (1H, dd, J = 2.7 and 9.9 Hz). IR(CHCl3): 3430, 3095, 3024, 3015, 2923, 2872, 1708, 1652, 1603, 1565, 1517, 1433 cm*1 [a]D25+25.8° (c=1.00°/〇, CHsOH) 7 . 0.88 (1H, d, J = 9.9 Hz), 1.11 and 1.26 (each 3H, each s), 1.50-1.90 (3H, m), 2.00-2.23 (8H, m), 2.40-2.50 (2H, m), 2.83 (1H, t, J = 12.0 Hz), 4.55 (1H, m), 5.24-5.44 (2H, m), 6.11 (1H, d, J = 9.0 Hz), 7.02 (1H, dd, J = 2.4 and 8.4 Hz), 7.67 (1H, d, J = 8.4 Hz), 7.75 (1H, s), 8.12 (1H, d, J = 2.4 Hz). IR(CHC13): 3425, 3222, 3028, 3022, 3015, 2923, 2872, 1707, 1637, 1601, 1519, 1456, 1437 cm*1 [a]D25+19.3° (c=1.00%, CHsOH)
匕卜血小板奁使〇 PGD2受容体®拮抗活性(IC50)
Compound No H Μ Compound No PL M 1 *(7.1%) 5 0.37 2 0.77 6 0.037 3 0.58 7 0.23 4 0.29 * 10 Μ Μ時©抑制率 以上 一2— 513422 資料1 la-2 1&·3 la-14 la-15 la-20 la-21 la-143 la-144 la· 145 la-155 la. 157 la· 158 la-159 la-160 la>171 la-172 la-173 la-174 la-184 la-188 la-189 la· 190 la-191 2flt-32 2a-33 2a>54 2a-55 2a-58 2a-59 2a-61 2a-63 実験例1 (MM) 0·13 0.03 1-2 0.4 0,76 0.6 実験例2 (江Μ) 0.08 0.18 実験例3 (%) 82 75 38 0.25 0.10 0.18 0.79 0.18 >1 0.46 0.18 6.0 0.55 5.9 >10 >10 3.8 1·50.6 7.5 10> 7.2 3·3 0·22 0.38 >1 >1 >1 513422 2a-67 0.0089 2a-69 0.0089 2a-89 1.4 2a-91 0.4 0.466 2a-93 2.0 0.22 38 2a-95 0·13 0.224 77 ' 2a-103 >10 >1 2a-139 0.015 0.29 16 2a-150 >1 2a-151 >1 2a-152 >1 2a-154 0.38 2a-156 >1 2a-170 0.0013 0.39 2a-171 0.024 0.24 2a-172 1.98 2a-174 0.28 2a-184 0.39 2a· 185 0.032 0.22 2a-186 >1 2a-188 0.032 0.064 34 2a-189 0.057 9 2a-190 26 2a-191 0.1 2a-192 0.026 2a· 198 0.18 2a-199 0.47 2a-200 0.50 2a-201 0.63 2a-206 0.082 2a-207 0.21 2a-274 0.44 2a-275 0.24 2a-278 0.219 2a-279 0.259 2a-282 0.47 2a-283 0.65
2 513422 SL 27
補充資料:自化合物「3d-l’」製備「3d:l」的方法 將取自於中文說明書第28頁實施例3所製備之化 合物3d_l’((2)-7-[(1以,23,33,43)-3-笨基磺醯基胺基雙 %[2,2,1]庚-2-基]-5_庚稀酸:1弓)依下述方法製備其水合 物一化合物3d-1。 (中文版) 於化合物(3d-Γ)(4.49克,11.9毫莫耳)中添加水(25毫升) 及1當量之氫氧化鈉水溶液(11.9毫升)。於所得之水溶液 中,在室溫下添加CaCl2(1.32克,11.9毫莫耳)溶於水(50毫 升)的溶液。將反應溶液攪拌6小時,濾取生成的結晶。將 所得之結晶以水清洗,得到4.68克(94.9%)化合物(3d-1), 為無色枉狀結晶。 (曰文版) 「化合物(3d —Γ ) (4.4 9g, 1 l/9mmol)丨C水(2 5ml)及VI規定水酸化 于卜y々厶水溶液(1 1 · 9 mL) ξ:加;水溶液1C、室通TCC a C 1 2 (1· 3 2g、ll.9mmol) S:、水(5 0mL){C溶加ΙΛ:水溶液ί:加文反応液 6時間携拌匕、生匕Λ:結晶奁5取結晶《:水T洗浄U 4. 68g (9 4· 9%) (〇化合物(3d — 1)奁無色柱状結晶tLT得Λ:β J 經濟部中央標準局貝工消費合作社印製 本紙張尺度適用中國國家棣準(CNS ) A4規格(210 X 297公釐)

Claims (1)

  1. 3 IX 5
    公 ABCD 六、申請專利範圍 第8篇425號專利申請案申請專利範圍修正本的年9月27日 1. -種用以料前列腺B2(PGD2)结抗劑之醫藥組成物 ,其係含有一以式(I)
    表示的雙環之環系胺基衍生物或其鹽亦或水合物作為有 效成分;(上述式中, 0 乃表示 A 為 -CH2-CH = CH-(CH2)3- 、 -ch2-ch=ch-(ch2)2-c(ch3)2- 、_ch2-c(=o)-(ch2)4-、 -CH=CH-(CH2)3-、c广c9烷撐基; 、一心一crv一 B為氫、Ci〜C6烷基、CrQ烷基苯基; R為 COORi、CH2OR2 或 CON(R3)R4 ; R1為氫或Cl〜C6烷基; R2為氮; 尺3及R4分別為氫、羥基或CpCs烷基磺醯基; 本紙張尺度適用中國國家標準(CNS) A4規格(210X297公釐) -239- 513422 Λ BCD ^、申請專利範圍 Χι為單鍵、苯樓基、嚷吩二基、吲哚二基或嘮唾二 基; Χ2為單鍵、-Ν=Ν-、-N=CH-、-CH=N-N-、-(Ι;Η=Ν-〇-、 -CH=CH_、-CH=(OH)-、-C(C1)=C(C1)-、-(CH2)n、-Ce C-、 -N(R5)-、-N(R51)CO-、-N(R53)CON(R54)-、-CON(R55)-、 ·0-、-S-、-SO-、-S02-、-CO-、-CH20-、秦吐二基,、 或四嗤二基; Χ3為烷基、c2〜c6烯基、苯基、萘基、菲基、 芴基、Ci〜C6烧基笨基、二苯并吱喃基、σ塞吩基、味唾基、 苯并σ塞吩基、盼三σ秦基、苯并噚ϋ坐基、二苯并噚σ比基、 嗎啉基、四唑基、咄啶基、呋喃基、噚唑基、。无烯基、 二羥噚二唑基、苯并間二氧雜還戊烯基、吲哚基、噻嗤 基、苯甲醯、苯并咪唑基、噻二唑基、異噻唑基、吼α各 基、四氫苯噻吩基(==環己噻吩基)、二苯并噻吼基、二氫 苯并噻吼基、仙基、二苯并二羥喹啉基、二苯并噻吩基、 C3〜Cs環烧基、C3〜Cg環婦基、亞σ塞唾琳基甲基、亞嘆嗤 啉基曱基、-CH=NR6、-N=C(R7)R8 ; R5、R51、R53、R54及 R55 為氫; r6為羥基、脲基、以苯基取代之脲基、硫脲基、以 笨基取代之硫脲基; R7&R8分別為苯基; η為1或2 ; Ζ為-S〇2-或-C0-, m為0或1 ; 本紙張尺度適用中國國家標準(CMS) A4規格(210X297公釐) -240- 513422 A B c D 六、申請專利範圍 於此等定義中,取代基為硝基、(^〜(^烷氧基、氨磺 醯基、胺基、以Cl〜C6烧基取之胺基、Cl〜C6烧基經基、 甲醯基、烧基羥基氧基、羥基、鹵素、(^〜(:6院基、 C2〜C:6炔基、羰基、(^〜(:6烧基氧基羰基、甲續酿氧基、 氰基、C2〜C6烯氧基、三氟甲基、(^〜(^烧硫基、-N=PPh3、 氧基、硫基、苯基、以氰基取代之苯基。 2·如申請專利範圍第1項之用以作為前列腺素D2(Pgd2^ 抗劑之醫藥組成物,於有效成分以式(I)所示的雙環之環 系胺基衍生物中, 0 乃表示 α m為0、Ζ為S〇2時,Χ^Χ2均為單鍵,χ3表示烷基、苯 基、萘基、苯乙烯基、喹啉基或噻吩甲基,此等之取代 基中,環狀者亦可被選自硝基、烷氧基、取代或非取代 胺基、_素、烷基及羥烷基中之1〜3個基所取代的雙環 之環系胺基衍生物或其鹽亦或水合物。 3·如申請專利範圍第i項之用以作為前列腺素〇2(1>(}£)2)括 抗劑之醫藥組成物,於有效成分為以式⑴所示的雙環之 環系胺基衍生物中,
    -241- 513422
    六、申請專利範圍 乃表不 α m為1時,Xi&X2均為單鍵,&為亦可被鹵素所取代之 苯基的雙環之環系胺基衍生物或其鹽亦或水合物。 4·如申請專利範圍第丨項之用以作為前列腺素D^pGD2)拮 抗劑之醫藥組成物,於有效成分乃以式⑴所示的雙環之 環系胺基衍生物中, · Q 乃表示 α m為1時’义丨為亞苯基,Xa-CH2-或-Ν=Ν· , &為苯基 的雙環之環系胺基衍生物或其鹽或水合物。 5·如申請專利範圍第1項之用以作為前列腺素D2(PGD2)拮 抗劑之醫藥組成物,係治療鼻塞之醫藥組成物。 6· —種雙環之環系胺基衍生物或其鹽或水合物,係以式 (la)所示,
    B (式中’a'b'r'x!、χ2&χ3乃與申請專利範圍第i 項之定義相同; 、申請專利範圍 但,(1瓜為單鍵、X2為單鍵、x^Ci〜C6烧基、取 代或非取代苯基或萘基; (2) X々單鍵、X2為-(CH2)n或-CH2CH2-、 炫基或芳基; (3) Χι為笨樓基、X2為單鍵、烧基; (4) Χ!為單鍵、X2為單鍵、&為σ比咬基時除外)。 7·如申請專利範圍第6項的雙環之環系胺基衍生物或其鹽 或水合物,Xi&X2為單鍵,X3為異噚唑基、噻嗔嗤基 、異噻唑基、嗎啉基、吲哚基、苯并呋喃基、二笨并呋 喃基、一本并二氧基、笨并σ塞吩基、二苯并11 塞吩基、吟 唑基、氧雜蒽基、酚三嗪基、二笨并哼σ比基、二苯并噻 0比基、二氮雜萘基、氧萘基、苯并咪唑基或二氫苯并噻 吡基、A、Β、R之定義同於申請專利範圍第1項。 8·如申請專利範圍第6項的雙環之環系胺基衍生物或其鹽 或水合物,义!為單鍵,X2為亞苯基、χ3為烯基、炔基 、-CH=NRA-N=C(R7)R8,a、Β、R、R6、rar8 乃與 申請專利範圍第1項之定義相同。 9·如申請專利範圍第6項的雙環之環系胺基衍生物或其鹽 或水合物,R表示COOR,乂1表示亞苯基或噻吩二基, x2表示單鍵、-N=N-、-CH=CH-、-CONH-、-NHCO-或 亞乙烯基,X3表示苯基、噻唑烷基甲基、噻唑嘻烷基甲 基或噻吩基,A、B、R!、R6、R7&r8乃與申請專利範 圍第1項之定義相同。 10· —種雙環之環系胺基衍生物或其鹽或水合物,係以式 513422 AB c D 六、申請專利範圍 (lb):
    係表示 CC 或 φ( A、B、R、Xi、X2及X3乃與申請專利範圍第1項之定義 相同;但,Xi&X2為單鍵,Xs為苯基時除外)所示。 11·如申請專利範圍第10項的雙環之環系胺基衍生物或其 鹽或水合物,於式(lb)所示之化合物中, 0 乃表不 α A、Β、R、X!、X2及X3乃與申請專利範圍第1項之定義 相同。 12·如申請專利範圍第11項的雙環之環系胺基衍生物或其 鹽或水合物,R為COORJRi乃與申請專利範圍第1項之 定義相同)。 本紙張尺度適用中國國家標準(CNS) A4規格(210X297公釐) -244- 513422 A B c D 六、申請專利範圍 13.如申請專利範圍第u項的雙環之環系胺基衍生物或其 鹽或水合物,X!為亞苯基或噻吩二基,χ2為單鍵、-N=N_ 、-CH-CH-,1,2-亞乙烯基、-〇-、-S-、-CO-、-CON(R55)-(R55乃與申請專利範圍第1項之定義相同)或 (RS1乃與申請專利範圍第丨項之定義相同) 及X3為苯基或σ塞吩基。 14·如申請專利範圍第1〇項的雙環之環系胺基衍生物或其 鹽或水合物,於式(lb)所示之化合物中, Q 乃表示 ¢( A、B、R、Xi、X2及X3乃與申請專利範圍第i項之定義 相同。 15. 如申請專利範圍第14項的雙環之環系胺基衍生物或其 鹽或水合物,B為氫,Xt&X2均為單鍵,χ3為噻吩甲基 、噻唑基、噻嗪唑基、異噻唑基、σ比咯基、σ比啶基、苯 并呋喃基、苯并咪唑基、苯并噻吩基、二苯并呋喃基、 二苯并噻吩基、喹啉基或吲哚基。 16. 如申請專利範圍第14項的雙環之環系胺基衍生物或其 鹽或水合物,Xi為亞苯基、噻吩二基、吲哚二基或哼唑 二基、X2為單鍵、-N=N-、-CH=CH-、1,2-亞乙烯基、 -S-、或- 0-、及X3為芳基或雜環。 本紙張尺度適用中國國家標準(CNS) A4規格(210X297公釐) -245- 8 8 8 8 A B c D 六、申請專利範圍 17.如申請專利範圍第1〇項的雙環之環系胺基衍生物或其 鹽或水合物,於式(lb)所示之化合物中, 0’ 乃表示 A為亦可具有氧基或不飽和鍵之烷撐基,b為氫,r為 CH2〇H或COOH,XAX2為單鍵,X3為取代或非取代之 本弁°塞吩基。 18· —種用以作為前列腺素D2(Pgd2)拮抗劑之醫藥組成物 ’其係含有申請專利範圍第6至17項中所載之化合物。 本紙張尺度適用中國國家標準(CNS) A4規格(210X297公釐) -246-
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