CN1140452A - 节肢动物杀虫剂四氢嘧啶 - Google Patents
节肢动物杀虫剂四氢嘧啶 Download PDFInfo
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- CN1140452A CN1140452A CN95191561.4A CN95191561A CN1140452A CN 1140452 A CN1140452 A CN 1140452A CN 95191561 A CN95191561 A CN 95191561A CN 1140452 A CN1140452 A CN 1140452A
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- 239000005052 trichlorosilane Substances 0.000 description 1
- DQJCHOQLCLEDLL-UHFFFAOYSA-N tricyclazole Chemical compound CC1=CC=CC2=C1N1C=NN=C1S2 DQJCHOQLCLEDLL-UHFFFAOYSA-N 0.000 description 1
- ITMCEJHCFYSIIV-UHFFFAOYSA-N triflic acid Chemical compound OS(=O)(=O)C(F)(F)F ITMCEJHCFYSIIV-UHFFFAOYSA-N 0.000 description 1
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- JARYYMUOCXVXNK-IMTORBKUSA-N validamycin Chemical compound N([C@H]1C[C@@H]([C@H]([C@H](O)[C@H]1O)O[C@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)CO)[C@H]1C=C(CO)[C@H](O)[C@H](O)[C@H]1O JARYYMUOCXVXNK-IMTORBKUSA-N 0.000 description 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
- 238000001238 wet grinding Methods 0.000 description 1
- CHNQZRKUZPNOOH-UHFFFAOYSA-J zinc;manganese(2+);n-[2-(sulfidocarbothioylamino)ethyl]carbamodithioate Chemical compound [Mn+2].[Zn+2].[S-]C(=S)NCCNC([S-])=S.[S-]C(=S)NCCNC([S-])=S CHNQZRKUZPNOOH-UHFFFAOYSA-J 0.000 description 1
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Abstract
节肢动物杀虫剂化合物,组合物和式(I)化合物的用途,其中X,A,R1,R2,R3,R4,R5和R6的定义如说明书所述。
Description
本发明涉及用作节肢动物杀虫剂的四氢嘧啶类化合物。U.S.4,831,036公开了杀虫剂四氢嘧啶,但不涉及本发明的内容。
发明概述
X选自硅或锗;
A选自C1-C20亚烷基,C2-C20亚链烯基,C2-C20亚炔基,C3-C8亚环烷基,C7-C10芳亚烷基和亚苯基,每个基团可由1-3个独立地选自W的取代基取代;或A是直接键。
R1和R3独立地选自H,C1-C10烷基,C2-C10链烯基或C2-C10炔基,每个基团任意地被独立地选自下列基团的1-2个取代基取代:卤素,CN,C(O)R7,C(S)R7,NO2,OH,SC(O)R7,SC(S)R7,OC(O)R7,OC(S)R7,NR8C(O)R7,NR8C(S)R7,SH,Si(R8)(R9)(R10),C1-C4烷氧基,C1-C4卤代烷氧基,C1-C4烷基硫基,C1-C4烷基氨基,C2-C8二烷基氨基,C3-C8环烷基和任意地被1-3个独立地选自W1的取代基取代的苯基;C3-C8环烷基,它们任意地被1-3个独立地选自卤素,C1-C2烷基和C1-C2的卤代烷基的取代基取代;C(O)R11;C(S)R11;任意地被1-3个独立地选自W1的取代基取代的苯基;通过碳或氮原子被5-或6-元芳环取代的C1-C3烷基,上述5-或6-元芳环含有独立地选自0-4个氮,0-1个氧,0-1个硫的1-4个杂原子,并且任意地被独立地选自W1的1-3个取代基取代;和一个通过碳或氮连接的,含有1至4个独立地选自0-4个氮,0-1个氧和0-1个硫杂原子的5元或6元芳环,该环任意地被1-3个独立地选自W1的取代基取代;
R2选自H,C1-C6的烷基,C1-C6的卤代烷基,C2-C6的链烯基,C2-C6的卤代链烯基,C2-C6的炔基,C2-C6的卤代炔基,C3-C7的环烷基,C3-C7的卤代环烷基和C4-C7的环烷基烷基,每个基团任意地被1-3个独立地选自W的取代基取代;或者R2和R3可被一起看作CH2CH2和CH2CH2CH2,每个基团任意地被1-2个甲基取代;
R4选自H和C3-C6三烷基甲硅烷基;或者R4选自C1-C10烷基,C2-C10链烯基,C2-C10炔基,C1-C10烷氧基,C1-C10烷硫基,苯基,苯氧基,苯硫基和萘基,每个基团任意地被1-3个选自W1的取代基取代;
R5和R6独立地选自C1-C10烷基,C1-C10链烯基,C2-C10炔基,C1-C10烷氧基,C1-C10烷硫基,苯基,苯氧基,苯硫基和萘基,每个基团任意地被1-3个选自W1的取代基取代;R5、R6亦可是OH和C3-C6三烷基甲硅烷基;
R7选自H,NH2,OH,C1-C6烷基和C1-C6卤代烷基,C1-C6烷氧基,C1-C6卤代烷氧基,C1-C6烷硫基,C1-C4烷基氨基,C2-C8二烷基氨基和任意地被1-3个独立地选自W1的取代基取代的苯基;
R8为H;或者R8选自C1-C10烷基,C2-C10链烯基,C2-C10炔基,C1-C10烷氧基,苯氧基,苯基和萘基,每个基团任意地被1-3个独立地选自W1的取代基取代;
R9和R10独立地选自C1-C10烷基,C2-C10链烯基,C2-C10炔基,C1-C10烷氧基,苯氧基,苯基和萘基,每个基团任意地被1-3个独立地选自W1的取代基取代;和OH;
R11选自H,NH2,OH,C1-C6烷基,C1-C6卤代烷基,C1-C6烷氧基,C1-C6卤代烷氧基,C1-C2烷硫基,C1-C4烷基氨基,C2-C8二烷基氨基和任意地被1-3个独立地选自W1的取代基取代的苯基;
W选自卤素,CN,NO2,OH,C1-C6烷基,C1-C6卤代烷基,C1-C6烷氧基和C1-C6卤代烷氧基;和
W1选自卤素,CN,NO2,C1-C2烷基,C1-C2卤代烷基,C1-C2烷氧基,C1-C2卤代烷氧基,C1-C2烷硫基,C1-C2卤代烷硫基,C1-C2烷基磺酰基,C1-C2卤代烷基磺酰基,C1-C4烷基氨基,C2-C8二烷基氨基和C3-C6三烷基甲硅烷基;
优选的化合物A是式I的化合物,其中:
A为C1-C6亚烷基;
R1是通过C或N连结的、含有1-4个独立地选自0-4个氮,0-1个氧和0-1个硫杂原子的5元或6元芳环取代的C1-C3烷基,该环任意地被1-3个独立地选自W1的取代基取代;
R4选自C1-C10烷基和苯基,每个基团任意地被1-3个独立地选自W1的取代基取代;
R5和R6独立地选自C1-C10烷基和苯基,每个基团任意地被1-3个独立地选自W1的取代基取代;
W1选自卤素和C1-C2卤代烷基。
优选的化合物B是优选的A化合物,其中:
X为硅;
R1是被吡啶基、噻唑或异噁唑取代的CH2,该环任意地被1-2个卤素或1-2个甲基取代;
R2和R3一起被看作CH2CH2或CH2CH2CH2,每个基团任意地被1-2个CH3取代;和
R4、R5和R6独立地选自C1-C3烷基,C1-C3烷氧基和苯基。
优选的化合物C是优选的A化合物,其中
X为硅;
R1是被吡啶基、噻唑或异噁唑取代的CH2,该环任意地被1-2个卤素取代;
R2选自H和C1-C3烷基,和
R4、R5和R6独立地选自C1-C3烷基,C1-C3烷氧基和苯基。
特别优选的有生物活性的化合物是优选的B中的化合物D:
1-[(6-氯-3-吡啶基)甲基]-1,2,3,5,6,7-六氢-2-甲基-8-硝基-6-[(三甲基甲硅烷基)甲基]咪唑并[1,2-c]嘧啶;
特别优选的有生物活性的化合物是优选的B中的化合物E:
1-[(6-氯-3-吡啶基)甲基]-1,2,3,5,6,7-六氢-8-硝基-6-[(三甲基甲硅烷基)甲基]咪唑并[1,2-c]嘧啶。
本发明的化合物可以以一种或多种立体异构体存在。各种立体异构体包括对映体、非对映异构体和几何异构体。本领域中的技术人员将会理解:一种立体异构体当将它与其它种立体异构体分离或是相对富集时可能更具活性和/或展现出良好的效果。另外,本领域的技术人员懂得怎样分离所说的立体异构体。因此,本发明包括外消旋混合物,单一异构体,和具有光学活性的式I的化合物及其农业上适合的盐类的混合物。
术语:“五元或六元芳环”定义为那些符合Huckel规则的环;例子包括含有0-4个杂原子的5元或6元单环芳环,比如苯基、呋喃基、呋咱基、噻吩基、吡咯基、吡唑基、噁唑基、噁二唑基、咪唑基、异噁唑基、噻唑基、噻二唑基、异噻唑基、四唑基、吡啶基、嘧啶基、哒嗪基、吡嗪基和三嗪基,它们通过任何合适的碳或氮连接。例如,当芳环为呋喃基时,它可以是2-呋喃基或3-呋喃基,对于吡咯基,芳环可以是1-吡咯基,2-吡咯基或3-吡咯基,对于吡啶基,芳环是2-吡啶基,3-吡啶基或4-吡啶基,其它的单环芳环相似。
在以上叙述中,单独使用的术语“烷基”或在复合词比如“烷基硫基”或“卤代烷基”中使用的术语“烷基”指直链或支链烷基,比如甲基、乙基、正丙基、异丙基或直到C10的各种异构体。亚烷基的例子包括CH2、CH2CH2、CH2CH2CH2和直到C20的各种异构体。“链烯基”指直链或支链的烯烃,比如甲乙烯基、1-丙烯基、2-丙烯基以及直到C10的各种异构体。“链烯基”也指多烯,比如1,3-己二烯。“亚链烯基”的例子包括CH=CH,CH2CH=CH,CH=CHCH2和直到C20的各种异构体。“炔基”指直链或支链的炔,比如乙炔基,1-丙炔基,3-丙炔基和直到C10的各种异构体。“亚炔基”的例子包括C≡C,CH2C=C,C≡CCH2和直到C20的各种异构体。“烷氧基”指,例如甲氧基、乙氧基、正丙氧基、异丙氧基和直到C10的各种异构体。“烷基硫基”指直链或支链烷基硫基部分,如甲基硫基、乙基硫基、以及不同的丙基硫基、丁基硫基、戊基硫基和己基硫基的异构体。“烷基磺酰基”指CH3S(O)2和CH3CH2S(O)2。“烷基氨基”指甲氨基、乙氨基、正丙氨基、异丙氨基及各种丁氨基异构体。“二烷基氨基”是指N原子上取代有两上可能不同的烷基基团。例子包括N,N-二甲基氨基和N-乙基-N-甲基氨基。“环烷基”指,例如环丙基、环丁基、环戊基、环己基、环庚基和环辛基。“环烷基烷基”的例子包括:环丙烷基甲基、环丙基乙基、环丁基甲基,以及连接到直链或支链烷基基团上的各种C6和C7异构体。单独或在象“卤代烷基”这样的复合词中使用的术语“卤素”是指F、Cl、Br或I。此外,在复合词比如“卤代烷基”中使用时,所说的烷基可能被相同或不同的卤素原子部分或全部取代。“卤代烷基”的例子包括F3C、ClCH2、CF3CH2和CF3CH2。“卤代链烯基”的例子包括(Cl)2C=CCH2和CF3CH2CH=CHCH2。“卤代炔基”的例子包括HC≡CCHCl,CF3C≡C、CCl3C≡C和FCH2C≡CCH2。“卤代烷氧基”的例子包括CF3O、CCl3CH2O、CF2HCH2CHO和CF3CH2O。“卤代烷基硫基”的例子包括CCl3S、CF3S以及CCl3CH2S。“卤代烷基磺酰基”的例子包括CF3SO2、CCl3SO2、CF3CH2SO2和CF3CF2SO2。取代基团中碳原子总数由“Ci-Cj”词头表明,其中i和j是从1到20的数。例如,C1-C20亚烷基指亚甲基、正乙烯和丙烯,直到十二碳烯的异构体;C2烷氧基指CH3CH2O-;和C3烷氧基指CH3CH2CH2O-或者(CH3)2CHO-。
发明的详细内容
式I的化合物可以由化合物II和等当量或过量的胺化合物III和至少两倍摩尔量的甲醛在合适的溶剂中由历程1制得。这些反应是典型地在0℃到溶剂的回流温度范围内进行的,优选的温度为0~25℃。历程1的反应一般可以在一天内反应完全,然而某些反应可能要求更长的时间(甚至5天)。合适的溶剂包括醇类,如:甲醇、乙醇、水,和极性非质子溶剂如四氢呋喃和二甲基甲酰胺。甲醛的用量为2-10摩尔量。固体的多聚甲醛或甲醛水溶液均可使用。在某些实例中,使用少量的强的非氧化性酸做为催化剂是比较理想的,比如HCl。另外,也可以用胺化合物III的氢卤酸盐或硫酸氢盐。
历程1
化合物II可以由化合物IV和胺V如历程2所示反应得到。一般的,在0-100℃温度范围内,于合适的溶剂中使化合物IV和1-20摩尔量的胺V反应。历程2中一般要6-48小时反应完全,然而有时也需要更长的时间。合适的溶剂包括但并不限定于,醇类如甲醇、乙醇和异丙醇;水;乙腈;二甲酰胺和二甲基乙酰胺。式V的胺可使用它的盐酸盐;此时反应中要加入等摩尔量的碱(如NaOH)到反应混合物中。
历程2
X1=合适的离去基团如卤素,SCH3或OC6H5。
另外,化合物II可以由化合物VI和式VII的胺通过历程3在同历程2完全类似的条件下反应制得。
化合物IV可由本领域公知的工艺采用硝基乙烯VIII和式VII的胺反应制备(反应历程4)。化合物VI可通过与化合物IV完全相类似的步骤制得。典型的反应条件是使等摩尔量的化合物VII和VIII是在合适的溶剂或混合溶剂中,于温度范围0-100℃下进行反应。历程4反应完全一般要6到48小时。适宜的溶剂一般要对化合物VII、VIII的溶液有足够的极性效应。包括醇类如甲醇、乙醇、异丙醇;醚类如二乙醚、四氢呋喃和二噁烷;酯类如醋酸乙酯;极性非质子溶剂如二甲基甲酰胺和二甲基乙酰胺;水及溶剂混合物。
历程4
此外,化合物I可以由历程5在与历程2完全类似的条件下由四氢嘧啶IX或胺VII反应制得。当R1或R2为H时历程5中制化合物I反应很方便。
化合物IX可由化合物VI和胺III如历程6所示在与历程1类似的条件下,在甲醛存在下反应制得。
此外,如历程7所示,化合物I(R1不是H)可由化合物I(R1为H)和烷基化试剂X在质子接受体存在下,于适宜的溶剂中反应得到。一般的质子接受体包括NaH、KH、K2CO3、NaHCO3、Cs2CO3,适宜的溶剂为DMF、THF,乙腈和水。有时,历程7在相转移情况下进行,所用溶剂有甲苯、二氯甲烷、二氯乙烷、乙醚、正己烷、苯等,以及碱的水溶液,包括NaOH、KOH、NaHCO3、Na2CO3、K2CO3。典型的相转移催化剂是四取代的卤化铵盐,如:四丁基碘化铵,苄基三乙基溴化铵等等。反应一般在20-150℃下反应1小时到三天可进行完全,然而优选时间为6-24小时。
R1=H,X2是适宜的离去基团如:卤素、甲苯磺酸盐、甲基磺酸盐、三氟甲基磺酸盐。
另外,化合物I(其中R3不是H)可以在同历程7完全类似的条件下经历程8制得。
历程9 X2为适宜的离去基团;
R1是H
B为R2和R3一起形成的五或六元环。
此外,化合物II(R2和R3连结成五或六元环)可如历程10制得。通常是等摩尔量的XII和XIII化合物在适宜的溶剂或混合溶剂中,于0-100℃条件下反应2-48小时。适宜的溶剂通常对XII和XIII的化合物的溶液有足够的极性,这些溶剂包括:醇类如甲醇、乙醇和异丙醇;醚,如二乙醚,四氢呋喃和二噁烷;酯如乙酸乙酯;极性非质子溶剂如二甲基甲酰胺、二甲基乙酰胺;水以及混合溶剂有足够的极化作用。
历程10
B为R2和R3相连, X1为一种适宜的离去基团。
二胺XII可用化合物X与过量的胺XIII反应如历程11所示制备。通常反应用1.5-10倍当量的XIII,在溶剂中进行,溶剂如:甲醇、乙醇、异丙醇、THF、水、乙腈以及其它。历程11的反应有时可在无溶剂的条件下进行。一般反应时间由30分钟到几天,通常优选6到24小时。
X2为一种合适的离去基团,B为R2和R3相连。
另外,二胺VII,其中B为任意取代的CH2CH2基团,可由历程12由两步法制得。第i)步中,胺XIV用KCN和化合物XV处理,在0到3倍当量酸存在下生成化合物XVI氨基氰化物。本领域的技术人员可认识到,化合物XV可以是甲醛、乙醛或丙酮。本方法中可以使用其它氰化物盐以及HCN,也可用XIV的卤化氢盐及其它酸的盐。适宜的溶剂有甲醇、乙醇、异丙醇和水,也包括混合溶剂。历程12的反应通常在24小时内即可进行完全。另外,制备氨基腈(如:化合物XVI)的方法可在以前的文献中找到(例如参见Synth.Commun.,(1985),15,157;Synthesis(1979),127)。
在历程12的ii)步中,氨基腈XVI被还原生成二胺XII。本还原反应通常用氢化铝锂或甲硼烷,加入量为0.75到3.0摩尔当量,溶剂为二乙醚或THF。反应温度范围由-20℃到溶剂的回流温度,时间从0.5小时到两天。此外,由化合物XVI到化合物XII的还原反应可采用催化氢化,催化剂用钯/炭或雷内镍,氢化还原反应中加入氨对于增大二胺XII的产率有时是有用的。
历程12 步骤i R12和R13独立地是H或CH3。步骤ii R12和R13独立地是H或CH3。
历程13中描绘了另一B为CH2CH2基团的二胺的制备方法。历程13的第i)步中,氨基酰胺XVII用1到2摩尔当量的酰氯XVIII处理,反应在1到3摩尔当量碱存在下进行,如:NaOH、KOH、K2CO3、NaHCO3、吡啶、三乙胺。适宜的溶剂有THF、CH2Cl2、水和吡啶。产品(化合物XIX)可萃取分离,或更方便如用移去溶剂的方法,并且以粗产品形式用作第ii)步的原料。酰胺XVII可以用中性或用盐的形式(通常是盐酸盐或CF3CO2H的盐)。当采用化合物XVII盐的形式时,则历程13的第i)步中要加入另一当量的碱。
在历程13的第ii)步中,酰胺XIX用还原剂如:LiAlH4、BH3·THF或BH3·SMe2处理可转化成二胺XII,反应在溶剂THF或Et2O中进行,温度范围由0℃到溶剂的回流温度。一般反应时间为0.5h到两天。类似的过程在以前文献中众所周知。(参见例如Synthesis,(1981),441)。
当R12为CH3,R13为H时,化合物XVII是丙氨酸酰胺。不管是用式XVII丙氨酸酰胺的D式或L式或其盐类都可以方便地得到二胺XII的富集的对映体。当化合物II由化合物XII的富集对映体经历程10制备时,得到的化合物II是富集对映体。用化合物II的富集对映体制备化合物I,经历程1得到化合物I的富集对映体。
历程13
R14为CH3SCH2,3-吡啶基,5-噻唑基,6-氯-3-吡啶基,2-氯-5-噻唑基或5,6-二氯-3-吡啶基。
另外,二胺XII通过对映体酸拆分可得到富集对映体,对映体酸如酒石酸。这种拆分对于本领域技术人员来说都知道。
胺III可以由历程14制得,即用如式XX所示的卤化硅或卤化锗同过量的氨反应。这些转化反应通常将化合物XX加入到无水的液氨中,(液氨为2-100当量)温度由-78-100℃。一旦要求温度高于-33℃,反应需在密封,高压装置中进行。一般反应中不用溶剂,有时会使用THF或二乙醚做溶剂。反应完全的时间一般是0.5-72小时。一般的处理步骤是蒸除过量的氨,可以加入醚沉淀卤化铵,然后将溶剂分去。本领域的技术人员都知道还有许多其它的方法可以将XX的卤化物转变成伯胺III。各种工艺的参考文献可在March,Adv.,Org.Chem.,4th Ed.,pp 1276-7中找到。历程14
X2是合适的离去基团
如式XX的硅烷和锗烷可如历程15所示制备,用式XXI的有机锂或格立尼雅试剂与氯硅烷或氯锗烷XXII反应。反应中通常加入等摩尔量的XXI和XXII的混合物,在有机溶剂如:戊烷、正己烷、THF、醚中进行。反应温度由-78-25℃,时间通常是2小时到四天。
M为Li、MgCl、MgBr、MgI
X2为一种适宜的离去基团。
式XXII的氯硅烷和氯锗烷可用二氯化物XXIII和等摩尔量的式XXIV的有机金属试剂反应制得,反应式如历程16所示。历程16的反应条件与历程15的条件类似。制备其中R4和R5相同的化合物XX可在历程16中用两倍当量的化合物XXIV。
X2是合适的离去基团,M是Li、MgCl、MgBr或MgI。
R4、R5和R6为同一基团的化合物XX可用化合物XXV的三氯化物同三倍当量的式XXIV的有机金属化合物如历程17所示反应制得。历程17的反应条件同历程15类似。
X2是合适的离去基团,M是Li、MgCl、MgBr或MgI。
R4为烷氧基或苯氧基的化合物XX的制备如历程18所示,采用式XXVI所示的醇或苯酚与式XXII所示的氯硅烷或氯锗烷在碱的存在下反应,碱有三乙胺,吡啶或NaH。
历程18
R15=C1-C10的烷基或苯基
本领域的技术人员对于醚XX(R4是烷氧基或苯氧基)的合成工艺是熟悉的(参见例如Org.Synth.,69,96,J.Chem.Soc.Chem.Commun(1988)802;J.Organomet.Chem.,(1970),22,599)。
R4、R5为烷氧基或苯氧基的式XX所示的硅烷或锗烷可用二氯化物XXIII与两倍当量的醇XXVI在碱的存在下反应制备,步骤同历程18类似。相类似的,其中R4、R5和R6为烷氧基或苯氧基的化合物XX可用式为XXV的三氯硅烷或三氯锗烷与三倍当量的醇XXVI在碱存在下反应制备,步骤同历程18的反应类似。
本领域的技术人员会认识到,制备化合物XX、XXII、XXIII和XXV的各种方法是本领域公知的。关于硅烷的主要参考文献包括如下:例如Fleming,I.,Organosilicon Chemstry,in Comprehensive OrganicChemistry(1979),3,541;Colvin,E.,Silicon in Organic SynthesisButterworths,Boston(1981)及Pawlenko,S.,Organosilicon Chemistry;Watter de Cruyter,New York(1986)有关锗烷的主要文献包括:
例如Riviere,P.,et al.,Cermanium,In Comprehesive Organo-metallic Chemistry(1982),2,399;Lesbre,M,et al.,The OrganicCompounds of Germanium,Wiley,London(1971)。
应该认识到:上面描述的制备化合物I的一些试剂和反应条件对于中间体中的某些官能团来说是不合适的。在这些情况中,加入保护和去保护工序在合成中将有助于得到目的产物。保护基团的使用和选择对于化学合成领域中的技术人员是明显的。
实施例1步骤A:甲基N-[(6-氯-3-吡啶基)羰基]丙氨酸
在60g(0.43mol)DL-丙氨酸甲酯盐酸盐和290ml碳酸氢钠饱和水溶液中加入50.5g(0.29mol)6-氯烟酰氯和290ml CH2Cl2溶液。然后加入5ml季铵氯化物336(Aldrich),两相混合物在25℃下快速搅拌24小时。最后的混合物在CH2Cl2和饱和NaHCO3之间分配。水层用CH2Cl2萃取三次。生成的有机物用饱和NaHCO3洗两次,MgSO4干燥,浓缩得到56.1g标题化合物,为粘稠黄色油状物。1H NMR(300MHz,CDCl3)δ8.82(d,J=2.4Hz,1H),8.10(dd,1H),7.41(d,1H),7.10(br,1H),4.78(quintet,1H),3.80(s,3H),1.53(d,3H)。步骤B:6-氯-N-[1-(氨酰基)-乙基]-3-吡啶甲酰胺。
步骤A中产品50.5g(0.21mol)和150mL无水甲醇,加入575mL15%无水的氨的无水甲醇溶液中。溶液在室温下搅拌48小时。过滤得到固体产品,乙醇洗涤,真空干燥,得到43.5g的白色固体标题产物:mp.>220℃。1H NMR(400MHz,(CH3)2,SO-d6)δ8.87(apparent,s,1H),8.79(d,1H),8.29(d,1H),7.65(d,1H),7.45(brs,1H),7.03(brs,1H),4.41(quintet,1H),1.33(d,3H)。步骤C:N2-[(6-氯-3-吡啶基)-甲基]-1,2-丙二胺
甲硼烷-甲基硫配合物(18.7mL,0.19mol)滴加到机械搅拌下的8.5g(0.04mol)步骤B的产物和112mL THF的混合物中,温度50-60℃。所得的桔黄色的悬浮液回流2小时,冷到室温,小心加入62mL 6NHCl停止反应。得到的浅黄色混合物室温下搅拌24小时,然后用三份的乙醚洗涤。水层用25mL 50%的NaOH(加入时冷却)调至碱性,用3×150ml 2∶1的二氯甲烷-氯仿溶液萃取。得到的有机层干燥(用K2CO3),浓缩得到3.5g黄色油状的标题产物。1H NMR(400MHz,CDCl3)δ8.33(apparent,s,1H),7.69(d,1H),7.30(d,1H),3.78(ABq,2H),2.75(d,1H),2.63(dd,1H),2.53(dd,1H),Ca.1.50(brs,3H),1.07(d,3H)。步骤D:2-氯-5-[[5-甲基-2-(硝基亚甲基)-1-咪唑烷基]甲基]吡啶
2.5g(0.013mol)步骤C的产品,1.6g(0.009mol)1,1-二(甲硫基)-2-硝基乙烯和63mL无水乙醇的悬浮液加热回流3小时,然后在24℃保持72小时。使所得混合物浓缩,用硅胶色谱层析,淋洗液为15∶1∶0.1的二氯乙烷∶乙醇∶30%氨水,得到0.7g黄色固态的标题产物;mp,127-131℃。1H NMR(400MHz,CDCl3)δ8.70(brs,1H),8.27(s,1H),7.56(d,1H),7.35(d,1H),6.56(s,1H),4.33(ABq,2H),3.95-3.85(m,2H),3.45-3,35(m,1H),1.33(d,3H)。步骤E:1-[(6-氯-3-吡啶基)甲基]-1,2,3,5,6,7-六氢-2-甲基-8-硝基-6-[(三甲基甲硅烷基)甲基]咪唑并[1,2 c]嘧啶(化合物1)
0.5g(1.9mmol)步骤D的产品,0.31mL(4.1mmol)37%的甲醛,0.21g(2.1mmol)三甲基甲硅烷基甲基胺,4mL乙醇的混合物,室温下搅拌18小时。使所得混合物浓缩,黄色的剩余物用二乙醚研磨,然后过滤得0.32g黄色固体标题产物;mp,112-115℃。1H NMR(300MHz,CDCl3)δ8.30(s,1H),7.81(d,1H),7.30(d,1H),5.04(1/2ABq,1H),3.98-3.68(m,6H),3.23(dd,1H),1.94(s,2H),1,26(d,3H),0.08(s,9H)。
实施例2步骤A:2-硝基亚甲基-咪唑啉
1,1-二(甲硫基)-2-硝基乙烯125g(0.76mol),乙二胺(50.6mL,0.76mol),乙醇757mL的悬浮液加热回流4小时。所得混合物冷却至5℃过滤。固体用冷的乙醇冲涤,真空干燥,得102.5g棕褐色固体。1H NMR(200MHz,Me2SO-d6)δ8.27(br,s,2H),6.33(s,1H),3.58(s,4H)。步骤B:1,2,3,5,6,7-六氢-8-硝基-6-[(三甲基甲硅烷基)甲基]-咪唑并[1,2-c]嘧啶
步骤A所得产品0.98g(7.6mmol),1.26mL(16.7mmol)37%的甲醛,15mL乙醇和1.11mL(8.3mmol)三甲基甲硅烷基甲基胺室温下反应。18小时后,将反应液浓缩得1.85g黄色固体。1H NMR(400MHz,CDCl3)δ8.33(br s,1H),4.00(s,2H),3.80(overlapping t,2H and s,2H),3.66(t,2H),2.14(s,2H),0.10(s,9H)。步骤C:1-[(6-氯-3-吡啶基)甲基]-1,2,3,5,6,7-六氢-8-硝基-6-[(三甲基甲硅烷基)甲基]-咪唑并[1,2-c]嘧啶
步骤B中产品0.5g(2.0mmol),0.8g(3.9mmol)6-氯-3-氯甲基吡啶盐酸盐,0.004g(0.1mmol)四正丁基碘化铵,6.4mL 50%KOH水溶液,8.4mL二氯甲烷混合后剧烈搅拌24小时。反应混合物倾入水中用3份二氯甲烷萃取。合并的有机层用饱和的NaHCO3水溶液洗涤,K2CO3干燥,然后浓缩。粗产品用二乙醚研磨,过滤,得到0.34g黄色固体标题产物。mp:145.5-147.0℃。1H NMR(400MHz,CDCl3)δ8.35(d,1H),7.90(dd,1H),7.33(d,1H),4.86(s,2H),3.90(s,2H),3.77(s,2H),3.68-3.55(m,4H),2.02(s,2H),0.10(s,9H)。
用上面所述的一般方法,或其显见的改进方法,表1-16和索引表A-D中的化合物可以被制得。表1中化合物,第1行为1-1,1-2,1-3和1-4(标出行和列)。表中所有其它化合物均以此类似规则标出。在表1-16和附表A-D中采用以下的记号:
表1 R1=
栏 | ||||
1 | 2 | 3 | 4 | |
123456 | HMeEtn-Pri-Prn-Bu | PhCH2Ph2-Cl-Ph3-Cl-Ph4-Cl-PhCH2(c-Pr) | 2-CH2-5-CF3-噻吩基NCCH2CH2AcNHCH2AcNHCH2CH2CH2NMe3ICH2CH2NMe3I | CH2(3,4-di-Cl-Ph)2-CH2-6-Cl-pyr3-CH2-6-Cl-pyr4-CH2-6-Cl-pyr2-CH2-5-Cl-pyr2-CH2-4-Cl-pyr |
789101112131415161718192021222324252627282930313233343536 | s-Bui-Buc-PrHCCCH2NCCH22-pyr3-pyr4-pyrAcSCH2Et2NCH2c-Bu环戊基环己基6-F-2-pyr6-Me-3-pyr6-Br-3-pyr6-F-3-pyr6-OMe-3-pyr6-Me-2-pyr6-Br-2-pyr5-Cl-2-pyr5-Me-2-pyr5-Br-2-pyr5-F-2-pyr6-OMe-2-pyr2-噻二唑基MeSCH26-Cl-2-pyr6-Cl-3-pyr6-Cl-4-pyr | 2-CH2-pyr3-CH2-pyr4-CH2-pyr5-CH2-异噁唑基Me2NCH2CH2(c-Bu)CH2(环戊基)CH2(环己基5-CH2-2-Me-噻唑基5-CH2-2-Br-噻唑基2-CH2-5-Me-噻吩基3-CH2-吡唑基4-CH2-吡唑基5-CH2-吡唑基2-CH2-5-Cl-噻吩基2-CH2-5-Me-噻吩基3-CH2-6-Me-pyr3-CH2-6-OMe-pyr3-CH2-6-Br-pyr2-CH2-6-CF3-pyr3-CH2-6-F-pyr3-CH2-6-CF3-pyr3-CH2-6-OCF3-pyr2-CH2-6-Me-pyr2-CH2-6-OMe-pyr2-CH2-6-Br-pyr2-CH2-6-F-pyr5-CH2-嘧啶基2-CH2-嘧啶基 | CH2(2-Cl-Ph)CH2(3-Cl-Ph)CH2(4-Cl-Ph)CH2C(Me)CH2HCCCH2CH2CH2CHCH2MeSCH2CH2AcSCH2CH22-CH2-呋喃基5,6-di-Cl-3-pyr5-OMe-2-pyr2-CH2-吡咯基3-CH2-吡咯基3-CH2-1-Me-吡唑基4-CH2-1-Me-吡唑基5-CH2-1-Me-吡唑基2-CH2-吡嗪基2-CH2-3-Me-吡嗪基2-CH2-5-Me-吡嗪基2-CH2-6-Me-吡嗪基3-CH2-哒嗪基3-CH2-6-Me-哒嗪基3-CH2-6-Cl-哒嗪基4-CH2-嘧啶基5-CH2-2-Me-嘧啶基2-CH2-5-CF3-噻二嗪基2-CH2-5-Br-噻吩基5-CH2-3-Me-异噁唑基5-CH2-3-F-异噁唑基 | 2-CH2-3-Cl-pyr2-CH2-5,6-di-Cl-pyr3-CH2-5-Cl-pyr3-CH2-4-Cl-pyr3-CH2-2-Cl-pyr3-CH2-5,6-di-Cl-pyr4-CH2-2,6-di-Cl-pyr5-CH2-2-Cl-噻唑基CH2CHCH2CH2CH2C(Me)CH2CH2CH3CHCHCH2CH3CHCHCH2CH2Et2NCH2CH2Me2NCH2CH22-CH2-1-Me-吡咯基3-CH2-1-Me-吡咯基5-CH2-噻唑基2-CH2-噻吩基5-CH2-2-Cl-嘧啶基2-CH2-5-Cl-吡嗪基2-CH2-6-OCF3-pyr2-CH2-噻二嗪基5-Me-2-噻二嗪基5-Cl-2-噻二嗪基5-CF2-2-噻二嗪基2-CH2-5-Me-噻二嗪基2-CH2-5-Cl-噻二嗪基5-CH2-3-Cl-异噁唑基5-CH2-3-Br-异噁唑基 |
表2 R1=
栏 | ||||
1 | 2 | 3 | 4 | |
3738394041424344454647484950515253545556575859606162636465 | HMeEtn-Pri-Prn-Bus-Bui-Buc-PrHCCCH2NCCH22-pyr3-pyr4-pyrAcSCH2Et2NCH2c-Bu环戊基环己基6-F-2-pyr6-Me-3-pyr6-Br-3-pyr6-F-3-pyr6-OMe-3-pyr6-Me-2-pyr6-Br-2-pyr5-Cl-2-pyr5-Me-2-pyr5-Br-2-pyr | PhCH2Ph2-Cl-Ph3-Cl-Ph4-Cl-PhCH2(c-Pr)2-CH2-pyr3-CH2-pyr4-CH2-pyr5-CH2-异噁唑基Me2NCH2CH2(c-Bu)CH2(环戊基)CH2(环己基)5-CH2-2-Me-噻唑基5-CH2-2-Br-噻唑基2-CH2-5-Me-噻吩基3-CH2-吡唑基4-CH2-吡唑基5-CH2-吡唑基2-CH2-5-Cl-噻吩基2-CH2-5-Me-噻吩基3-CH2-6-Me-pyr3-CH2-6-OMe-pyr3-CH2-6-Br-pyr2-CH2-6-CF3-pyr3-CH2-6-F-pyr3-CH2-6-CF3-pyr3-CH2-6-OCF3-pyr | 2-CH2-5-CF3-噻吩基NCCH2CH2AcNHCH2AcNHCH2CH2CH2NMe3ICH2CH2NMe3ICH2(2-Cl-Ph)CH2(3-Cl-Ph)CH2(4-Cl-Ph)CH2C(Me)CH2HCCCH2CH2CH2CHCH2MeSCH2CH2AcSCH2CH22-CH2-呋喃基5,6-di-Cl-3-pyr5-OMe-2-pyr2-CH2-吡咯基3-CH2-吡咯基3-CH2-1-Me-吡唑基4-CH2-1-Me-吡唑基5-CH2-1-Me-吡唑基2-CH2-吡嗪基2-CH2-3-Me-吡嗪基2-CH2-5-Me-吡嗪基2-CH2-6-Me-吡嗪基3-CH2-哒嗪基3-CH2-6-Me-哒嗪基3-CH2-6-Cl-哒嗪基 | CH2(3,4-di-Cl-Ph)2-CH2-6-Cl-pyr3-CH2-6-Cl-pyr4-CH2-6-Cl-pyr2-CH2-5-Cl-pyr2-CH2-4-Cl-pyr2-CH2-3-Cl-pyr2-CH2-5,6-di-Cl-pyr3-CH2-5-Cl-pyr3-CH2-4-Cl-pyr3-CH2-2-Cl-pyr3-CH2-5,6-di-Cl-pyr4-CH2-2,6-di-Cl-pyr5-CH2-2-Cl-噻唑基CH2CHCH2CH2CH2C(Me)CH2CH2CH3CHCHCH2CH3CHCHCH2CH2Et2NCH2CH2Me2NCH2CH22-CH2-1-Me-吡咯基3-CH2-1-Me-吡咯基5-CH2-噻唑基2-CH2-噻吩基5-CH2-2-Cl-嘧啶基2-CH2-5-Cl-吡嗪基2-CH2-6-OCF3-pyr2-CH2-噻二嗪基5-Me-2-噻二嗪基 |
66676869707172 | 5-F-2-pyr6-OMe-2-pyr2-噻二唑基MeSCH26-Cl-2-pyr6-Cl-3-pyr6-Cl-4-pyr | 2-CH2-6-Me-pyr2-CH2-6-OMe-pyr2-CH2-6-Br-pyr2-CH2-6-F-pyr5-CH2-嘧啶基2-CH2-嘧啶基 | 4-CH2-嘧啶基5-CH2-2-Me-嘧啶基2-CH2-5-CF3-噻二嗪基2-CH2-5-Br-噻吩基5-CH2-3-Me-异噁唑基5-CH2-3-F-异噁唑基 | 5-Cl-2-噻二嗪基5-CF2-2-噻二嗪基2-CH2-5-Me-噻二嗪基2-CH2-5-Cl-噻二嗪基5-CH2-3-Cl-异噁唑基5-CH2-3-Br-异噁唑基 |
表3 R1=
栏 | ||||
1 | 2 | 3 | 4 | |
737475767778798081828384858687888990919293 | HMeErn-Pri-Prn-Bus-Bui-Buc-PrHCCCH2NCCH22-pyr3-pyr4-pyrAcSCH2Et2NCH2c-Bu环戊基环己基6-F-2-pyr6-Me-3-pyr | PhCH2Ph2-Cl-Ph3-Cl-Ph4-Cl-PhCH2(c-Pr)2-CH2-pyr3-CH2-pyr4-CH2-pyr5-CH2-异噁唑基Me2NCH2CH2(c-Bu)CH2(环戊基)CH2(环己基)5-CH2-2-Me-噻唑基5-CH2-2-Br-噻唑基2-CH2-5-Me-噻吩基3-CH2-吡唑基4-CH2-吡唑基5-CH2-吡唑基2-CH2-5-Cl-噻吩基 | 2-CH2-5-CF3-噻吩基NCCH2CH2AcNHCH2AcNHCH2CH2CH2NMe3ICH2CH2NMe3ICH2(2-Cl-Ph)CH2(3-Cl-Ph)CH2(4-Cl-Ph)CH2C(Me)CH2HCCCH2CH2CH2CHCH2MeSCH2CH2AcSCH2CH22-CH2-呋喃基5,6-di-Cl-3-pyr5-OMe-2-pyr2-CH2-吡咯基3-CH2-吡咯基3-CH2-1-Me-吡唑基4-CH2-1-Me-吡唑基 | CH2(3,4-di-Cl-Ph)2-CH2-6-Cl-pyr3-CH2-6-Cl-pyr4-CH2-6-Cl-pyr2-CH2-5-Cl-pyr2-CH2-4-Cl-pyr2-CH2-3-Cl-pyr2-CH2-5,6-di-Cl-pyr3-CH2-5-Cl-pyr3-CH2-4-Cl-pyr3-CH2-2-Cl-pyr3-CH2-5,6-di-Cl-pyr4-CH2-2,6-di-Cl-pyr5-CH2-2-Cl-噻唑基CH2CHCH2CH2CH2C(Me)CH2CH2CH3CHCHCH2CH3CHCHCH2CH2Et2NCH2CH2Me2NCH2CH22-CH2-1-Me-吡咯基 |
949596979899100101102103104105106107108 | 6-Br-3-pyr6-F-3-pyr6-OMe-3-pyr6-Me-2-pyr6-Br-2-pyr5-Cl-2-pyr5-Me-2-pyr5-Br-2-pyr5-F-2-pyr6-OMe-2-pyr2-噻二唑基MeSCH26-Cl-2-pyr6-Cl-3-pyr6-Cl-4-pyr | 2-CH2-5-Me-噻吩基3-CH2-6-Me-pyr3-CH2-6-OMe-pyr3-CH2-6-Br-pyr2-CH2-6-CF3-pyr3-CH2-6-F-pyr3-CH2-6-CF3-pyr3-CH2-6-OCF3-pyr2-CH2-6-Me-pyr2-CH2-6-OMe-pyr2-CH2-6-Br-pyr2-CH2-6-F-pyr5-CH2-嘧啶基2-CH2-嘧啶基 | 5-CH2-1-Me-吡唑基2-CH2-吡嗪基2-CH2-3-Me-吡嗪基2-CH2-5-Me-吡嗪基2-CH2-6-Me-吡嗪基3-CH2-哒嗪基3-CH2-6-Me-哒嗪基3-CH2-6-Cl-哒嗪基4-CH2-嘧啶基5-CH2-2-Me-嘧啶基2-CH2-5-CF3-噻二嗪基2-CH2-5-Br-噻吩基5-CH2-3-Me-异噁唑基5-CH2-3-F-异噁唑基 | 3-CH2-1-Me-吡咯基5-CH2-噻唑基2-CH2-噻吩基5-CH2-2-Cl-嘧啶基2-CH2-5-Cl-吡嗪基2-CH2-6-OCF3-pyr2-CH2-噻二嗪基5-Me-2-噻二嗪基5-Cl-2-噻二嗪基5-CF2-2-噻二嗪基2-CH2-5-Me-噻二嗪基2-CH2-5-Cl-噻二嗪基5-CH2-3-Cl-异噁唑基5-CH2-3-Br-异噁唑基 |
表4 R1=
栏 | ||||
1 | 2 | 3 | 4 | |
109110111112113114115116117118119120 | HMeEtn-Pri-Prn-Bus-Bui-Buc-PrHCCCH2NCCH22-pyr | PhCH2Ph2-Cl-Ph3-Cl-Ph4-Cl-PhCH2(c-Pr)2-CH2-pyr3-CH2-pyr4-CH2-pyr5-CH2-异噁唑基Me2NCH2CH2(c-Bu) | 2-CH2-5-CF3-噻吩基NCCH2CH2AcNHCH2AcNHCH2CH2CH2NMe3ICH2CH2NMe3ICH2(2-Cl-Ph)CH2(3-Cl-Ph)CH2(4-Cl-Ph)CH2C(Me)CH2HCCCH2CH2CH2CHCH2 | CH2(3,4-di-Cl-Ph)2-CH2-6-Cl-pyr3-CH2-6-Cl-pyr4-CH2-6-Cl-pyr2-CH2-5-Cl-pyr2-CH2-4-Cl-pyr2-CH2-3-Cl-pyr2-CCH2-5,6-di-Cl-pyr3-CH2-5-Cl-pyr3-CH2-4-Cl-pyr3-CH2-2-Cl-Pyr3-CH2-5,6-di-Cl-pyr |
121122123124125126127128129130131132133134135136137138139140141142143144 | 3-pyr4-pyrAcSCH2Et2NCH2c-Bu环戊基环己基6-F-2-pyr6-Me-3-pyr6-Br-3-pyr6-F-3-pyr6-OMe-3-pyr6-Me-2-pyr6-Br-2-pyr5-Cl-2-pyr5-Me-2-pyr5-Br-2-pyr5-F-2-pyr6-OMe-2-pyr2-噻二唑基MeSCH26-Cl-2-pyr6-Cl-3-pyr6-Cl-4-pyr | CH2(环戊基)CH2(环己基)5-CH2-2-Me-噻唑基5-CH2-2-Br-噻唑基2-CH2-5-Me-噻吩基3-CH2-吡唑基4-CH2-吡唑基5-CH2-吡唑基2-CH2-5-Cl-噻吩基2-CH2-5-Me-噻吩基3-CH2-6-Me-pyr3-CH2-6-OMe-pyr3-CH2-6-Br-yr2-CH2-6-CF3-pyr3-CH2-6-F-pyr3-CH2-6-CF3-pyr3-CH2-6-OCF3-pyr2-CH2-6-Me-pyr2-CH2-6-OMe-pyr2-CH2-6-Br-pyr2-CH2-6-F-pyr5-CH2-嘧啶基2-CH2-嘧啶基 | MeSCH2CH2AcSCH2CH22-CH2-呋喃基5,6-di-Cl-3-pyr5-OMe-2-pyr2-CH2-吡咯基3-CH2-吡咯基3-CH2-1-Me-吡唑基4-CH2-1-Me-吡唑基5-CH2-1-Me-吡唑基2-CH2-吡嗪基2-CH2-3-Me-吡嗪基2-CH2-5-Me-吡嗪基2-CH2-6-Me-吡嗪基3-CH2-哒嗪基3-CH2-6-Me-哒嗪基3-CH2-6-Cl-哒嗪基4-CH2-嘧啶基5-CH2-2-Me-嘧啶基2-CH2-5-CF3-噻二嗪基2-CH2-5-Br-噻吩基5-CH2-3-Me-异噁唑基5-CH2-3-F-异噁唑基 | 4-CH2-2,6-di-Cl-pyr5-CH2-2-Cl-噻唑基CH2CHCH2CH2CH2C(Me)CH2CH2CH3CHCHCH2CH3CHCHCH2CH2Et2NCH2CH2Me2NCH2CH22-CH2-1-Me-吡咯基3-CH2-1-Me-吡咯基5-CH2-噻唑基2-CH2-噻吩基5-CH2-2-Cl-嘧啶基2-CH2-5-Cl-吡嗪基2-CH2-6-OCF3-pyr2-CH2-噻二嗪基5-Me-2-噻二嗪基5-Cl-2-噻二嗪基5-CF2-2-噻二嗪基2-CH2-5-Me-噻二嗪基2-CH2-5-Cl-噻二嗪基5-CH2-3-Cl-异噁唑基5-CH2-3-Br-异噁唑基 |
表5 R1=
栏 | ||||
1 | 2 | 3 | 4 | |
145146147148149 | HMeEtn-Pri-Pr | PhCH2Ph2-Cl-Ph3-Cl-Ph4-Cl-Ph | 2-CH2-5-CF3-噻吩基NCCH2CH2AcNHCH2AcNHCH2CH2CH2NMe3I | CH2(3,4-di-Cl-Ph)2-CH2-6-Cl-pyr3-CH2-6-Cl-pyr4-CH2-6-Cl-pyr2-CH2-5-Cl-pyr |
150151152153154155156157158159160161162163164165166167168169170171172173174175176177178179180 | n-Bus-Bui-Buc-PrHCCCH2NCCH22-pyr3-pyr4-pyrAcSCH2Et2NCH2c-Bu环戊基环己基6-F-2-pyr6-Me-3-pyr6-Br-3-pyr6-F-3-pyr6-OMe-3-pyr6-Me-2-pyr6-Br-2-pyr5-Cl-2-pyr5-Me-2-pyr5-Br-2-pyr5-F-2-pyr6-OMe-2-pyr2-噻二唑基MeSCH26-Cl-2-pyr6-Cl-3-pyr6-Cl-4-pyr | CH2(c-Pr)2-CH2-pyr3-CH2-pyr4-CH2-pyr5-CH2-异噁唑基Me2NCH2CH2(c-Bu)CH2(环戊基)CH2(环己基)5-CH2-2-Me-噻唑基5-CH2-2-Br-噻唑基2-CH2-5-Me-噻吩基3-CH2-吡唑基4-CH2-吡唑基5-CH2-吡唑基2-CH2-5-Cl-噻吩基2-CH2-5-Me-噻吩基3-CH2-6-Me-pyr3-CH2-6-OMe-pyr3-CH2-6-Br-pyr2-CH2-6-CF3-pyr3-CH2-6-F-pyr3-CH2-6-CF3-pyr3-CH2-6-OCF3-pyr2-CH2-6-Me-pyr2-CH2-6-OMe-pyr2-CH2-6-Br-pyr2-CH2-6-F-pyr5-CH2-嘧啶基2-CH2-嘧啶基 | CH2CH2NMe3ICH2(2-Cl-Ph)CH2(3-Cl-Ph)CH2(4-Cl-Ph)CH2C(Me)CH2HCCCH2CH2CH2CHCH2MeSCH2CH2AcSCH2CH22-CH2-呋喃基5,6-di-Cl-3-pyr5-OMe-2-pyr2-CH2-吡咯基3-CH2-吡咯基3-CH2-1-Me-吡唑基4-CH2-1-Me-吡唑基5-CH2-1-Me-吡唑基2-CH2-吡嗪基2-CH2-3-Me-吡嗪基2-CH2-5-Me-吡嗪基2-CH2-6-Me-吡嗪基3-CH2-哒嗪基3-CH2-6-Me-哒嗪基3-CH2-6-Cl-哒嗪基4-CH2-嘧啶基5-CH2-2-Me-嘧啶基2-CH2-5-CF3-噻二嗪基2-CH2-5-Br-噻吩基5-CH2-3-Me-异噁唑基5-CH2-3-F-异噁唑基 | 2-CH2-4-Cl-pyr2-CH2-3-Cl-pyr2-CH2-5,6-di-Cl-pyr3-CH2-5-Cl-pyr3-CH2-4-Cl-pyr3-CH2-2-Cl-pyr3-CH2-5,6-di-Cl-pyr4-CH2-2,6-di-Cl-pyr5-CH2-2-Cl-噻唑基CH2CHCH2CH2CH2C(Me)CH2CH2CH3CHCHCH2CH3CHCHCH2CH2Et2NCH2CH2Me2NCH2CH22-CH2-1-Me-吡咯基3-CH2-1-Me-吡咯基5-CH2-噻唑基2-CH2-噻吩基5-CH2-2-Cl-嘧啶基2-CH2-5-Cl-吡嗪基2-CH2-6-OCF3-pyr2-CH2-噻二嗪基5-Me-2-噻二嗪基5-Cl-2-噻二嗪基5-CF2-2-噻二嗪基2-CH2-5-Me-噻二嗪基2-CH2-5-Cl-噻二嗪基5-CH2-3-Cl-异噁唑基5-CH2-3-Br-异噁唑基 |
表6 R1=
栏 | ||||
1 | 2 | 3 | 4 | |
181182183184185186187188189190191192193194195196197198199200201202203204205206207208209 | HMeEtn-Pri-Prn-Bus-Bui-Buc-PrHCCCH2NCCH22-pyr3-pyr4-pyrAcSCH2Et2NCH2c-Bu环戊基环己基6-F-2-pyr6-Me-3-pyr6-Br-3-pyr6-F-3-pyr6-OMe-3-pyr6-Me-2-pyr6-Br-2-pyr5-Cl-2-pyr5-Me-2-pyr5-Br-2-pyr | PhCH2Ph2-Cl-Ph3-Cl-Ph4-Cl-PhCH2(c-Pr)2-CH2-pyr3-CH2-pyr4-CH2-pyr5-CH2-异噁唑基Me2NCH2CH2(c-Bu)CH2(环戊基)CH2(环己基)5-CH2-2-Me-噻唑基5-CH2-2-Br-噻唑基2-CH2-5-Me-噻吩基3-CH2-吡唑基4-CH2-吡唑基5-CH2-吡唑基2-CH2-5-Cl-噻吩基2-CH2-5-Me-噻吩基3-CH2-6-Me-pyr3-CH2-6-OMe-pyr3-CH2-6-Br-pyr2-CH2-6-CF3-pyr3-CH2-6-F-pyr3-CH2-6-CF3-pyr3-CH2-6-OCF3-pyr | 2-CH2-5-CF3-噻吩基NCCH2CH2AcNHCH2AcNHCH2CH2CH2NMe3ICH2CH2NMe3ICH2(2-Cl-Ph)CH2(3-Cl-Ph)CH2(4-Cl-Ph)CH2C(Me)CH2HCCCH2CH2CH2CHCH2MeSCH2CH2AcSCH2CH22-CH2-呋喃基5,6-di-Cl-3-pyr5-OMe-2-pyr2-CH2-吡咯基3-CH2-吡咯基3-CH2-1-Me-吡唑基4-CH2-1-Me-吡唑基5-CH2-1-Me-吡唑基2-CH2-吡嗪基2-CH2-3-Me-吡嗪基2-CH2-5-Me-吡嗪基2-CH2-6-Me-吡嗪基3-CH2-哒嗪基3-CH2-6-Me-哒嗪基3-CH2-6-Cl-哒嗪基 | CH2(3,4-di-Cl-Ph)2-CH2-6-Cl-pyr3-CH2-6-Cl-pyr4-CH2-6-Cl-pyr2-CH2-5-Cl-pyr2-CH2-4-Cl-pyr2-CH2-3-Cl-pyr2-CH2-5,6-di-Cl-pyr3-CH2-5-Cl-pyr3-CH2-4-Cl-pyr3-CH2-2-Cl-pyr3-CH2-5,6-di-Cl-pyr4-CH2-2,6-di-Cl-pyr5-CH2-2-Cl-噻唑基CH2CHCH2CH2CH2C(Me)CH2CH2CH3CHCHCH2CH3CHCHCH2CH2Et2NCH2CH2Me2NCH2CH22-CH2-1-Me-吡咯基3-CH2-1-Me-吡咯基5-CH2-噻唑基2-CH2-噻吩基5-CH2-2-Cl-嘧啶基2-CH2-5-Cl-吡嗪基2-CH2-6-OCF3-pyr2-CH2-噻二嗪基5-Me-2-噻二嗪基 |
210211212213214215216 | 5-F-2-pyr6-OMe-2-pyr2-噻二唑基MeSCH26-Cl-2-pyr6-Cl-3-pyr6-Cl-4-pyr | 2-CH2-6-Me-pyr2-CH2-6-OMe-pyr2-CH2-6-Br-pyr2-CH2-6-F-pyr5-CH2-嘧啶基2-CH2-嘧啶基 | 4-CH2-嘧啶基5-CH2-2-Me-嘧啶基2-CH2-5-CF3-噻二嗪基2-CH2-5-Br-噻吩基5-CH2-3-Me-异噁唑基5-CH2-3-F-异噁唑基 | 5-Cl-2-噻二嗪基5-CF2-2-噻二嗪基2-CH2-5-Me-噻二嗪基2-CH2-5-Cl-噻二嗪基5-CH2-3-Cl-异噁嗪基5-CH2-3-Br-异噁嗪基 |
表7 R1=
栏 | ||||
1 | 2 | 3 | 4 | |
217218219220221222223224225226227228229230231232233234235236237 | HMeEtn-Pri-Prn-Bus-Bui-Buc-PrHCCCH2NCCH22-pyr3-pyr4-pyrAcSCH2Et2NCH2c-Bu环戊基环己基6-F-2-pyr6-Me-3-pyr | PhCH2Ph2-Cl-Ph3-Cl-Ph4-Cl-PhCH2(c-Pr)2-CH2-pyr3-CH2-pyr4-CH2-pyr5-CH2-异噁唑基Me2NCH2CH2(c-Bu)CH2(环戊基)CH2(环己基)5-CH2-2-Me-噻唑基5-CH2-2-Br-噻唑基2-CH2-5-Me-噻吩基3-CH2-吡唑基4-CH2-吡唑基5-CH2-吡唑基2-CH2-5-Cl-噻吩基 | 2-CH2-5-CF3-噻吩基NCCH2CH2AcNHCH2AcNHCH2CH2CH2NMe3ICH2CH2NMe3ICH2(2-Cl-Ph)CH2(3-Cl-Ph)CH2(4-Cl-Ph)CH2C(Me)CH2HCCCH2CH2CH2CHCH2MeSCH2CH2AcSCH2CH22-CH2-呋喃基5,6-di-Cl-3-py5-OMe-2-pyr2-CH2-吡咯基3-CH2-吡咯基3-CH2-1-Me-吡唑基4-CH2-1-Me-吡唑基 | CH2(3,4-di-Cl-Ph)2-CH2-6-Cl-pyr3-CH2-6-Cl-pyr4-CH2-6-Cl-pyr2-CH2-5-Cl-pyr2-CH2-4-Cl-pyr2-CH2-3-Cl-pyr2-CH2-5,6-di-Cl-Pyr3-CH2-5-Cl-pyr3-CH2-4-Cl-pyr3-CH2-2-Cl-pyr3-CH2-5,6-di-Cl-pyr4-CH2-2,6-di-Cl-pyr5-CH2-2-Cl-噻唑基CH2CHCH2CH2CH2C(Me)CH2CH2CH3CHCHCH2CH3CHCHCH2CH2Et2NCH2CH2Me2NCH2CH22-CH2-1-Me-吡咯基 |
238239240241242243244245246247248249250251252 | 6-Br-3-pyr6-F-3-pyr6-OMe-3-pyr6-Me-2-pyr6-Br-2-pyr5-Cl-2-pyr5-Me-2-pyr5-Br-2-pyr5-F-2-pyr6-OMe-2-pyr2-噻二唑基MeSCH26-Cl-2-pyr6-Cl-3-pyr6-Cl-4-pyr | 2-CH2-5-Me-thienyl3-CH2-6-Me-pyr3-CH2-6-OMe-pyr3-CH2-6-Br-pyr2-CH2-6-CF3-pyr3-CH2-6-F-Pyr3-CH2-6-CF3-pyr3-CH2-6-OCF3-pyr2-CH2-6-Me-pyr2-CH2-6-OMe-pyr2-CH2-6-Br-pyr2-CH2-6-F-pyr5-CH2-嘧啶基2-CH2-嘧啶基 | 5-CH2-1-Me-吡唑基2-CH2-吡嗪基2-CH2-3-Me-吡嗪基2-CH2-5-Me-吡嗪基2-CH2-6-Me-吡嗪基3-CH2-哒嗪基3-CH2-6-Me-哒嗪基3-CH2-6-Cl-哒嗪基4-CH2-嘧啶基5-CH2-2-Me-嘧啶基2-CH2-5-CF3-噻二嗪基2-CH2-5-Br-噻吩基5-CH2-3-Me-异噁唑基5-CH2-3-F-异噁唑基 | 3-CH2-1-Me-吡咯基5-CH2-噻唑基2-CH2-噻吩基5-CH2-2-Cl-嘧啶基2-CH2-5-Cl-吡嗪基2-CH2-6-OCF3-pyr2-CH2-噻二嗪基5-Me-2-噻二嗪基5-Cl-2-噻二嗪基5-CF2-2-噻二嗪基2-CH2-5-Me-噻二嗪基2-CH2-5-Cl-噻二嗪基5-CH2-3-Cl-异噁唑基5-CH2-3-Br-异噁唑基 |
表8 R1=
栏 | ||||
1 | 2 | 3 | 4 | |
253254255256257258259260261262263264265 | HMeEtn-Pri-Prn-Bus-Bui-Buc-PrHCCCH2NCCH22-pyr3-pyr | PhCH2Ph2-Cl-Ph3-Cl-Ph4-Cl-PhCH2(c-Pr)2-CH2-pyr3-CH2-pyr4-CH2-pyr5-CH2-异噁唑基Me2NCH2CH2(c-Bu)CH2(环戊基) | 2-CH2-5-CF3-噻吩基NCCH2CH2AcNHCH2AcNHCH2CH2CH2NMe3ICH2CH2NMe3ICH2(2-Cl-Ph)CH2(3-Cl-Ph)CH2(4-Cl-Ph)CH2C(Me)CH2HCCCH2CH2CH2CHCH2MeSCH2CH2 | CH2(3,4-di-Cl-Ph)2-CH2-6-Cl-pyr3-CH2-6-Cl-pyr4-CH2-6-Cl-pyr2-CH2-5-Cl-pyr2-CH2-4-Cl-pyr2-CH2-3-Cl-pyr2-CH2-5,6-di-Cl-pyr3-CH2-5-Cl-pyr3-CH2-4-Cl-pyr3-CH2-2-Cl-pyr3-CH2-5,6-di-Cl-pyr4-CH2-2,6-di-Cl-pyr |
266267268269270271272273274275276277278279280281282283284285286287288 | 4-pyrAcSCH2Et2NCH2c-Bu环戊基环己基6-F-2-pyr6-Me-3-pyr6-Br-3-pyr6-F-3-pyr6-OMe-3-pyr6-Me-2-pyr6-Br-2-pyr5-Cl-2-pyr5-Me-2-pyr5-Br-2-pyr5-F-2-pyr6-OMe-2-pyr2-噻二唑基MeSCH26-Cl-2-pyr6-Cl-3-pyr6-Cl-4-pyr | CH2(环己基)5-CH2-2-Me-噻唑基5-CH2-2-Br-噻唑基2-CH2-5-Me-噻吩基3-CH2-吡唑基4-CH2-吡唑基5-CH2-吡唑基2-CH2-5-Cl-噻吩基2-CH2-5-Me-噻吩基3-CH2-6-Me-pyr3-CH2-6-OMe-pyr3-CH2-6-Br-pyr2-CH2-6-CF3-pyr3-CH2-6-F-pyr3-CH2-6-CF3-pyr3-CH2-6-OCF3-pyr2-CH2-6-Me-pyr2-CH2-6-OMe-pyr2-CH2-6-Br-pyr2-CH2-6-F-pyr5-CH2-嘧啶基2-CH2-嘧啶基 | AcSCH2CH22-CH2-呋喃基5,6-di-Cl-3-pyr5-OMe-2-pyr2-CH2-吡咯基3-CH2-吡咯基3-CH2-1-Me-吡唑基4-CH2-1-Me-吡唑基5-CH2-1-Me-吡唑基2-CH2-吡嗪基2-CH2-3-Me-吡嗪基2-CH2-5-Me-吡嗪基2-CH2-6-Me-吡嗪基3-CH2-哒嗪基3-CH2-6-Me-哒嗪基3-CH2-6-Cl-哒嗪基4-CH2-嘧啶基5-CH2-2-Me-嘧啶基2-CH2-5-CF3-噻二嗪基2-CH2-5-Br-噻吩基5-CH2-3-Me-异噁唑基5-CH2-3-F-异噁唑基 | 5-CH2-2-Cl-噻唑基CH2CHCH2CH2CH2C(Me)CH2CH2CH3CHCHCH2CH3CHCHCH2CH2Et2NCH2CH2Me2NCH2CH22-CH2-1-Me-吡咯基3-CH2-1-Me-吡咯基5-CH2-噻唑基2-CH2-噻吩基5-CH2-2-Cl-嘧啶基2-CH2-5-Cl-吡嗪基2-CH2-6-OCF3-pyr2-CH2-噻二嗪基5-Me-2-噻二嗪基5-Cl-2-噻二嗪基5-CF2-2-噻二嗪基2-CH2-5-Me-噻二嗪基2-CH2-5-Cl-噻二嗪基5-CH2-3-Cl-异噁唑基5-CH2-3-Br-异噁唑基 |
表9 R1=
栏 | ||||
1 | 2 | 3 | 4 | |
289290291292293294 | HMeEtn-Pri-Prn-Bu | PhCH2Ph2-Cl-Ph3-Cl-Ph4-Cl-PhCH2(c-Pr) | 2-CH2-5-CF3-噻吩基NCCH2CH2AcNHCH2AcNHCH2CH2CH2NMe3ICH2CH2NMe3I | CH2(3,4-di-Cl-Ph)2-CH2-6-Cl-pyr3-CH2-6-Cl-pyr4-CH2-6-Cl-pyr2-CH2-5-Cl-pyr2-CH2-4-Cl-pyr |
295296297298299300301302303304305306307308309310311312313314315316317318319320321322323324 | s-Bui-Buc-PrHCCCH2NCCH22-pyr3-pyr4-pyrAcSCH2Et2NCH2c-Bu环戊基环己基6-F-2-pyr6-Me-3-pyr6-Br-3-pyr6-F-3-pyr6-OMe-3-pyr6-Me-2-pyr6-Br-2-pyr5-Cl-2-pyr5-Me-2-pyr5-Br-2-pyr5-F-2-pyr6-OMe-2-pyr2-噻二唑基MeSCH26-Cl-2-pyr6-Cl-3-pyr6-Cl-4-pyr | 2-CH2-pyr3-CH2-pyr4-CH2-pyr5-CH2-异噁唑基Me2NCH2CH2(c-Bu)CH2(环戊基)CH2(环己基)5-CH2-2-Me-噻唑基5-CH2-2-Br-噻唑基2-CH2-5-Me-噻吩基3-CH2-吡唑基4-CH2-吡唑基5-CH2-吡唑基2-CH2-5-Cl-噻吩基2-CH2-5-Me-噻吩基3-CH2-6-Me-pyr3-CH2-6-OMe-pyr3-CH2-6-Br-pyr2-CH2-6-CF3-pyr3-CH2-6-F-pyr3-CH2-6-CF3-pyr3-CH2-6-OCF3-pyr2-CH2-6-Me-pyr2-CH2-6-OMe-pyr2-CH2-6-Br-pyr2-CH2-6-F-pyr5-CH2-嘧啶基2-CH2-嘧啶基 | CH2(2-Cl-Ph)CH2(3-Cl-Ph)CH2(4-Cl-Ph)CH2C(Me)CH2HCCCH2CH2CH2CHCH2MeSCH2CH2AcSCH2CH22-CH2-呋喃基5,6-di-Cl-3-pyr5-OMe-2-pyr2-CH2-吡咯基3-CH2-吡咯基3-CH2-1-Me-吡唑基4-CH2-1-Me-吡唑基5-CH2-1-Me-吡唑基2-CH2-吡嗪基2-CH2-3-Me-吡嗪基2-CH2-5-Me-吡嗪基2-CH2-6-Me-吡嗪基3-CH2-哒嗪基3-CH2-6-Me-哒嗪基3-CH2-6-Cl哒嗪基4-CH2-嘧啶基5-CH2-2-Me-嘧啶基2-CH2-5-CF3-噻二嗪基2-CH2-5-Br-噻吩基5-CH2-3-Me-异噁唑基5-CH2-3-F-异噁唑基 | 2-CH2-3-Cl-pyr2-CH2-5,6-di-Cl-pyr3-CH2-5-Cl-pyr3-CH2-4-Cl-pyr3-CH2-2-Cl-pyr3-CH2-5,6-di-Cl-pyr4-CH2-2,6-di-Cl-pyr5-CH2-2-Cl-噻唑基CH2CHCH2CH2CH2C(Me)CH2CH2CH3CHCHCH2CH3CHCHCH2CH2Et2NCH2CH2Me2NCH2CH22-CH2-1-Me-吡咯基3-CH2-1-Me-吡咯基5-CH2-噻唑基2-CH2-噻吩基5-CH2-2-Cl-嘧啶基2-CH2-5-Cl-吡嗪基2-CH2-6-OCF3-pyr2-CH2-噻二嗪基5-Me-2-噻二嗪基5-Cl-2-噻二嗪基5-CF2-2-噻二嗪基2-CH2-5-Me-噻二嗪基2-CH2-5-Cl-噻二嗪基5-CH2-3-Cl-异噁唑基5-CH2-3-Br-异噁唑基 |
表10 R3=
表11 R3=
栏 | ||||
1 | 2 | 3 | 4 | |
325326327328329330331332333334335336337338339340341342343344345346347348349350351352353354355356357358359360 | HMeEtn-Pri-Prn-Bus-Bui-Buc-PrHCCCH2NCCH22-pyr3-pyr4-pyrAcSCH2Et2NCH2c-Bu环戊基环己基6-F-2-pyr6-Me-3-pyr6-Br-3-pyr6-F-3-pyr6-OMe-3-pyr6-Me-2-pyr6-Br-2-pyr5-Cl-2-pyr5-Me-2-pyr5-Br-2-pyr5-F-2-pyr6-OMe-2-pyr2-噻二唑基MeSCH26-Cl-2-pyr6-Cl-3-pyr6-Cl-4-pyr | PhCH2Ph2-Cl-ph3-Cl-Ph4-Cl-PhCH2(c-Pr)2-CH2-pyr3-CH2-pyr4-CH2-pyr5-CH2-异噁唑基Me2NCH2CH2(c-Bu)CH2(环戊基)CH2(环己基)5-CH2-2-Me-噻唑基5-CH2-2-Br-噻唑基2-CH2-5-Me-噻吩基3-CH2-吡唑基4-CH2-吡唑基5-CH2-吡唑基2-CH2-5-Cl-噻吩基2-CH2-5-Me-噻吩基3-CH2-6-Me-pyr3-CH2-6-OMe-pyr3-CH2-6-Br-pyr2-CH2-6-CF3-pyr3-CH2-6-F-pyr3-CH2-6-CF3-pyr3-CH2-6-OCF3-pyr2-CH2-6-Me-pyr2-CH2-6-OMe-pyr2-CH2-6-Br-pyr2-CH2-6-F-pyr5-CH2-嘧啶基2-CH2-嘧啶基 | 2-CH2-5-CF3-噻吩基NCCH2CH2AcNHCH2AcNHCH2CH2CH2NMe3ICH2CH2NMe3ICH2(2-Cl-Ph)CH2(3-Cl-Ph)CH2(4-Cl-Ph)CH2C(Me)CH2HCCCH2CH2CH2CHCH2MeSCH2CH2AcSCH2CH22-CH2-呋喃基5,6-di-Cl-3-pyr5-OMe-2-pyr2-CH2-吡咯基3-CH2-吡咯基3-CH2-1-Me-吡唑基4-CH2-1-Me-吡唑基5-CH2-1-Me-吡唑基2-CH2-吡嗪基2-CH2-3-Me-吡嗪基2-CH2-5-Me-吡嗪基2-CH2-6-Me-吡嗪基3-CH2-哒嗪基3-CH2-6-Me-哒嗪基3-CH2-6-Cl-哒嗪基4-CH2-嘧啶基5-CH2-2-Me-嘧啶基2-CH2-5-CF3-噻二嗪基2-CH2-5-Br-噻吩基5-CH2-3-Me-异噁唑基5-CH2-3-F-异噁唑基 | CH2(3,4-di-Cl-Ph)2-CH2-6-Cl-pyr3-CH2-6-Cl-pyr4-CH2-6-Cl-pyr2-CH2-5-Cl-pyr2-CH2-4-Cl-pyr2-CH2-3-Cl-pyr2-CH2-5,6-di-Cl-pyr3-CH2-5-Cl-pyr3-CH2-4-Cl-pyr3-CH2-2-Cl-pyr3-CH2-5,6-di-Cl-pyr4-CH2-2,6-di-Cl-pyr5-CH2-2-Cl-噻唑基CH2CHCH2CH2CH2C(Me)CH2CH2CH3CHCHCH2CH3CHCHCH2CH2Et2NCH2CH2Me2NCH2CH22-CH2-1-Me-吡咯基3-CH2-1-Me吡咯基5-CH2-噻唑基2-CH2-噻吩基5-CH2-2-Cl-嘧啶基2-CH2-5-Cl-吡嗪基2-CH2-6-OCF3-pyr2-CH2-噻二嗪基5-Me-2-噻二嗪基5-Cl-2-噻二嗪基5-CF2-2-噻二嗪基2-CH2-5-Me-噻二嗪基2-CH2-5-Cl-噻二嗪基5-CH2-3-Cl-异噁唑基5-CH2-3-Br-异噁唑基 |
栏 | ||||
1 | 2 | 3 | 4 | |
361362363364365366367368369370371372373374375376377378379380381382383384385386387388389390 | HMeEtn-Pri-Prn-Bus-Bui-Buc-PrHCCCH2NCCH22-pyr3-pyr4-pyrAcSCH2Et2NCH2c-Bu环戊基环己基6-F-2-pyr6-Me-3-pyr6-Br-3-pyr6-F-3-pyr6-OMe-3-pyr6-Me-2-pyr6-Br-2-pyr5-Cl-2-pyr5-Me-2-pyr5-Br-2-pyr5-F-2-pyr | PhCH2Ph2-Cl-Ph3-Cl-Ph4-Cl-PhCH2(c-Pr)2-CH2-pyr3-CH2-pyr4-CH2-pyr5-CH2-异噁唑基Me2NCH2CH2(c-Bu)CH2(环戊基)CH2(环己基)5-CH2-2-Me-噻唑基5-CH2-2-Br-噻唑基2-CH2-5-Me-噻吩基3-CH2-吡唑基4-CH2-吡唑基5-CH2-吡唑基2-CH2-5-Cl-噻吩基2-CH2-5-Me-噻吩基3-CH2-6-Me-pyr3-CH2-6-OMe-pyr3-CH2-6-Br-pyr2-CH2-6-CF3-pyr3-CH2-6-F-pyr3-CH2-6-CF3-pyr3-CH2-6-OCF3-pyr2-CH2-6-Me-pyr | 2-CH2-5-CF3-噻吩基NCCH2CH2AcNHCH2AcNHCH2CH2CH2NMe3ICH2CH2NMe3ICH2(2-Cl-Ph)CH2(3-Cl-Ph)CH2(4-Cl-Ph)CH2C(Me)CH2HCCCH2CH2CH2CHCH2MeSCH2CH2AcSCH2CH22-CH2-呋喃基5,6-di-Cl-3-pyr5-OMe-2-pyr2-CH2-吡咯基3-CH2-吡咯基3-CH2-1-Me-吡唑基4-CH2-1-Me-吡唑基5-CH2-1-Me-吡唑基2-CH2-吡嗪基2-CH2-3-Me-吡嗪基2-CH2-5-Me-吡嗪基2-CH2-6-Me-吡嗪基3-CH2-哒嗪基3-CH2-6-Me-哒嗪基3-CH2-6-Cl-哒嗪基4-CH2-嘧啶基 | CH2(3,4-di-Cl-Ph)2-CH2-6-Cl-pyr3-CH2-6-Cl-pyr4-CH2-6-Cl-pyr2-CH2-5-Cl-pyr2-CH2-4-Cl-pyr2-CH2-3-Cl-pyr2-CH2-5,6-di-Cl-pyr3-CH2-5-Cl-pyr3-CH2-4-Cl-pyr3-CH2-2-Cl-pyr3-CH2-5,6-di-Cl-pyr4-CH2-2,6-di-Cl-pyr5-CH2-2-Cl-噻唑基CH2CHCH2CH2CH2C(Me)CH2CH2CH3CHCHCH2CH3CHCHCH2CH2Et2NCH2CH2Me2NCH2CH22-CH2-1-Me-吡咯基3-CH2-1-Me-吡咯基5-CH2-噻唑基2-CH2-噻吩基5-CH2-2-Cl-嘧啶基2-CH2-5-Cl-吡嗪基2-CH2-6-OCF3-pyr2-CH2-噻二嗪基5-Me-2-噻二嗪基5-Cl-2-噻二嗪基 |
391392393394395396 | 6-OMe-2-pyr2-噻二唑基MeSCH26-Cl-2-pyr6-Cl-3-pyr6-Cl-4-pyr | 2-CH2-6-OMe-pyr2-CH2-6-Br-pyr2-CH2-6-F-pyr5-CH2-嘧啶基2-CH2-嘧啶基 | 5-CH2-2-Me-嘧啶基2-CH2-5-CF3-噻二嗪基2-CH2-5-Br-噻吩基5-CH2-3-Me-异噁唑基5-CH2-3-F-异噁唑基 | 5-CF2-2-噻二嗪基2-CH2-5-Me-噻二嗪基2-CH2-5-Cl-噻二嗪基5-CH2-3-Cl-异噁嗪基5-CH2-3-Br-异噁嗪基 |
表12 R3=
栏 | ||||
1 | 2 | 3 | 4 | |
397398399400401402403404405406407408409410411412413414415416417418419420421 | HMeEtn-Pri-Prn-Bus-Bui-Buc-PrHCCCH2NCCH22-pyr3-pyr4-pyrAcSCH2Et2NCH2c-Bu环戊基环己基6-F-2-pyr6-Me-3-pyr6-Br-3-pyr6-F-3-pyr6-OMe-3-pyr6-Me-2-pyr | PhCH2Ph2-Cl-Ph3-Cl-Ph4-Cl-PhCH2(c-Pr)2-CH2-pyr3-CH2-pyr4-CH2-pyr5-CH2-异噁唑基Me2NCH2CH2(c-Bu)CH2(环戊基)CH2(环己基)5-CH2-2-Me-噻唑基5-CH2-2-Br-噻唑基2-CH2-5-Me-噻吩基3-CH2-吡唑基4-CH2-吡唑基5-CH2-吡唑基2-CH2-5-Cl-噻吩基2-CH2-5-Me-噻吩基3-CH2-6-Me-pyr3-CH2-6-OMe-pyr3-CH2-6-Br-pyr | 2-CH2-5-CF3-噻吩基NCCH2CH2AcNHCH2AcNHCH2CH2CH2NMe3ICH2CH2NMe3ICH2(2-Cl-Ph)CH2(3-Cl-Ph)CH2(4-Cl-Ph)CH2C(Me)CH2HCCCH2CH2CH2CHCH2MeSCH2CH2AcSCH2CH22-CH2-呋喃基5,6-di-Cl-3-pyr5-OMe-2-pyr2-CH2-吡咯基3-CH2-吡咯基3-CH2-1-Me-吡唑基4-CH2-1-Me-吡唑基5-CH2-1-Me-吡唑基2-CH2-吡嗪基2-CH2-3-Me-吡嗪基2-CH2-5-Me-吡嗪基 | CH2(3,4-di-Cl-Ph)2-CH2-6-Cl-pyr3-CH2-6-Cl-pyr4-CH2-6-Cl-pyr2-CH2-5-Cl-pyr2-CH2-4-Cl-pyr2-CH2-3-Cl-pyr2-CH2-5,6-di-Cl-pyr3-CH2-5-Cl-pyr3-CH2-4-Cl-pyr3-CH2-2-Cl-pyr3-CH2-5,6-di-Cl-pyr4-CH2-2,6-di-Cl-pyr5-CH2-2-Cl-噻唑基CH2CHCH2CH2CH2C(Me)CH2CH2CH3CHCHCH2CH3CHCHCH2CH2Et2NCH2CH2Me2NCH2CH22-CH2-1-Me-吡咯基3-CH2-1-Me-吡咯基5-CH2-噻唑基2-CH2-噻吩基5-CH2-2-Cl-嘧啶基 |
422423424425426427428429430431432 | 6-Br-2-pyr5-Cl-2-pyr5-Me-2-pyr5-Br-2-pyr5-F-2-pyr6-OMe-2-pyr2-噻二唑基MeSCH26-Cl-2-pyr6-Cl-3-pyr6-Cl-4-pyr | 2-CH2-6-CF3-pyr3-CH2-6-F-pyr3-CH2-6-CF3-pyr3-CH2-6-OCF3-pyr2-CH2-6-Me-pyr2-CH2-6-OMe-pyr2-CH2-6-Br-pyr2-CH2-6-F-pyr5-CH2-嘧啶基2-CH2-嘧啶基 | 2-CH2-6-Me-吡嗪基3-CH2-哒嗪基3-CH2-6-Me-哒嗪基3-CH2-6-Cl-哒嗪基4-CH2-嘧啶基5-CH2-2-Me-嘧啶基2-CH2-5-CF3-噻二嗪基2-CH2-5-Br-噻吩基5-CH2-3-Me-异噁唑基5-CH2-3-F-异噁唑基 | 2-CH2-5-Cl-吡嗪基2-CH2-6-OCF3-pyr2-CH2-噻二嗪基5-Me-2-噻二嗪基5-Cl-2-噻二嗪基5-CF2-2-噻二嗪基2-CH2-5-Me-噻二嗪基2-CH2-5-Cl-噻二嗪基5-CH2-3-Cl-异噁唑基5-CH2-3-Br-异噁唑基 |
表13 R3=
栏 | ||||
1 | 2 | 3 | 4 | |
433434435436437438439440441442443444445446447448449450451 | HMeEtn-Pri-Prn-Bus-Bui-Buc-PrHCCCH2NCCH22-pyr3-pyr4-pyrAcSCH2Et2NCH2c-Bu环戊基环己基 | PhCH2Ph2-Cl-Ph3-Cl-Ph4-Cl-PhCH2(c-Pr)2-CH2-pyr3-CH2-pyr4-CH2-pyr5-CH2-异噁唑基Me2NCH2CH2(c-Bu)CH2(环戊基)CH2(环己基)5-CH2-2-Me-噻唑基5-CH2-2-Br-噻唑基2-CH2-5-Me-噻吩基3-CH2-吡唑基4-CH2-吡唑基 | 2-CH2-5-CF3-噻吩基NCCH2CH2AcNHCH2AcNHCH2CH2CH2NMe3ICH2CH2NMe3ICH2(2-Cl-Ph)CH2(3-Cl-Ph)CH2(4-Cl-Ph)CH2C(Me)CH2HCCCH2CH2CH2CHCH2MeSCH2CH2AcSCH2CH22-CH2-呋喃基5,6-di-Cl-3-pyr5-OMe-2-pyr2-CH2-吡咯基3-CH2-吡咯基 | CH2(3,4-di-Cl-Ph)2-CH2-6-Cl-pyr3-CH2-6-Cl-pyr4-CH2-6-Cl-pyr2-CH2-5-Cl-pyr2-CH2-4-Cl-pyr2-CH2-3-Cl-pyr2-CH2-5,6-di-Cl-pyr3-CH2-5-Cl-pyr3-CH2-4-Cl-pyr3-CH2-2-Cl-pyr3-CH2-5,6-di-Cl-pyr4-CH2-2,6-di-Cl-pyr5-CH2-2-Cl-噻唑基CH2CHCH2CH2CH2C(Me)CH2CH2CH3CHCHCH2CH3CHCHCH2CH2Et2NCH2CH2 |
452453454455456457458459460461462463464465466467468 | 6-F-2-pyr6-Me-3-pyr6-Br-3-pyr6-F-3-pyr6-OMe-3-pyr6-Me-2-pyr6-Br-2-pyr5-Cl-2-pyr5-Me-2-pyr5-Br-2-pyr5-F-2-pyr6-OMe-2-pyr2-噻二唑基MeSCH26-Cl-2-pyr6-Cl-3-Pyr6-Cl-4-pyr | 5-CH2-吡唑基2-CH2-5-Cl-噻吩基2-CH2-5-Me-噻吩基3-CH2-6-Me-pyr3-CH2-6-OMe-pyr3-CH2-6-Br-pyr2-CH2-6-CF3-pyr3-CH2-6-F-pyr3-CH2-6-CF3-pyr3-CH2-6-OCF3-pyr2-CH2-6-Me-pyr2-CH2-6-OMe-pyr2-CH2-6-Br-pyr2-CH2-6-F-pyr5-CH2-嘧啶基2-CH2-嘧啶基 | 3-CH2-1-Me-吡唑基4-CH2-1-Me-吡唑基5-CH2-1-Me-吡唑基2-CH2-吡嗪基2-CH2-3-Me-吡嗪基2-CH2-5-Me-吡嗪基2-CH2-6-Me-吡嗪基3-CH2-哒嗪基3-CH2-6-Me-哒嗪基3-CH2-6-Cl-哒嗪基4-CH2-嘧啶基5-CH2-2-Me-嘧啶基2-CH2-5-CF3-噻二嗪基2-CH2-5-Br-噻吩基5-CH2-3-Me-异噁唑基5-CH2-3-F-异噁唑基 | Me2NCH2CH22-CH2-1-Me-吡咯基3-CH2-1-Me-吡咯基5-CH2-噻唑基2-CH2-噻吩基5-CH2-2-Cl-嘧啶基2-CH2-5-Cl-吡嗪基2-CH2-6-OCF3-pyr2-CH2-噻二嗪基5-Me-2-噻二嗪基5-Cl-2-噻二嗪基5-CF2-2-噻二嗪基2-CH2-5-Me-噻二嗪基2-CH2-5-Cl-噻二嗪基5-CH2-3-Cl-异噁唑基5-CH2-3-Br-异噁唑基 |
表14 R3=
栏 | ||||
1 | 2 | 3 | 4 | |
469470471472473474475476477478479480 | HMeEtn-Pri-Prn-Bus-Bui-Buc-PrHCCCH2NCCH22-pyr | PhCH2Ph2-Cl-Ph3-Cl-Ph4-Cl-PhCH2(c-Pr)2-CH2-pyr3-CH2-pyr4-CH2-pyr5-CH2-异噁唑基Me2NCH2CH2(c-Bu) | 2-CH2-5-CF3-噻吩基NCCH2CH2AcNHCH2AcNHCH2CH2CH2NMe3ICH2CH2NMe3ICH2(2-Cl-Ph)CH2(3-Cl-Ph)CH2(4-Cl-Ph)CH2C(Me)CH2HCCCH2CH2CH2CHCH2 | CH2(3,4-di-Cl-Ph)2-CH2-6-Cl-pyr3-CH2-6-Cl-pyr4-CH2-6-Cl-pyr2-CH2-5-Cl-pyr2-CH2-4-Cl-pyr2-CH2-3-Cl-pyr2-CH2-5,6-di-Cl-pyr3-CH2-5-Cl-pyr3-CH2-4-Cl-pyr3-CH2-2-Cl-pyr3-CH2-5,6-di-Cl-pyr |
481482483484485486487488489490491492493494495496497498499500501502503504 | 3-pyr4-pyrAcSCH2Et2NCH2c-Bu环戊基环己基6-F-2-pyr6-Me-3-pyr6-Br-3-pyr6-F-3-pyr6-OMe-3-pyr6-Me-2-pyr6-Br-2-pyr5-Cl-2-pyr5-Me-2-pyr5-Br-2-pyr5-F-2-pyr6-OMe-2-pyr2-噻二唑基MeSCH26-Cl-2-pyr6-Cl-3-pyr6-Cl-4-pyr | CH2(环戊基)CH2(环己基)5-CH2-2-Me-噻唑基5-CH2-2-Br-噻唑基2-CH2-5-Me-噻吩基3-CH2-吡唑基4-CH2-吡唑基5-CH2-吡唑基2-CH2-5-Cl-噻吩基2-CH2-5-Me-噻吩基3-CH2-6-Me-pyr3-CH2-6-OMe-pyr3-CH2-6-Br-pyr2-CH2-6-CF3-pyr3-CH2-6-F-pyr3-CH2-6-CF3-pyr3-CH2-6-OCF3-pyr2-CH2-6-Me-pyr2-CH2-6-OMe-pyr2-CH2-6-Br-pyr2-CH2-6-F-pyr5-CH2-嘧啶基2-CH2-嘧啶基 | MeSCH2CH2AcSCH2CH22-CH2-呋喃基5,6-di-Cl-3-pyr5-OMe-2-pyr2-CH2-吡咯基3-CH2-吡咯基3-CH2-1-Me-吡唑基4-CH2-1-Me-吡唑基5-CH2-1-Me-吡唑基2-CH2-吡嗪基2-CH2-3-Me-吡嗪基2-CH2-5-Me-吡嗪基2-CH2-6-Me-吡嗪基3-CH2-哒嗪基3-CH2-6-Me-哒嗪基3-CH2-6-Cl-哒嗪基4-CH2-嘧啶基5-CH2-2-Me-嘧啶基2-CH2-5-CF3-噻二嗪基2-CH2-5-Br-噻吩基5-CH2-3-Me-异噁唑基5-CH2-3-F-异噁唑基 | 4-CH2-2,6-di-Cl-pyr5-CH2-2-Cl-噻唑基CH2CHCH2CH2CH2C(Me)CH2CH2CH3CHCHCH2CH3CHCHCH2CH2Et2NCH2CH2Me2NCH2CH22-CH2-1-Me-吡咯基3-CH2-1-Me-吡咯基5-CH2-噻唑基2-CH2-噻吩基5-CH2-2-Cl-嘧啶基2-CH2-5-Cl-吡嗪基2-CH2-6-OCF3-pyr2-CH2-噻二嗪基5-Me-2-噻二嗪基5-Cl-2-噻二嗪基5-CF2-2-噻二嗪基2-CH2-5-Me-噻二嗪基2-CH2-5-Cl-噻二嗪基5-CH2-3-Cl-异噁唑基5-CH2-3-Br-异噁唑基 |
表15-16中Q的各种含意为:Q-1=6-氯-3-吡啶基、Q-2=5,6-二氯-3-吡啶基、Q-3=2-氯-5-噻唑基、Q-4=3-氯-5-异噁唑基和Q-5=CH3SCH2-。
表15 Q=
栏
1 2 3 4 5505 A=直接键;R2=H;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5506 A=直接键;R2=H;R3=Me;R4=t-Bu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5507 A=直接键;R2=H;R3=Me;R4=Ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5508 A=直接键;R2=H;R3=Me;R4=i-Pr;R5=i-Pr;R6=i-Pr; Q-1 Q-2 Q-3 Q-4 Q-5509 A=直接键;R2=H;R3=Me;R4=t-Bu;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5510 A=直接键;R2=H;R3=Me;R4=Ph;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5511 A=CH2;R2=H;R3=Me;R4=t-Bu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5512 A=CH2;R2=H;R3=Me;R4=Ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5513 A=CH2;R2=H;R3=Me;R4=i-Pr;R5=i-Pr;R6=i-Pr; Q-1 Q-2 Q-3 Q-4 Q-5514 A=CH2;R2=H;R3=Me;R4=t-Bu;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5515 A=CH2;R2=H;R3=Me;R4=Ph;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5516 A=CH2;R2=H;R3=Me;R4=Et;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5517 A=CH2;R2=H;R3=Me;R4=CH2CH;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5518 A=CH2;R2=H;R3=Me;R4=CH2CHCH2;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5519 A=CH2;R2=H;R3=Me;R4=EtO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5512 A=CH2;R2=H;R3=Me;R4=i-PrO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5513 A=CH2;R2=H;R3=Me;R4=EtO;R5=EtO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5514 A=CH2;R2=H;R3=Me;R4=i-PrO;R5=i-PrO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5515 A=CH2;R2=H;R3=Me;R4=EtO;R5=EtO;R6=EtO; Q-1 Q-2 Q-3 Q-4 Q-5516 A=CH2;R2=H;R3=Me;R4=i-PrO;R5=i-PrO;R6=i-PrO; Q-1 Q-2 Q-3 Q-4 Q-5517 A=CH2;R2=H;R3=Me;R4=H;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5518 A=CH2;R2=H;R3=Me;R4=H;R5=Et;R6=Et; Q-1 Q-2 Q-3 Q-4 Q-5519 A=CH2CH2;R2=H;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5520 A=(CH2)3;R2=H;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5521 A=CH2CHCH;R2=H;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5522 A=CH2CC;R2=H;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5523 A=CH2CH2CHCH;R2=H;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5524 A=CH2CH2CC;R2=H;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5525 A=o-Ph;R2=H;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5526 A=m-Ph;R2=H;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5527 A=p-Ph;R2=H;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5528 A=直接键R2=Me;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5529 A=直接键R2=Me;R3=Me;R4=r-Bu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5530 A=直接键;R2=Me;R3=Me;R4=Ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5531 A=直接键;R2=Me;R3=Me;R4=i-Pr;R5=i-Pr;R6=i-Pr; Q-1 Q-2 Q-3 Q-4 Q-5532 A=直接键;R2=Me;R3=Me;R4=t-Bu;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5533 A=直接键;R2=Me;R3=Me;R4=Ph;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5534 A=直接键;R2=H;R3=Me;R4=Me;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5535 A=CH2;R2=H;R3=Me;R4=Me;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5536 A=CH2;R2=Me;R3=Me;R4=Me;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5537 A=CH2;R2=Me;R3=Me;R4=t-Bu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5538 A=CH2;R2=Me;R3=Me;R4=Ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5539 A=CH2;R2=Me;R3=Me;R4=i-Pr;R5=i-Pr;R6=i-Pr; Q-1 Q-2 Q-3 Q-4 Q-5540 A=CH2;R2=Me;R3=Me;R4=t-Bu;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5541 A=CH2;R2=Me;R3=Me;R4=Ph;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5542 A=CH2;R2=Me;R3=Me;R4=Et;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5543 A=CH2;R2=Me;R3=Me;R4=CH2CH;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5544 A=CH2;R2=Me;R3=Me;R4=CH2CHCH2;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5545 A=CH2;R2=Me;R3=Me;R4=EtO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5546 A=CH2;R2=Me;R3=Me;R4=i-PrO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5547 A=CH2;R2=Me;R3=Me;R4=EtO;R5=EtO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5548 A=CH2;R2=Me;R3=Me;R4=i-PrO;R5=i-PrO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5549 A=CH2;R2=Me;R3=Me;R4=EtO;R5=EtO;R6=EtO; Q-1 Q-2 Q-3 Q-4 Q-5550 A=CH2;R2=Me;R3=Me;R4=MeO;R5=MeO;R6=MeO; Q-1 Q-2 Q-3 Q-4 Q-5551 A=CH2;R2=Me;R3=Me;R4=MeO;R5=MeO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5552 A=CH2;R2=Me;R3=Me;R4=MeO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5553 A=CH2;R2=Me;R3=Me;R4=H;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5554 A=CH2;R2=Me;R3=Me;R4=H;R5=Et;R6=Et; Q-1 Q-2 Q-3 Q-4 Q-5555 A=CH2CH2;R2=Me;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5556 A=(CH2)3;R2=Me;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5557 A=CH2CHCH;R2=Me;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5558 A=CH2CC;R2=Me;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5559 A=CH2CH2CHCH;R2=Me;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5560 A=CH2CH2CC;R2=Me;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5561 A=o-Ph;R2=Me;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5562 A=m-Ph;R2=Me;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5563 A=P-Ph;R2=Me;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5564 A=CH2;R2=H;R3=Me;R4=MeO;R5=MeO;R6=MeO; Q-1 Q-2 Q-3 Q-4 Q-5565 A=CH2;R2=H;R3=Me;R4=MeO;R5=MeO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5566 A=CH2;R2=H;R3=Me;R4=MeO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5567 A=直接键;R2=Et;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5568 A=直接键;R2=Et;R3=Me;R4=t-Bu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5569 A=直接键;R2=Et;R3=Me;R4=ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5570 A=直接键;R2=Et;R3=Me;R4=i-Pr;R5=i-Pr;R6=i-Pr; Q-1 Q-2 Q-3 Q-4 Q-5571 A=直接键;R2=Et;R3=Me;R4=t-Bu;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5572 A=直接键;R2=Et;R3=Me;R4=Ph;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5573 A=直接键;R2=Et;R3=Me;R4=Me;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5574 A=CH2;R2=Et;R3=Me;R4=Me;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5575 A=CH2;R2=Et;R3=Me;R4=t-Bu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5576 A=CH2;R2=Et;R3=Me;R4=Ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5577 A=CH2;R2=Et;R3=Me;R4=i-Pr;R5=i-Pr;R6=i-Pr; Q-1 Q-2 Q-3 Q-4 Q-5578 A=CH2;R2=Et;R3=Me;R4=t-Bu;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5579 A=CH2;R2=Et;R3=Me;R4=Ph;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5580 A=CH2;R2=Et;R3=Me;R4=Et;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5581 A=CH2;R2=Et;R3=Me;R4=CH2CH;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5582 A=CH2;R2=Et;R3=Me;R4=CH2CHCH2;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5583 A=CH2;R2=Et;R3=Me;R4=EtO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5584 A=CH2;R2=Et;R3=Me;R4=i-PrO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5585 A=CH2;R2=Et;R3=Me;R4=EtO;R5=EtO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5586 A=CH2;R2=Et;R3=Me;R4=i-PrO;R5=i-PrO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5587 A=CH2;R2=Et;R3=Me;R4=EtO;R5=EtO;R6=EtO; Q-1 Q-2 Q-3 Q-4 Q-5588 A=CH2;R2=Et;R3=Me;R4=MeO;R5=MeO;R6=MeO; Q-1 Q-2 Q-3 Q-4 Q-5589 A=CH2;R2=Et;R3=Me;R4=MeO;R5=MeO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5590 A=CH2;R2=Et;R3=Me;R4=MeO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5591 A=CH2;R2=Et;R3=Me;R4=H;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5592 A=CH2;R2=Et;R3=Me;R4=H;R5=Et;R6=Et; Q-1 Q-2 Q-3 Q-4 Q-5593 A=CH2CH2;R2=Et;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5594 A=(CH2)3;R2=Et;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5595 A=CH2CHCH;R2=Et;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5596 A=CH2CC;R2=Et;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5597 A=CH2CH2CHCH;R2=Et;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5598 A=CH2CH2CC;R2=Et;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5599 A=o-Ph;R2=Et;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5600 A=m-Ph;R2=Et;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5601 A=p-Ph;R2=Et;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5602 A=直接键;R2+R3=-CH2CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5603 A=直接键;R2+R3=-CH2CH2-;R4=t-Bu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5604 A=直接键;R2+R3=-CH2CH2-;R4=Ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5605 A=直接键;R2+R3=-CH2CH2-;R4=i-Pr;R5=i-Pr;R6=i-Pr; Q-1 Q-2 Q-3 Q-4 Q-5606 A=直接键;R2+R3=-CH2CH2-;R4=t-Bu;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5607 A=直接键;R2+R3=-CH2CH2-;R4=Ph;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5608 A=直接键;R2+R3=-CH2CH2-;R4=Me;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5609 A=CH2;R2+R3=-CH2CH2-;R4=Me;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5610 A=CH2;R2+R3=-CH2CH2-;R4=t-Bu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5611 A=CH2;R2+R3=-CH2CH2-;R4=Ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5612 A=CH2;R2+R3=-CH2CH2-;R4=i-Pr;R5=i-Pr;R6=i-Pr; Q-1 Q-2 Q-3 Q-4 Q-5613 A=CH2;R2+R3=-CH2CH2-;R4=t-Bu;R5=Ph;R6=ph; Q-1 Q-2 Q-3 Q-4 Q-5614 A=CH2;R2+R3=-CH2CH2-;R4=Ph;R5=Ph;R6=ph; Q-1 Q-2 Q-3 Q-4 Q-5615 A=CH2;R2+R3=-CH2CH2-;R4=Et;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5616 A=CH2;R2+R3=-CH2CH2-;R4=CH2CH;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5617 A=CH2;R2+R3=-CH2CH2-;R4=CH2CHCH2;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5618 A=CH2;R2+R3=-CH2CH2-;R4=EtO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5619 A=CH2;R2+R3=-CH2CH2-;R4=i-PrO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5620 A=CH2;R2+R3=-CH2CH2-;R4=EtO;R5=EtO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5621 A=CH2;R2+R3=-CH2CH2-;R4=i-PrO;R5=i-PrO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5622 A=CH2;R2+R3=-CH2CH2-;R4=EtO;R5=EtO;R6=EtO; Q-1 Q-2 Q-3 Q-4 Q-5623 A=CH2;R2+R3=-CH2CH2-;R4=MeO;R5=MeO;R6=MeO; Q-1 Q-2 Q-3 Q-4 Q-5624 A=CH2;R2+R3=-CH2CH2-;R4=MeO;R5=MeO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5625 A=CH2;R2+R3=-CH2CH2-;R4=MeO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5626 A=CH2;R2+R3=-CH2CH2-;R4=H;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5627 A=CH2;R2+R3=-CH2CH2-;R4=H;R5=Et;R6=Et; Q-1 Q-2 Q-3 Q-4 Q-5628 A=CH2CH2;R2+R3=-CH2CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5629 A=(CH2)3;R2+R3=-CH2CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5630 A=CH2CHCH;R2+R3=-CH2CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5631 A=CH2CC;R2+R3=-CH2CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5632 A=CH2CH2CHCH;R2+R3=-CH2CH2-;R4=Me;R5=Me; Q-1 Q-2 Q-3 Q-4 Q-5
R6=Me;633 A=CH2CH2CC;R2+R3=-CH2CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5634 A=o-Ph;R2+R3=-CH2CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5635 A=m-Ph;R2+R3=-CH2CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5636 A=p-Ph;R2+R3=-CH2CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5637 A=直接键;R2+R3=-CH(Me)CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5638 A=直接键;R2+R3=-CH(Me)CH2-;R4=t-Bu;R5=Me; Q-1 Q-2 Q-3 Q-4 Q-5
R6=Me;639 A=直接键;R2+R3=-CH(Me)CH2-;R4=Ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5640 A=直接键;R2+R3=-CH(Me)CH2-;R4=i-Pr;R5=i-Pr; Q-1 Q-2 Q-3 Q-4 Q-5
R6=i-Pr;641 A=直接键;R2+R3=-CH(Me)CH2-;R4=t-Bu;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5642 A=直接键;R2+R3=-CH(Me)CH2-;R4=Ph;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5643 A=直接键;R2+R3=-CH(Me)CH2-;R4=Me;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5644 A=CH2;R2+R3=-CH(Me)CH2-;R4=Me;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5645 A=CH2;R2+R3=-CH(Me)CH2-;R4=t-Bu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5646 A=CH2;R2+R3=-CH(Me)CH2-;R4=Ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5647 A=CH2;R2+R3=-CH(Me)CH2-;R4=i-Pr;R5=i-Pr;R6=i-Pr; Q-1 Q-2 Q-3 Q-4 Q-5648 A=CH2;R2+R3=-CH(Me)CH2-;R4=t-Bu;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5649 A=CH2;R2+R3=-CH(Me)CH2-;R4=Ph;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5650 A=CH2;R2+R3=-CH(Me)CH2-;R4=Et;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5651 A=CH2;R2+R3=-CH(Me)CH2-;R4=CH2CH;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5652 A=CH2;R2+R3=-CH(Me)CH2-;R4=CH2CHCH2;R5=Me; Q-1 Q-2 Q-3 Q-4 Q-5
R6=Me;653 A=CH2;R2+R3=-CH(Me)CH2-;R4=EtO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5654 A=CH2;R2+R3=-CH(Me)CH2-;R4=i-PrO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5655 A=CH2;R2+R3=-CH(Me)CH2-;R4=EtO;R5=EtO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5656 A=CH2;R2+R3=-CH(Me)CH2-;R4=i-PrO;R5=i-PrO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5657 A=CH2;R2+R3=-CH(Me)CH2-;R4=EtO;R5=EtO;R6=EtO; Q-1 Q-2 Q-3 Q-4 Q-5658 A=CH2;R2+R3=-CH(Me)CH2-;R4=MeO;R5=MeO;R6=MeO; Q-1 Q-2 Q-3 Q-4 Q-5659 A=CH2;R2+R3=-CH(Me)CH2-;R4=MeO;R5=MeO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5660 A=CH2;R2+R3=-CH(Me)CH2-;R4=MeO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5661 A=CH2;R2+R3=-CH(Me)CH2-;R4=H;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5662 A=CH2;R2+R3=-CH(Me)CH2-;R4=H;R5=Et;R6=Et; Q-1 Q-2 Q-3 Q-4 Q-5663 A=CH2CH2;R2+R3=-CH(Me)CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5664 A=(CH2)3;R2+R3=-CH(Me)CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5665 A=CH2CHCH;R2+R3=-CH(Me)CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5666 A=CH2CC;R2+R3=-CH(Me)CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5667 A=CH2CH2CHCH;R2+R3=-CH(Me)CH2-;R4=Me;R5=Me; Q-1 Q-2 Q-3 Q-4 Q-5
R6=Me;668 A=CH2CH2CC;R2+R3=-CH(Me)CH2-;R4=Me;R5=Me; Q-1 Q-2 Q-3 Q-4 Q-5
R6=Me;669 A=o-Ph;R2+R3=-CH(Me)CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5670 A=m-Ph;R2+R3=-CH(Me)CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5671 A=p-Ph;R2+R3=-CH(Me)CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5672 A=(CH2)3;R2+R3=-CH2CH2-;R4=Et;R5=Et;R6=Et; Q-1 Q-2 Q-3 Q-4 Q-5673 A=(CH2)3;R2+R3=-CH2CH2-;R4=iPr;R5=iPr;R6=iPr; Q-1 Q-2 Q-3 Q-4 Q-5674 A=(CH2)3;R2+R3=-CH2CH2-;R4=Ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5675 A=(CH2)3;R2+R3=-CH2CH2-;R4=tBu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5676 A=(CH2)3;R2+R3=-CH2CH2-;R4=EtO;R5=EtO;R6=EtO; Q-1 Q-2 Q-3 Q-4 Q-5677 A=(CH2)3;R2+R3=-CH2CH2-;R4=MeO;R5=MeO;R6=MeO; Q-1 Q-2 Q-3 Q-4 Q-5678 A=(CH2)3;R2+R3=-CH2CH2-;R4=EtO;R5=EtO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5679 A=(CH2)3;R2+R3=-CH2CH2-;R4=EtO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5680 A=(CH2)3;R2+R3=-CH2CH2-;R4=n-PrO;R5=n-PrO;R6=n- Q-1 Q-2 Q-3 Q-4 Q-5
PrO;681 A=(CH2)3;R2+R3=-CH2CH2-;R4=i-PrO;R5=i-PrO;R6=i-PrO; Q-1 Q-2 Q-3 Q-4 Q-5682 A=(CH2)3;R2+R3=-CH(Me)CH2-;R4=Et;R5=Et;R6=Et; Q-1 Q-2 Q-3 Q-4 Q-5683 A=(CH2)3;R2+R3=-CH(Me)CH2-;R4=iPr;R5=iPr;R6=ipr; Q-1 Q-2 Q-3 Q-4 Q-5684 A=(CH2)3;R2+R3=-CH(Me)CH2-;R4=Ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5685 A=(CH2)3;R2+R3=-CH(Me)CH2-;R4=tBu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5686 A=(CH2)3;R2+R3=-CH(Me)CH2-;R4=EtO;R5=EtO;R6=EtO; Q-1 Q-2 Q-3 Q-4 Q-5687 A=(CH2)3;R2+R3=-CH(Me)CH2-;R4=MeO;R5=MeO; Q-1 Q-2 Q-3 Q-4 Q-5
R6=MeO;688 A=(CH2)3;R2+R3=-CH(Me)CH2-;R4=EtO;R5=EtO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5689 A=(CH2)3;R2+R3=-CH(Me)CH2-;R4=EtO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5690 A=(CH2)3;R2+R3=-CH(Me)CH2-;R4=n-PrO;R5=n-prO;R6=n- Q-1 Q-2 Q-3 Q-4 Q-5
PrO;691 A=(CH2)3;R2+R3=-CH(Me)CH2-;R4=i-PrO;R5=i-PrO;R6=i- Q-1 Q-2 Q-3 Q-4 Q-5
PrO;692 A=(CH2)4;R2+R3=-CH2CH2-;R4=Et;R5=Et;R6=Et; Q-1 Q-2 Q-3 Q-4 Q-5693 A=(CH2)4;R2+R3=-CH2CH2-;R4=EtO;R5=EtO;R6=EtO; Q-1 Q-2 Q-3 Q-4 Q-5694 A=(CH2)4;R2+R3=-CH2CH2-;R4=MeO;R5=MeO;R6=MeO; Q-1 Q-2 Q-3 Q-4 Q-5695 A=(CH2)4;R2+R3=-CH2CH2-;R4=EtO;R5=EtO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5696 A=(CH2)4;R2+R3=-CH(Me)CH2-;R4=Et;R5=Et;R6=Et; Q-1 Q-2 Q-3 Q-4 Q-5697 A=(CH2)4;R2+R3=-CH(Me)CH2-;R4=EtO;R5=EtO;R6=EtO; Q-1 Q-2 Q-3 Q-4 Q-5698 A=(CH2)4;R2+R3=-CH(Me)CH2-;R4=MeO;R5=MeO; Q-1 Q-2 Q-3 Q-4 Q-5
R6=MeO;699 A=(CH2)4;R2+R3=-CH(Me)CH2-;R4=EtO;R5=EtO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5700 A=CH2;R2+R3=-(CH2)3-;R4=Me;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5701 A=CH2;R2+R3=-(CH2)3-;R4=t-Bu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5702 A=CH2;R2+R3=-(CH2)3-;R4=Ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5703 A=CH2;R2+R3=-(CH2)3-;R4=i-Pr;R5=i-Pr;R6=i-Pr; Q-1 Q-2 Q-3 Q-4 Q-5704 A=CH2;R2+R3=-(CH2)3-;R4=t-Bu;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5705 A=CH2;R2+R3=-(CH2)3-;R4=Ph;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5706 A=CH2;R2+R3=-(CH2)3-;R4=Et;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5707 A=CH2;R2+R3=-(CH2)3-;R4=CH2CH;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5708 A=CH2;R2+R3=-(CH2)3-;R4=CH2CHCH2;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5709 A=CH2;R2+R3=-(CH2)3-;R4=EtO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5710 A=CH2;R2+R3=-(CH2)3-;R4=i-PrO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5711 A=CH2;R2+R3=-(CH2)3-;R4=EtO;R5=EtO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5712 A=CH2;R2+R3=-(CH2)3-;R4=i-PrO;R5=i-PrO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5713 A=CH2;R2+R3=-(CH2)3-;R4=EtO;R5=EtO;R6=EtO; Q-1 Q-2 Q-3 Q-4 Q-5714 A=CH2;R2+R3=-(CH2)3-;R4=MeO;R5=MeO;R6=MeO; Q-1 Q-2 Q-3 Q-4 Q-5715 A=CH2;R2+R3=-(CH2)3-;R4=MeO;R5=MeO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5716 A=CH2;R2+R3=-(CH2)3-;R4=MeO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5717 A=CH2;R2+R3=-(CH2)3-;R4=H;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5718 A=CH2;R2+R3=-(CH2)3-;R4=H;R5=Et;R6=Et; Q-1 Q-2 Q-3 Q-4 Q-5719 A=CH2CH2;R2+R3=-(CH2)3-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5720 A=(CH2)3;R2+R3=-(CH2)3-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5721 A=CH2CHCH;R2+R3=-(CH2)3-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5722 A=CH2CC;R2+R3=-(CH2)3-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5723 A=CH2CH2CHCH;R2+R3=-(CH2)3-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5724 A=CH2CH2CC;R2+R3=-(CH2)3-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5725 A=o-Ph;R2+R3=-(CH2)3-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5726 A=m-Ph;R2+R3=-(CH2)3-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5727 A=p-Ph;R2+R3=-(CH2)3-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5728 A=(CH2)3;R2+R3=-(CH2)3-;R4=Et;R5=Et;R6=Et; Q-1 Q-2 Q-3 Q-4 Q-5729 A=(CH2)3;R2+R3=-(CH2)3-;R4=iPr;R5=iPr;R6=iPr; Q-1 Q-2 Q-3 Q-4 Q-5730 A=(CH2)3;R2+R3=-(CH2)3-;R4=Ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5731 A=(CH2)3;R2+R3=-(CH2)3-;R4=tBu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5732 A=(CH2)3;R2+R3=-(CH2)3-;R4=EtO;R5=EtO;R6=EtO; Q-1 Q-2 Q-3 Q-4 Q-5733 A=(CH2)3;R2+R3=-(CH2)3-;R4=MeO;R5=MeO;R6=MeO; Q-1 Q-2 Q-3 Q-4 Q-5734 A=(CH2)3;R2+R3=-(CH2)3-;R4=EtO;R5=EtO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5735 A=(CH2)3;R2+R3=-(CH2)3-;R4=EtO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5736 A=(CH2)3;R2+R3=-(CH2)3-;R4=n-PrO;R5=n-PrO;R6=n-PrO; Q-1 Q-2 Q-3 Q-4 Q-5737 A=(CH2)3;R2+R3=-(CH2)3-;R4=i-PrO;R5=i-PrO;R6=i-PrO; Q-1 Q-2 Q-3 Q-4 Q-5738 A=(CH2)4;R2+R3=-(CH2)3-;R4=Et;R5=Et;R6=Et; Q-1 Q-2 Q-3 Q-4 Q-5739 A=(CH2)4;R2+R3=-(CH2)3-;R4=EtO;R5=EtO;R6=EtO; Q-1 Q-2 Q-3 Q-4 Q-5740 A=(CH2)4;R2+R3=-(CH2)3-;R4=MeO;R5=MeO;R6=MeO; Q-1 Q-2 Q-3 Q-4 Q-5741 A=(CH2)4;R2+R3=-(CH2)3-;R4=EtO;R5=EtO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5742 A=(CH2)3;R2=Me;R3=Me;R4=Et;R5=Et;R6=Et; Q-1 Q-2 Q-3 Q-4 Q-5743 A=(CH2)3;R2=Me;R3=Me;R4=Ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5744 A=(CH2)3;R2=Me;R3=Me;R4=tBu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5745 A=(CH2)3;R2=Me;R3=Me;R4=EtO;R5=EtO;R6=EtO; Q-1 Q-2 Q-3 Q-4 Q-5746 A=(CH2)3;R2=Me;R3=Me;R4=MeO;R5=MeO;R6=MeO; Q-1 Q-2 Q-3 Q-4 Q-5747 A=(CH2)3;R2=Et;R3=Me;R4=Et;R5=Et;R6=Et; Q-1 Q-2 Q-3 Q-4 Q-5748 A=(CH2)3;R2=Et;R3=Me;R4=Ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5S749 A=(CH2)3;R2=Et;R3=Me;R4=tBu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5750 A=(CH2)3;R2=Et;R3=Me;R4=EtO;R5=EtO;R6=EtO; Q-1 Q-2 Q-3 Q-4 Q-5751 A=(CH2)3;R2=Et;R3=Me;R4=MeO;R5=MeO;R6=MeO; Q-1 Q-2 Q-3 Q-4 Q-5752 A=(CH2)4;R2=Me;R3=Me;R4=Ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5753 A=(CH2)4;R2=Me;R3=Me;R4=tBu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5754 A=(CH2)4;R2=Et;R3=Me;R4=Ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5755 A=(CH2)4;R2=Et;R3=Me;R4=tBu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5756 A=(CH2)4;R2+R3=CH2CH2;R4=Me3Si;R5=Me3Si;R6=Me3Si; Q-1 Q-2 Q-3 Q-4 Q-5757 A=(CH2)3;R2+R3=CH2CH2;R4=Me3Si;R5=Me3Si;R6=Me3Si; Q-1 Q-2 Q-3 Q-4 Q-5758 A=(CH2)3;R2+R3=CH2CH2;R4=Me;R5=Me;R6=Me3SiCH2; Q-1 Q-2 Q-3 Q-4 Q-5759 A=(CH2)3;R2+R3=CH2CH2;R4=Me;R5=Me;R6=Me3SiCH2O; Q-1 Q-2 Q-3 Q-4 Q-5760 A=(CH2)3;R2+R3=CH2CH2;R4=Me;R5=Me; Q-1 Q-2 Q-3 Q-4 Q-5
R6=Me3SiCH2CH2O;761 A=CH2)3;R2+R3=CH2CH2;R4=Me;R5=Me; Q-1 Q-2 Q-3 Q-4 Q-5
R6=Me3SiCH2CH2S;762 A=(CH2)3;R2+R3=CH2CH2;R4=Me3SiCH2O; Q-1 Q-2 Q-3 Q-4 Q-5
R5=Me3SiCH2O;R6=Me3SiCH2O;763 A=(CH2)3;R2+R3=CH2CH2;R4=Me3Si(CH2)2O; Q-1 Q-2 Q-3 Q-4 Q-5
R5=Me3Si(CH2)2O;R6=Me3Si(CH2)2O;764 A=(CH2)3;R2+R3=CH2CH2;R4=MeS;R5=MeS;R6=MeS; Q-1 Q-2 Q-3 Q-4 Q-5765 A=(CH2)3;R2+R3=CH2CH2;R4=Ph;R5=Ph;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5766 A=(CH2)3;R2+R3=CH2CH2;R4=nBu;R5=nBu;R6=nBu; Q-1 Q-2 Q-3 Q-4 Q-5767 A=(CH2)3;R2+R3=CH2CH2;R4=Me;R5=Me3SiCH2; Q-1 Q-2 Q-3 Q-4 Q-5
R6=Me3SiCH2;768 A=CH2;R2=H;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5769 A=CH2;R2=Me;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5770 A=CH2;R2=Et;R3=Et;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5771 A=CH2;R2+R3=-CH2CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5772 A=CH2;R2+R3=CH(Me)CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5
栏
1 2 3 4 5773 A=直接键;R2=H;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5774 A=直接键;R2=H;R3=Me;R4=t-Bu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5775 A=直接键;R2=H;R3=Me;R4=Ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5776 A=直接键;R2=H;R3=Me;R4=i-Pr;R5=i-Pr;R6=i-Pr; Q-1 Q-2 Q-3 Q-4 Q-5777 A=直接键;R2=H;R3=Me;R4=t-Bu;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5778 A=直接键;R2=H;R3=Me;R4=Ph;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5779 A=CH2;R2=H;R3=Me;R4=t-Bu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5512 A=CH2;R2=H;R3=Me;R4=Ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5513 A=CH2;R2=H;R3=Me;R4=i-Pr;R5=i-Pr;R6=i-Pr; Q-1 Q-2 Q-3 Q-4 Q-5514 A=CH2;R2=H;R3=Me;R4=t-Bu;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5515 A=CH2;R2=H;R3=Me;R4=Ph;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5516 A=CH2;R2=H;R3=Me;R4=Et;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5517 A=CH2;R2=H;R3=Me;R4=CH2CH;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5518 A=CH2;R2=H;R3=Me;R4=CH2CHCH2;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5519 A=CH2;R2=H;R3=Me;R4=EtO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5780 A=CH2;R2=H;R3=Me;R4=i-PrO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5781 A=CH2;R2=H;R3=Me;R4=EtO;R5=EtO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5782 A=CH2;R2=H;R3=Me;R4=i-PrO;R5=i-PrO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5783 A=CH2;R2=H;R3=Me;R4=EtO;R5=EtO;R6=EtO; Q-1 Q-2 Q-3 Q-4 Q-5784 A=CH2;R2=H;R3=Me;R4=i-PrO;R5=i-PrO;R6=i-PrO; Q-1 Q-2 Q-3 Q-4 Q-5785 A=CH2;R2=H;R3=Me;R4=H;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5786 A=CH2;R2=H;R3=Me;R4=H;R5=Et;R6=Et; Q-1 Q-2 Q-3 Q-4 Q-5787 A=CH2CH2;R2=H;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5788 A=(CH2)3;R2=H;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5789 A=CH2CHCH;R2=H;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5790 A=CH2CC;R2=H;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5791 A=CH2CH2CHCH;R2=H;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5792 A=CH2CH2CC;R2=H;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5793 A=o-Ph;R2=H;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5794 A=m-Ph;R2=H;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5795 A=p-Ph;R2=H;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5796 A=直接键;R2=Me;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5797 A=直接键;R2=Me;R3=Me;R4=t-Bu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5798 A=直接键;R2=Me;R3=Me;R4=Ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5799 A=直接键;R2=Me;R3=Me;R4=i-Pr;R5=i-Pr;R6=i-Pr; Q-1 Q-2 Q-3 Q-4 Q-5800 A=直接键;R2=Me;R3=Me;R4=t-Bu;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5801 A=直接键;R2=Me;R3=Me;R4=Ph;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5802 A=直接键;R2=H;R3=Me;R4=Me;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5803 A=CH2;R2=H;R3=Me;R4=Me;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5804 A=CH2;R2=Me;R3=Me;R4=Me;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5805 A=CH2;R2=Me;R3=Me;R4=t-Bu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5806 A=CH2;R2=Me;R3=Me;R4=Ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5807 A=CH2;R2=Me;R3=Me;R4=i-Pr;R5=i-Pr;R6=i-Pr; Q-1 Q-2 Q-3 Q-4 Q-5808 A=CH2;R2=Me;R3=Me;R4=t-Bu;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5809 A=CH2;R2=Me;R3=Me;R4=Ph;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5810 A=CH2;R2=Me;R3=Me;R4=Et;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5811 A=CH2;R2=Me;R3=Me;R4=CH2CH;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5812 A=CH2;R2=Me;R3=Me;R4=CH2CHCH2;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5813 A=CH2;R2=Me;R3=Me;R4=EtO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5814 A=CH2;R2=Me;R3=Me;R4=i-PrO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5815 A=CH2;R2=Me;R3=Me;R4=EtO;R5=EtO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5816 A=CH2;R2=Me;R3=Me;R4=i-PrO;R5=i-PrO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5817 A=CH2;R2=Me;R3=Me;R4=EtO;R5=EtO;R6=EtO; Q-1 Q-2 Q-3 Q-4 Q-5818 A=CH2;R2=Me;R3=Me;R4=MeO;R5=MeO;R6=MeO; Q-1 Q-2 Q-3 Q-4 Q-5819 A=CH2;R2=Me;R3=Me;R4=MeO;R5=MeO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5820 A=CH2;R2=Me;R3=Me;R4=MeO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5821 A=CH2;R2=Me;R3=Me;R4=H;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5822 A=CH2;R2=Me;R3=Me;R4=H;R5=Et;R6=Et; Q-1 Q-2 Q-3 Q-4 Q-5823 A=CH2CH2;R2=Me;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5824 A=(CH2)3;R2=Me;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5825 A=CH2CHCH;R2=Me;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5826 A=CH2CC;R2=Me;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5827 A=CH2CH2CHCH;R2=Me;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5828 A=CH2CH2CC;R2=Me;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5829 A=o-Ph;R2=Me;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5830 A=m-Ph;R2=Me;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5831 A=p-Ph;R2=Me;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5832 A=CH2;R2=H;R3=Me;R4=MeO;R5=MeO;R6=MeO; Q-1 Q-2 Q-3 Q-4 Q-5833 A=CH2;R2=H;R3=Me;R4=MeO;R5=MeO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5834 A=CH2;R2=H;R3=Me;R4=MeO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5835 A=直接键;R2=Et;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5836 A=直接键;R2=Et;R3=Me;R4=t-Bu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5837 A=直接键;R2=Et;R3=Me;R4=Ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5838 A=直接键;R2=Et;R3=Me;R4=i-Pr;R5=i-Pr;R6=i-Pr; Q-1 Q-2 Q-3 Q-4 Q-5839 A=直接键;R2=Et;R3=Me;R4=t-Bu;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5840 A=直接键;R2=Et;R3=Me;R4=Ph;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5841 A=直接键;R2=Et;R3=Me;R4=Me;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5842 A=CH2;R2=Et;R3=Me;R4=Me;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5843 A=CH2;R2=Et;R3=Me;R4=t-Bu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5844 A=CH2;R2=Et;R3=Me;R4=Ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5845 A=CH2;R2=Et;R3=Me;R4=i-Pr;R5=i-Pr;R6=i-Pr; Q-1 Q-2 Q-3 Q-4 Q-5846 A=CH2;R2=Et;R3=Me;R4=t-Bu;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5847 A=CH2;R2=Et;R3=Me;R4=Ph;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5848 A=CH2;R2=Et;R3=Me;R4=Et;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5849 A=CH2;R2=Et;R3=Me;R4=CH2CH;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5850 A=CH2;R2=Et;R3=Me;R4=CH2CHCH2;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5851 A=CH2;R2=Et;R3=Me;R4=EtO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5852 A=CH2;R2=Et;R3=Me;R4=i-PrO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5853 A=CH2;R2=Et;R3=Me;R4=EtO;R5=EtO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5854 A=CH2;R2=Et;R3=Me;R4=i-PrO;R5=i-PrO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5855 A=CH2;R2=Et;R3=Me;R4=EtO;R5=EtO;R6=EtO; Q-1 Q-2 Q-3 Q-4 Q-5856 A=CH2;R2=Et;R3=Me;R4=MeO;R5=MeO;R6=MeO; Q-1 Q-2 Q-3 Q-4 Q-5857 A=CH2;R2=Et;R3=Me;R4=MeO;R5=MeO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5858 A=CH2;R2=Et;R3=Me;R4=MeO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5859 A=CH2;R2=Et;R3=Me;R4=H;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5860 A=CH2;R2=Et;R3=Me;R4=H;R5=Et;R6=Et; Q-1 Q-2 Q-3 Q-4 Q-5861 A=CH2CH2;R2=Et;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5862 A=(CH2)3;R2=Et;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5863 A=CH2CHCH;R2=Et;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5864 A=CH2CC;R2=Et;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5865 A=CH2CH2CHCH;R2=Et;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5866 A=CH2CH2CC;R2=Et;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5867 A=o-Ph;R2=Et;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5868 A=m-Ph;R2=Et;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5869 A=p-Ph;R2=Et;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5870 A=直接键;R2+R3=-CH2CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5871 A=直接键;R2+R3=-CH2CH2-;R4=t-Bu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5872 A=直接键;R2+R3=-CH2CH2-;R4=Ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5873 A=直接键;R2+R3=-CH2CH2-;R4=i-Pr;R5=i-Pr;R6=i-Pr; Q-1 Q-2 Q-3 Q-4 Q-5874 A=直接键;R2+R3=-CH2CH2-;R4=t-Bu;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5875 A=直接键;R2+R3=-CH2CH2-;R4=Ph;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5876 A=直接键;R2+R3=-CH2CH2-;R4=Me;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5877 A=CH2;R2+R3=-CH2CH2-;R4=Me;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5878 A=CH2;R2+R3=-CH2CH2-;R4=t-Bu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5879 A=CH2;R2+R3=-CH2CH2-;R4=ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5880 A=CH2;R2+R3=-CH2CH2-;R4=i-Pr;R5=i-pr;R6=i-Pr; Q-1 Q-2 Q-3 Q-4 Q-5881 A=CH2;R2+R3=-CH2CH2-;R4=t-Bu;R5=ph;R6=ph; Q-1 Q-2 Q-3 Q-4 Q-5882 A=CH2;R2+R3=-CH2CH2-;R4=ph;R5=ph;R6=ph; Q-1 Q-2 Q-3 Q-4 Q-5883 A=CH2;R2+R3=-CH2CH2-;R4=Et;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5884 A=CH2;R2+R3=-CH2CH2-;R4=CH2CH;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5885 A=CH2;R2+R3=-CH2CH2-;R4=CH2CHCH2;R5=Me; Q-1 Q-2 Q-3 Q-4 Q-5
R6=Me;886 A=CH2;R2+R3=-CH2CH2-;R4=EtO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5887 A=CH2;R2+R3=-CH2CH2-;R4=i-PrO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5888 A=CH2;R2+R3=-CH2CH2-;R4=EtO;R5=EtO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5889 A=CH2;R2+R3=-CH2CH2-;R4=i-PrO;R5=i-PrO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5890 A=CH2;R2+R3=-CH2CH2-;R4=EtO;R5=EtO;R6=EtO; Q-1 Q-2 Q-3 Q-4 Q-5891 A=CH2;R2+R3=-CH2CH2-;R4=MeO;R5=MeO;R6=MeO; Q-1 Q-2 Q-3 Q-4 Q-5892 A=CH2;R2+R3=-CH2CH2-;R4=MeO;R5=MeO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5893 A=CH2;R2+R3=-CH2CH2-;R4=MeO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5894 A=CH2;R2+R3=-CH2CH2-;R4=H;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5895 A=CH2;R2+R3=-CH2CH2-;R4=H;R5=Et;R6=Et; Q-1 Q-2 Q-3 Q-4 Q-5896 A=CH2CH2;R2+R3=-CH2CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5897 A=(CH2)3;R2+R3=-CH2CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5898 A=CH2CHCH;R2+R3=-CH2CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5899 A=CH2CC;R2+R3=-CH2CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5900 A=CH2CH2CHCH;R2+R3=-CH2CH2-;R4=Me;R5=Me; Q-1 Q-2 Q-3 Q-4 Q-5
R6=Me;901 A=CH2CH2CC;R2+R3=-CH2CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5902 A=o-Ph;R2+R3=-CH2CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5903 A=m-ph;R2+R3=-CH2CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5904 A=p-Ph;R2+R3=-CH2CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5905 A=直接键;R2+R3=-CH(Me)CH2-;R4=Me;R5=Me; Q-1 Q-2 Q-3 Q-4 Q-5
R6=Me;906 A=直接键;R2+R3=-CH(Me)CH2-;R4=t-Bu;R5=Me; Q-1 Q-2 Q-3 Q-4 Q-5
R6=Me;907 A=直接键;R2+R3=-CH(Me)CH2-;R4=ph;R5=Me; Q-1 Q-2 Q-3 Q-4 Q-5
R6=Me;908 A=直接键; R2+R3=-CH(Me)CH2-;R4=i-Pr;R5=i-Pr; Q-1 Q-2 Q-3 Q-4 Q-5
R6=i-Pr;909 A=直接键;R2+R3=-CH(Me)CH2-;R4=t-Bu;R5=ph; Q-1 Q-2 Q-3 Q-4 Q-5
R6=ph;910 A=直接键;R2+R3=-CH(Me)CH2-;R4=ph;R5=ph;R6=ph; Q-1 Q-2 Q-3 Q-4 Q-5911 A=直接键;R2+R3=-CH(Me)CH2-;R4=Me;R5=Ph; Q-1 Q-2 Q-3 Q-4 Q-5
R6=Ph;912 A=CH2;R2+R3=-CH(Me)CH2-;R4=Me;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5913 A=CH2;R2+R3=-CH(Me)CH2-;R4=t-Bu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5914 A=CH2;R2+R3=-CH(Me)CH2-;R4=Ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5915 A=CH2;R2+R3=-CH(Me)CH2-;R4=i-Pr;R5=i-Pr;R6=i-Pr; Q-1 Q-2 Q-3 Q-4 Q-5916 A=CH2;R2+R3=-CH(Me)CH2-;R4=t-Bu;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5917 A=CH2;R2+R3=-CH(Me)CH2-;R4=Ph;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5918 A=CH2;R2+R3=-CH(Me)CH2-;R4=Et;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5919 A=CH2;R2+R3=-CH(Me)CH2-;R4=CH2CH;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5920 A=CH2;R2+R3=-CH(Me)CH2-;R4=CH2CHCH2;R5=Me; Q-1 Q-2 Q-3 Q-4 Q-5
R6=Me;921 A=CH2;R2+R3=-CH(Me)CH2-;R4=EtO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5922 A=CH2;R2+R3=-CH(Me)CH2-;R4=i-PrO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5923 A=CH2;R2+R3=-CH(Me)CH2-;R4=EtO;R5=EtO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5924 A=CH2;R2+R3=-CH(Me)CH2-;R4=i-PrO;R5=i-PrO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5925 A=CH2;R2+R3=-CH(Me)CH2-;R4=EtO;R5=EtO;R6=EtO; Q-1 Q-2 Q-3 Q-4 Q-5926 A=CH2;R2+R3=-CH(Me)CH2-;R4=MeO;R5=MeO; Q-1 Q-2 Q-3 Q-4 Q-5
R6=MeO;927 A=CH2;R2+R3=-CH(Me)CH2-;R4=MeO;R5=MeO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5928 A=CH2;R2+R3=-CH(Me)CH2-;R4=MeO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5929 A=CH2;R2+R3=-CH(Me)CH2-;R4=H;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5930 A=CH2;R2+R3=-CH(Me)CH2-;R4=H;R5=Et;R6=Et; Q-1 Q-2 Q-3 Q-4 Q-5931 A=CH2CH2;R2+R3=-CH(Me)CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5932 A=(CH2)3;R2+R3=-CH(Me)CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5933 A=CH2CHCH;R2+R3=-CH(Me)CH2-;R4=Me;R5=Me; Q-1 Q-2 Q-3 Q-4 Q-5
R6=Me;934 A=CH2CC;R2+R3=-CH(Me)CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5935 A=CH2CH2CHCH;R2+R3=-CH(Me)CH2-;R4=Me;R5=Me; Q-1 Q-2 Q-3 Q-4 Q-5
R6=Me;936 A=CH2CH2CC;R2+R3=-CH(Me)CH2-;R4=Me;R5=Me; Q-1 Q-2 Q-3 Q-4 Q-5
R6=Me;937 A=o-Ph;R2+R3=-CH(Me)CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5938 A=m-Ph;R2+R3=-CH(Me)CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5939 A=p-Ph;R2+R3=-CH(Me)CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5940 A=(CH2)3;R2+R3=-CH2CH2-;R4=Et;R5=Et;R6=Et; Q-1 Q-2 Q-3 Q-4 Q-5941 A=(CH2)3;R2+R3=-CH2CH2-;R4=iPr;R5=iPr;R6=iPr; Q-1 Q-2 Q-3 Q-4 Q-5942 A=(CH2)3;R2+R3=-CH2CH2-;R4=Ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5943 A=(CH2)3;R2+R3=-CH2CH2-;R4=tBu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5944 A=(CH2)3;R2+R3=-CH2CH2-;R4=EtO;R5=EtO;R6=EtO; Q-1 Q-2 Q-3 Q-4 Q-5945 A=(CH2)3;R2+R3=-CH2CH2-;R4=MeO;R5=MeO;R6=MeO; Q-1 Q-2 Q-3 Q-4 Q-5946 A=(CH2)3;R2+R3=-CH2CH2-;R4=EtO;R5=EtO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5947 A=(CH2)3;R2+R3=-CH2CH2-;R4=EtO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5948 A=(CH2)3;R2+R3=-CH2CH2-;R4=n-PrO;R5=n-PrO;R6=n- Q-1 Q-2 Q-3 Q-4 Q-5
PrO;949 A=(CH2)3;R2+R3=-CH2CH2-;R4=i-PrO;R5=i-PrO;R6=i- Q-1 Q-2 Q-3 Q-4 Q-5
PrO;950 A=(CH2)3;R2+R3=-CH(Me)CH2-;R4=Et;R5=Et;R6=Et; Q-1 Q-2 Q-3 Q-4 Q-5951 A=(CH2)3;R2+R3=-CH(Me)CH2-;R4=iPr;R5=iPr;R6=iPr; Q-1 Q-2 Q-3 Q-4 Q-5952 A=(CH2)3;R2+R3=-CH(Me)CH2-;R4=Ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5953 A=(CH2)3;R2+R3=-CH(Me)CH2-;R4=tBu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5954 A=(CH2)3;R2+R3=-CH(Me)CH2-;R4=EtO;R5=EtO; Q-1 Q-2 Q-3 Q-4 Q-5
R6=EtO;955 A=(CH2)3;R2+R3=-CH(Me)CH2-;R4=MeO;R5=MeO; Q-1 Q-2 Q-3 Q-4 Q-5
R6=MeO;956 A=(CH2)3;R2+R3=-CH(Me)CH2-;R4=EtO;R5=EtO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5957 A=(CH2)3;R2+R3=-CH(Me)CH2-;R4=EtO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5958 A=(CH2)3;R2+R3=-CH(Me)CH2-;R4=n-PrO;R5=n-PrO; Q-1 Q-2 Q-3 Q-4 Q-5
R6=n-PrO;959 A=(CH2)3;R2+R3=-CH(Me)CH2-;R4=i-PrO;R5=i-PrO; Q-1 Q-2 Q-3 Q-4 Q-5
R6=i-PrO;960 A=(CH2)4;R2+R3=-CH2CH2-;R4=Et;R5=Et;R6=Et; Q-1 Q-2 Q-3 Q-4 Q-5961 A=(CH2)4;R2+R3=-CH2CH2-;R4=EtO;R5=EtO;R6=EtO; Q-1 Q-2 Q-3 Q-4 Q-5962 A=(CH2)4;R2+R3=-CH2CH2-;R4=MeO;R5=MeO;R6=MeO; Q-1 Q-2 Q-3 Q-4 Q-5963 A=(CH2)4;R2+R3=-CH2CH2-;R4=EtO;R5=EtO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5964 A=(CH2)4;R2+R3=-CH(Me)CH2-;R4=Et;R5=Et;R6=Et; Q-1 Q-2 Q-3 Q-4 Q-5965 A=(CH2)4;R2+R3=-CH(Me)CH2-;R4=EtO;R5=EtO; Q-1 Q-2 Q-3 Q-4 Q-5
R6=EtO;966 A=(CH2)4;R2+R3=-CH(Me)CH2-;R4=MeO;R5=MeO; Q-1 Q-2 Q-3 Q-4 Q-5
R6=MeO;967 A=(CH2)4;R2+R3=-CH(Me)CH2-;R4=EtO;R5=EtO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5968 A=CH2;R2+R3=-(CH2)3-;R4=Me;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5969 A=CH2;R2+R3=-(CH2)3-;R4=t-Bu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5970 A=CH2;R2+R3=-(CH2)3-;R4=ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5971 A=CH2;R2+R3=-(CH2)3-;R4=i-Pr;R5=i-Pr;R6=i-Pr; Q-1 Q-2 Q-3 Q-4 Q-5972 A=CH2;R2+R3=-(CH2)3-;R4=t-Bu;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5973 A=CH2;R2+R3=-(CH2)3-;R4=Ph;R5=Ph;R6=Ph; Q-1 Q-2 Q-3 Q-4 Q-5974 A=CH2;R2+R3=-(CH2)3-;R4=Et;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5975 A=CH2;R2+R3=-(CH2)3-;R4=CH2CH;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5976 A=CH2;R2+R3=-(CH2)3-;R4=CH2CHCH2;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5977 A=CH2;R2+R3=-(CH2)3-;R4=EtO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5978 A=CH2;R2+R3=-(CH2)3-;R4=i-PrO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5979 A=CH2;R2+R3=-(CH2)3-;R4=EtO;R5=EtO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5980 A=CH2;R2+R3=-(CH2)3-;R4=i-PrO;R5=i-PrO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5981 A=CH2;R2+R3=-(CH2)3-;R4=EtO;R5=EtO;R6=EtO; Q-1 Q-2 Q-3 Q-4 Q-5982 A=CH2;R2+R3=-(CH2)3-;R4=MeO;R5=MeO;R6=MeO; Q-1 Q-2 Q-3 Q-4 Q-5983 A=CH2;R2+R3=-(CH2)3-;R4=MeO;R5=MeO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5984 A=CH2;R2+R3=-(CH2)3-;R4=MeO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5985 A=CH2;R2+R3=-(CH2)3-;R4=H;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5986 A=CH2;R2+R3=-(CH2)3-;R4=H;R5=Et;R6=Et; Q-1 Q-2 Q-3 Q-4 Q-5987 A=CH2CH2;R2+R3=-(CH2)3-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5988 A=(CH2)3;R2+R3=-(CH2)3-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5989 A=CH2CHCH R2+R3=-(CH2)3-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5990 A=CH2CC;R2+R3=-(CH2)3-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5991 A=CH2CH2CHCH;R2+R3=-(CH2)3-;R4=Me;R5=Me; Q-1 Q-2 Q-3 Q-4 Q-5
R6=Me;992 A=CH2CH2CC;R2+R3=-(CH2)3-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5993 A=o-Ph;R2+R3=-(CH2)3-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5994 A=m-Ph;R2+R3=-(CH2)3-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5995 A=p-Ph;R2+R3=-(CH2)3-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5996 A=(CH2)3;R2+R3=-(CH2)3-;R4=Et;R5=Et;R6=Et; Q-1 Q-2 Q-3 Q-4 Q-5997 A=(CH2)3;R2+R3=-(CH2)3-;R4=iPr;R5=iPr;R6=iPr; Q-1 Q-2 Q-3 Q-4 Q-5998 A=(CH2)3;R2+R3=-(CH2)3-;R4=Ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5999 A=(CH2)3;R2+R3=-(CH2)3-;R4=tBu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-51000 A=(CH2)3;R2+R3=-(CH2)3-;R4=EtO;R5=EtO;R6=EtO; Q-1 Q-2 Q-3 Q-4 Q-51001 A=(CH2)3;R2+R3=-(CH2)3-;R4=MeO;R5=MeO;R6=MeO; Q-1 Q-2 Q-3 Q-4 Q-51002 A=(CH2)3;R2+R3=-(CH2)3-;R4=EtO;R5=EtO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-51003 A=(CH2)3;R2+R3=-(CH2)3-;R4=EtO;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-51004 A=(CH2)3;R2+R3=-(CH2)3-;R4=n-PrO;R5=n-PrO; Q-1 Q-2 Q-3 Q-4 Q-5
R6=n-PrO;1005 A=(CH2)3;R2+R3=-(CH2)3-;R4=i-PrO;R5=i-PrO; Q-1 Q-2 Q-3 Q-4 Q-5
R6=i-PrO;1006 A=(CH2)4;R2+R3=-(CH2)3-;R4=Et;R5=Et;R6=Et; Q-1 Q-2 Q-3 Q-4 Q-51007 A=(CH2)4;R2+R3=-(CH2)3-;R4=EtO;R5=EtO;R6=EtO; Q-1 Q-2 Q-3 Q-4 Q-51008 A=(CH2)4;R2+R3=-(CH2)3-;R4=MeO;R5=MeO;R6=MeO; Q-1 Q-2 Q-3 Q-4 Q-51009 A=(CH2)4;R2+R3=-(CH2)3-;R4=EtO;R5=EtO;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-51010 A=(CH2)3;R2=Me;R3=Me;R4=Et;R5=Et;R6=Et; Q-1 Q-2 Q-3 Q-4 Q-51011 A=(CH2)3;R2=Me;R3=Me;R4=Ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-51012 A=(CH2)3;R2=Me;R3=Me;R4=tBu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-51013 A=(CH2)3;R2=Me;R3=Me;R4=EtO;R5=EtO;R6=EtO; Q-1 Q-2 Q-3 Q-4 Q-51014 A=(CH2)3;R2=Me;R3=Me;R4=MeO;R5=MeO;R6=MeO; Q-1 Q-2 Q-3 Q-4 Q-51015 A=(CH2)3;R2=Et;R3=Me;R4=Et;R5=Et;R6=Et; Q-1 Q-2 Q-3 Q-4 Q-51016 A=(CH2)3;R2=Et;R3=Me;R4=Ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-51017 A=(CH2)3;R2=Et;R3=Me;R4=tBu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-51018 A=(CH2)3;R2=Et;R3=Me;R4=EtO;R5=EtO;R6=EtO; Q-1 Q-2 Q-3 Q-4 Q-51019 A=(CH2)3;R2=Et;R3=Me;R4=MeO;R5=MeO;R6=MeO; Q-1 Q-2 Q-3 Q-4 Q-51020 A=(CH2)4;R2=Me;R3=Me;R4=Ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-51021 A=(CH2)4;R2=Me;R3=Me;R4=tBu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-51022 A=(CH2)4;R2=Et;R3=Me;R4=Ph;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-51023 A=(CH2)4;R2=Et;R3=Me;R4=tBu;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-51024 A=(CH2)4;R2+R3=CH2CH2;R4=Me3Si;R5=Me3Si; Q-1 Q-2 Q-3 Q-4 Q-5
R6=Me3Si;1025 A=(CH2)3;R2+R3=CH2CH2;R4=Me3Si;R5=Me3Si; Q-1 Q-2 Q-3 Q-4 Q-5
R6=Me3Si;1026 A=(CH2)3;R2+R3=CH2CH2;R4=Me;R5=Me; Q-1 Q-2 Q-3 Q-4 Q-5
R6=Me3SiCH2;1027 A=(CH2)3;R2+R3=CH2CH2;R4=Me;R5=Me; Q-1 Q-2 Q-3 Q-4 Q-5
R6=Me3SiCH2O;1028 A=(CH2)3;R2+R3=CH2CH2;R4=Me;R5=Me; Q-1 Q-2 Q-3 Q-4 Q-5
R6=Me3SiCH2CH2O;1029 A=(CH2)3;R2+R3=CH2CH2;R4=Me;R5=Me; Q-1 Q-2 Q-3 Q-4 Q-5
R6=Me3SiCH2CH2S;1030 A=(CH2)3;R2+R3=CH2CH2;R4=Me3SiCH2O; Q-1 Q-2 Q-3 Q-4 Q-5
R5=Me3SiCH2O;R6=Me3SiCH2O;1031 A=(CH2)3;R2+R3=CH2CH2;R4=Me3Si(CH2)2O; Q-1 Q-2 Q-3 Q-4 Q-5
R5=Me3Si(CH2)2O;R6=Me3Si(CH2)2O;1032 A=(CH2)3;R2+R3=CH2CH2;R4=MeS;R5=MeS;R6=MeS; Q-1 Q-2 Q-3 Q-4 Q-51033 A=(CH2)3;R2+R3=CH2CH2;R4=Ph;R5=Ph;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-51034 A=(CH2)3;R2+R3=CH2CH2;R4=nBu;R5=nBu;R6=nBu; Q-1 Q-2 Q-3 Q-4 Q-51035 A=(CH2)3;R2+R3=CH2CH2;R4=Me;R5=Me3SiCH2; Q-1 Q-2 Q-3 Q-4 Q-5
R6=Me3SiCH2;1036 A=CH2;R2=H;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-51037 A=CH2;R2=Me;R3=Me;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-51038 A=CH2;R2=Et;R3=Et;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-51039 A=CH2;R2+R3=-CH2CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-51040 A=CH2;R2+R3=CH(Me)CH2-;R4=Me;R5=Me;R6=Me; Q-1 Q-2 Q-3 Q-4 Q-5制剂/用途
本发明的化合物通常用于带有一种包括液体或固体稀释剂的农业上适当的载体的制剂中。有用的制剂包括粉剂、颗粒、毒饵、片剂、溶液、悬浮液、乳状液、可湿的粉剂、乳油、干的飞散剂等等,它们与活性成分的物理性质、应用方式和诸如土壤类型、湿度和温度等环境因素一致。可喷雾的制剂可分散在适当的介质中,并以每公顷约一到几百升的喷淋体积使用。高强度组合物主要用作另外的制剂的中间产品。制剂典型地包含有效量的下述大约变化范围内的活性成分、稀释剂和表面活性剂,它们加起来为百分之百的重量。
重量百分比
活性成分
稀释剂
表面活性剂可湿的粉剂 5-90 0-74 1-10油悬浮液、乳状液、 5-50 40-95 0-15溶液(包括乳油)粉剂 1-25 70-99 0-15颗粒、毒饵和片剂 0.01-99 5-99.99 0-15高强度组合物 90-99 0-10 0-2
典型的固体稀释剂在Watkins,et al.,Handbook of InsecticideDust Diluent and Carriers,2nd Ed.,Dorland Books,Caldwell,NewJersey中有所描述。典型的液体稀释剂和溶剂在Marsden,Solvents Guide,2nd Ed.,Interscience,New York,1950.中有所描述。McCutcheon’sDetergents and Emulsifiers Annual,Allured Publ.Corp.,Ridgewood,New Jersey以及Sisley and Wood,Encyclopedia ofSurface Active Agents,Chemical Publ.Co.,Inc.,New York,1964列举了表面活性剂和推荐的用法。所有制剂都可以含有少量添加剂来减少泡沫、结块、腐蚀、微生物的生长等。
溶液是通过类似地混合这些成分来制备的。精细固体组合物是通过掺合以及通常如在一个锤磨机或流体能量磨粉机中研磨来制备的。水分散颗粒可以通过使一种细粉组合物凝聚来生产;例如见Cross et al.,Pesticide Formulation,Washington,D.C.,1988,pp 251-259。悬浮液是通过湿磨粉来制备的;例如见U.S.3,060,084。颗粒和片剂可以通过把活性物质喷淋到处理过的颗粒载体上或者通过凝聚技术来制备。见Browning,“Agglomeration”,Chemical Engineering,December 4,1967,pp 147-148,Perry’s Chemical Engineer’s Handbook,4thEd.,McGraw-Hill,New York,1963,第8-57页和下面的内容,以及WO 91/13546。
有关制剂技术的进一步信息,可见U.S.3,235,361第6栏第16行到第7栏第19行和实例10-41;U.S.3,309,192第5栏第43行到第7栏第62行和实例8、12、15、39、41、52、53、58、132、138-140、162-164、166、167和169-182;U.S.2,891,855第3栏第66行到第5栏第17行和实例1-4;Klingman,Weed Controlas a Science,John Wiley and Sons,Inc.,New York,1961,pp 81-96;和Hance et al.,Weed Control Handbook,8th Ed.,BlackwellScientific Publications,Oxford,1989。
在下面的实例中,所有百分率均为重量百分数,所有制剂以常规方法制备。化合物号码指的是索引表A中的化合物。
实施例A 可湿的粉剂化合物1 65.0%十二烷基酚聚乙二醇醚 2.0%木质素磺酸钠 4.0%硅铝酸钠 6.0%蒙脱土(煅烧的) 23.0%
实施例B 颗粒化合物1 10%硅镁土颗粒(低挥发性物质,0.71/0.30mm;U.S.S.No.25-50筛) 90%
实施例C 挤出片剂化合物1 25.0%无水硫酸钠 10.0%粗木质素磺酸钙 5.0%烷基萘磺酸钠 1.0%钙/镁膨润土 59.0%
实施例D 乳油
化合物1 20.0%
油溶性磺酸盐掺合物和聚氧乙烯醚的掺合物 10.0%
异佛尔酮 70.0%
本发明的化合物对一系列吃叶、吃果子、吃茎或根、吃种子的水生和土生节肢动物(术语“节肢动物”包括昆虫、小虫和线虫)具有广谱的活性,上述节肢动物是生长的和贮存的农作物、森林、温室农作物、观赏植物、苗圃农作物、贮存的食物和纤维制品、家畜、日用品、公众和动物健康的害虫。本领域中的技术人员希望并不是所有的化合物对所有害虫的所有成长阶段等同地有效。然而,本发明的所有化合物对以下害虫显示活性:鳞翅目的卵、幼虫和成虫;鞘翅目的卵、吃叶子、吃果子、吃根、吃种子幼虫和成虫;半翅目和同翅目的卵、幼虫和成虫;OrdersAcari的卵、幼虫、若虫和成虫;缨翅目、直翅目和革翅目的卵、幼虫和成虫;双翅目的卵、幼虫和成虫;线虫门的卵、幼虫和成虫。本发明的化合物对膜翅目、等翅目、蚤目、_蠊目、缨尾目和啮虫目以及属于蛛形纲和Platyhelminthes门害虫也有效。具体地说,这些化合物对以下害虫有效:南部南瓜十二星叶甲(十一星瓜叶甲)、紫莞叶蝉(Mascrostelesfascifrons)、棉子象鼻虫(棉铃象甲)、棉红蜘蛛(棉红蜘蛛)、秋粘虫(草地粘虫)、豆蚜(蚕豆蚜)、桃蚜(桃蚜)、棉蚜(棉蚜)、俄罗斯麦蚜(Diuraphis noxia)、英国谷蚜(麦长管蚜)、菸夜蛾(美洲菸夜蛾)、稻象甲(稻象甲)、稻负泥虫(稻负泥虫)、白背飞虱(白背飞虱)、大青叶蝉(黑尾叶蝉)、稻褐飞虱(稻褐飞虱)、稻灰飞虱(稻灰飞虱)、水稻螟虫(Chilo suppressalis)、稻卷叶虫(稻纵卷叶野螟)、黑稻褐蝽(稻黑蝽)、稻褐蝽(Oebalus pugnax)、稻蝽(Leptocorisa chinensis)、大针缘蝽(稻棘缘蝽)和稻绿蝽(稻绿蝽)。这些化合物对螨有效,对以下类别显示出能杀卵的,能杀幼虫的和化学杀菌剂的活性:叶螨科,包括棉叶螨、红叶螨、迈叶螨、太平洋叶螨、草莓叶螨、Byrobia rubrioculus、榆全爪螨、桔全爪螨、枥始叶螨北方亚种、始叶螨属、hicoriae、六点始叶螨、尤马始叶螨、Eotetranychusbanksi和草地小爪螨;细须螨属,包括葡萄短须螨、紫红短须螨、加州短须螨和卵形短须螨;瘿螨科,包括桔芸锈螨、桔芽瘿螨、桃刺锈螨、梨埃瘿螨和Eriophyes magniferae。更详细的害虫描述见WO 90/10623和WO 92/00673。
本发明的化合物也可以与一种或多种其它的杀虫剂、杀真菌剂、杀线虫剂、杀菌剂、杀螨剂、生长调节剂、化学杀菌剂、半化学品、驱虫剂、引诱剂、信息素、饲料兴奋剂或其它的生物活性化合物混合,形成一种具有更宽的农业保护范围的多组分农药。其它能和本发明化合物一起配制的农业保护剂的实例可简述如下:杀虫剂,比如阿弗麦菌素B、久效磷,虫螨威,杀虫威,马拉硫磷、甲基对硫磷,灭多虫,杀虫脒,二嗪农,deltamethrin,草氨酰,fenvalerate,esfenvalerate,二氯苯醚菊酯,溴丙磷,乙丙硫磷,triflumuron,diflubenzuron,蒙五一五,buprofezin,硫代二卡巴,高灭磷,谷硫磷,毒死蜱,乐果,fipromil,flufenprox,地虫磷,isofenphos,杀扑磷,甲胺磷,亚胺硫磷,磷胺,伏杀磷,抗蚜威,3911,terbufos,敌百虫,甲氧滴滴涕,bifenthrin,biphenate,cyfluthrin,tefluthrin,分扑菊酯,fluvalinate,flucythrinate,tralomethrin,imidacloprid,多聚乙醛和鱼腾酮;杀真菌剂如苯脒氯甲酯,二硫四甲基秋兰姆,十二烷基胍乙酸盐,代森锰锌,氯代森锰锌,苯菌灵,cymoxanil,fenpropidine,fenpropimorph,triadimefon,克菌丹,甲基托布津,涕必灵,藻菌灵,百菌清,氯硝胺,氨丙灵,敌灭丹,二氯苯基甲乙基二氧咪唑烷羧酸胺,oxadixyl,vinclozolin,春雷霉素,myclobatanil,tebuconazole,difenconazole,diniconazole,fluquineonazole,ipconazole,metconazole,penconazole,propiconazole,uniconazole,flutriafol,prochloraz,pyrifenox,异嘧菌醇,唑菌醇,diclobutrazol,氧氯化铜,呋氨丙灵,folpet,flusilazol,灭瘟素,diclomezine,克瘟散,富士一号,iprobenfos,mepronu,新磷甲砷,pencycuron,噻菌灵,pyroquilon,三环唑,有效霉素及flutolanil;杀线虫剂如砜灭威,克线磷和伐线丹;杀菌剂如土霉素,链霉素,和三碱基硫酸铜;杀螨剂如乐杀螨,喹甲硫酯,乙酯杀螨醇,开乐散,除螨灵,三环锡,hexythiazox,二甲苯胺藤,克螨特,tebafenpyrad,杀螨锡;以及生物制剂如使昆虫致病的细菌,病毒和真菌。
在某些情况中,与其它具有相似控制范围,而作用方式不同的节肢类动物杀虫剂混合将特别有利于抗性控制。
控制节肢动物害虫,并且通过将有效量应用一种或多种本发明的化合物施用到包括农业和/或非农业危害区的害虫的环境中,施用到保护区中或者直接用到被控制的害虫上面来达到农业的,园艺的和特殊的农作物的保护、动物和人类健康的保护。这样,本发明还包括一种控制叶生和土生节肢动物以及线虫害虫和保护农业和/或非农业农作物的方法,该方法包括将有效量应用一种或多种式I的化合物或包含至少一种这样的化合物的组合物施用到包括农业和/或非农业危害区的害虫的环境中,到保护区中或直接到被控制的害虫上面。一种优选的应用方法是喷洒。另外,这些化合物的粒状制剂可以被应用于植物叶子或土壤。其它的应用方法包括直接和残留喷洒法、空中喷洒法、种子涂覆法、微囊法、内吸吸收法、诱饵法、耳标法、丸剂法、烟雾发生器法、烟雾剂法、气溶胶法、粉尘法和许多其它的方法。本发明化合物可以掺入到被节肢动物吃掉的诱饵中或放入到比如捕集器等这样的设备中。
本发明化合物可以以其纯态形式应用,但是最常用的是一种包括一种或多种带有适当载体、稀释剂和表面活性剂的化合物以及可能地与一种取决于预计的最终用途的食物结合的制剂。一种优选的应用方法涉及喷洒一种此化合物的水分散液或精制油溶液。与喷洒油、喷洒油浓缩物、喷洒剂粘着剂、辅助剂、增效剂以及其它溶剂,比如胡椒基丁醚相结合经常会增强化合物的功效。
有效控制需要的用量将取决于下列因素:被控制的节肢动物的种类、害虫的生命循环、生活阶段、其大小、位置、年期、寄宿的作物或动物、吃料行为、成熟行为、环境湿度、温度等。在正常情况下,每公顷大约0.01到2kg活性成分的用量足以控制农业生态系统中的害虫,但是少至0.001千克/公顷的量也许是足够的,或者也许需要多至8千克/公顷。对于非农业应用,有效用量为大约1.0到50毫克/平方米,但是少至0.1毫克/平方米也许是足够的,或者也许需要多至150毫克/平方米。
下列试验表明本发明化合物对特定害虫的控制功效。“控制功效”表示抑制使食量明显减少的节肢动物演变(包括不可免的死亡)。然而,由此化合物提供的害虫控制保护不仅限于这些类别。对化合物的描述见索引表A-E。
索引表A Cmpd
R 1
R 2 +R 3
m.p.(℃)
构型(a)1 3-CH2-6-Cl-pyr -CH(CH3)CH2-(b) 112-115 外消旋的2 3-CH2-6-Cl-pyr -CH(CH3)CH2-(b) 145-147 R3 3-CH2-6-Cl-pyr -CH2CH2- 145.5-147.0 非手性的4 5-CH2-2-Cl-噻唑基 -CH2CH2- 148-151 非手性的5 5-CH2-2-Cl-噻唑基 -CH(CH3)CH2-(b) 133-137 外消旋的6 MeSCH2CH2 -CH2CH2- 105-107 非手性的7 MeSCH2CH2 -CH(CH3)CH2-(b) oil 外消旋的8 3-CH2-pyr -CH2CH2- 158.5-160.0 非手性的9 3-CH2-pyr -CH(CH3)CH2-(b) 155.0-156.5 外消旋的10 3-CH2-5.6-di-Cl-pyr -CH2CH2- 162.5-164.0 非手性的11 3-CH2-6-Cl-pyr -(CH2)3- 89-93 非手性的12 5-CH2-3-Me-异噁唑基 -CH2CH2- 116-118 非手性的Cmpd
R 1
R 2
R 3
m.p.(℃)
构型(a)13 3-CH2-6-Cl-pyr Et Me oil (手性的)(a)构型是指手性碳原子的构型。符号“R”是按照Cahn、Ingold
和Prelog方法定义的。“外消旋的”定义为一种基本上等量的R
和S对映体的混合物。“非手性的”表示不含手性中心的化合物。(b)CH碳原子连接到含R1的氮原子上。
索引表B Cmpd
R
A
R 4
R 5
R 6
m.p.(℃)
构型(a)14 H (CH2)3 EtO EtO EtO 140-142 非手性的15 H (CH2)3 MeO MeO MeO 87-90 非手性的16 H (CH2)3 EtO EtO Me 112-114 非手性的17 H (CH2)4 EtO EtO Me 97-98 非手性的18 Me (CH2)3 EtO EtO EtO 138-140 外消旋的19 H CH2 Ph Me Me 147-149 非手性的20 Me CH2 Ph Me Me oil 外消旋的21 Me CH2 Ph Me Me oil R22 Me (CH2)3 Ph Me Me 81-85 外消旋的23 H (CH2)3 Ph Me Me 133-136 非手性的24 H (CH2)3 tBu Me Me 152-153 非手性的25 H (CH2)3 Et Et Et 148-150 非手性的26 H (CH2)3 Ph Ph Ph 144-149 非手性的(a)构型是指手性碳原子的构型。符号“R”是按照Cahn、Ingold
和Prelog方法定义的。“外消旋的”定义为一种基本上等量的R
和S对映体的混合物。非手性表示不含手性中心的化合物。
下面额外的符号用来表示表C中Q的各种实例:Q-1=6-氯-3-吡啶基、Q-2=5,6-二氯-3-吡啶基、Q-3=2-氯-5-噻唑基、和Q-5=CH3SCH2-。
索引表C Cmpd
Q
R
A
X
R 4
R 5
R 6
m.p.(℃)27 Q-3 H CH2 Si Ph Me Me 油28 Q-1 H (CH2)3Ge nBu nBu nBu 104-10629 Q-5 Me(a) CH2 Si Ph Me Me 油30 Q-1 H CH2 Si Et Me Me 152.5-154.031 Q-1 Me(b) CH2 Si Et Me Me 108-11032 Q-2 H CH2 Si Et Me Me 134-14133 Q-2 H CH2 Si Et Me Me 98-104(a)外消旋的(b)R-对映体
索引表D Cmpd
R 1
A
X
R 4
R 5
R 6
m.p.(℃)34 3-CH2-6-Cl-pyr CH2 Si Et Me Me 115-11735 3-CH2-6-Cl-pyr CH2 Si Ph Me Me 油
索引表E 1 H NMR(CDCl 3 )数据 (a) Cmpd.No.7 4.47-4.36(m,1H),4.02(d,2H),3.90-3.73(m,4H),3.49(dt,1H),
3.22(dd,1H),2.82-2.68(m,2H),2.12(s,3H),2.08(ABq,2H),
1.39(d,3H),0.10(s,9H).13 8.30(d,1H),7.69(dd,1H),7.32(d,1H),4.50(d,1H),4.18(d,1H),
3.60-3.40(m,5H),3.32-3.21(m,1H),2.99(s,3H),1.97(s,2H),1.19
t,3H),0.10(s,9H).20 (300MHz)8.31(d,1H),7.78(dd,1H),7.50(dd,2H),7.40-7.32(m,3H),
7.30(d,1H),5.08(d,1H),4.65(d,1H),3.9-3.65(m,5H),3.18(t,1H),
2.83(dd,1H),2.19(ABq,2H),1.19(d,3H),0.39(s,3H),0.35(s,3H).21 (300MHz)8.32(d,1H),7.79(dd,1H),7.52(dd,2H),7.42-7.35(m,3H),
7.30(d,1H),5.07(d,1H),4.66(d,1H),3.9-3.65(m,5H),3.17(t,1H),
2.83(dd,1H),2.19(ABq,2H),1.19(d,3H),0.39(s,3H),0.35(s,3H).22 (300MHz)8.30(s,1H),7.80(d,1H),7.50-7.40(m,2H),7.40-7.30
(m,3H),7.30(d,1H),5.00(d,1H),4.75(d,1H),3.90-3.65(m,6H),
3.20-3.10(m,1H),2.40-2.30(m,2H),1.60-1.45(m,2H),1.24(d,3H),
0.80-0.70(m,2H),0.28(s,6H).26 8.35(s,1H),7.85(d,1H),7.60(d,1H),7.55-7.50(m,6H),7.43-7.35
(m,9H),4.79(s,2H),3.84(s,2H),3.78(s,2H),3.51(s,4H),2.5(t,2H),
1.80-1.65(m,2H),1.45-1.35(m,2H).27 (300MHz)7.52(dd,2H),7.45(s,1H),7.42-7.35(m,3H),4.93(s,2H),
3.81(s,2H),3.78(s,2H),3.54(变形的t,2H),3.14(变形的t,2H),
2.28(s,2H),0.38(s,6H).29 (300MHz)7.57(dd,2H),7.39(m,2H),4.40(dt?,1H),3.93-3.82(m,4H),
3.72(d,1H),3.45(m,1H),3.34(t,1H),2.85(dd,1H),2.8-2.6(m,2H),
2.35(ABq,2H),2.10(s,3H),1.3 1(d,3H),0.40(s,3H),0.36(s,3H).32 (300MHz)8.26(s,1H),8.07(s,1H),4.85(s,2H),3.91(s,2H),3.78
(s,2H),3.63(m,4H),2.07(s,2H),0.96(t,3H),0.58(q,2H),0.09(s,6H).33 (300MHz)8.27(s,1H),8.05(s,1H),7.55(m,2H),7.40(m,3H),4.82
(s,2H),3.82(s,2H),3.79(s,2H),3.46(m,2H),3.15(变形的t,2H),
2.31(s,2H),0.40(s,6H).35 8.30(s,1H),7.64(明显的d,1H),7.54(m,2H),7.38(m,3H),7.31
(d,1H),4.59(br s,2H),3.72(m,4H),3.27(m,2H),3.11(t,2H),2.17
(s,2H),1.97(m,2H),0.39(s,6H).(a)除非特别说明,波谱是在CDCl3中、400MHz下获得的。化学位
移值(δ)是相对于Me4Si=0.00ppm的数值。s=单峰、d-
双峰、t=三重峰、q=四重峰、m=多重峰。
试验A 秋粘虫
制备了每个由一种H.I.S.(高耐冲击苯乙烯)托盘组成的、具有16个测定池的试验单元。将湿滤纸和大约8cm2利马豆叶置于12个测定池中。将0.5cm厚的小麦胚芽食物层置于余下的4个测定池中。十五至二十个秋粘虫第三龄幼虫(草地贪夜蛾)放入一个230mL(8盎司)塑料杯中。将每个试验化合物在75/25的丙酮/蒸馏水溶剂中的溶液喷入到托盘和塑料杯中。喷洒是通过把托盘和杯子传递到一个直接位于一个扁扇形液压喷头下面的输送带上来完成的,该喷头以速率每公顷0.55kg活性成分(大约每英亩0.5英磅)、在207kPa(30p.s.i.)下排放雾液。将害虫从230mL杯子转移到H.I.S.托盘(每个测定池一个害虫)。托盘加盖,并在27℃和50%相对湿度下保持48h,然后对带有利马豆叶的十二个测定池进行记录。在测验的化合物中,下列给出80%或更高的控制有效性水平:1、2、3、4*、5*、6、14*、19*、27*、28*、29*、30*、31*和27*。
* -在0.14kg/ha下测得的。
试验B 南方南瓜十二星叶甲
制备了每个由含有2.54cm2(1平方英寸)小麦胚芽食物栓的230mL(8盎司)塑料杯的试验单元。这些试验单元按试验A所述方法用单个的试验化合物溶液喷洒。杯上的喷液干燥后,将五个第二龄南方南瓜十二星叶甲幼虫(瓜十一星叶甲)放入每个杯子中。这些杯子在27℃和50%相对湿度下保持48h,然后记录死亡率读数。测验的化合物中,下列给出了80%或更高的控制有效性水平:1、2、3、4、5、6、7、8、9、10、11、13、14*、15*、16*、20*、21*、22*、24*、26*、27*、28*、30*、32*和34*。
*-在0.14kg/ha下测得的。
试验C 六点叶蝉
制备了一系列的350mL(12盎司)杯子试验单元,每个含有在2.54cm(1英寸)消毒土壤层中的燕麦(Avena sativa)苗。这些试验单元按照试验A所述方法用单个的试验化合物溶液喷洒。燕麦喷液干后,将10至15个六点叶蝉成虫(Mascrosteles fascifrons)吸入每个杯子中。这些杯子用带通气孔的盖子盖上,并在27℃,50%相对湿度下保持48h,然后记录死亡率读数。试验的化合物中,下列给出了80%或更高的死亡率水平:1、2、3、4、5、6、7、10、11、13、14*和16*、19*、20*、21*、23*、24*、25*、26*、27*、28*、29*、30*、31*、32*和34*。
*-在0.14kg/ha下测得的。
试验D 棉子象鼻虫
制备了由含有五个棉子象鼻虫(棉铃象)的260mL(9盎司)杯子组成的试验单元。这些试验单元按照试验A中所述的方法用单个的试验化合物溶液喷洒。每个杯子用一个带通气孔的盖子盖上,并在27℃、50%相对湿度下保持48h,然后记录死亡率读数。试验的化合物中,下列给出了80%或更高的死亡率水平:2、3、4、5、6、7、10和16*。
*-在0.14kg/ha下测得的。
试验E 蚕豆蚜
单个的旱金莲叶子用10至15个蚜虫(甜菜蚜的所有形态和生长阶段)侵蚀,并且如在试验A中所述,对它们的下侧面喷洒。然后将叶子放置于含有4mL糖溶液(大约每升1.4g)的直径为0.94cm(3/8英寸)的小瓶内,并且用一个29mL(1盎司)的透明塑料杯盖上,从而防止从叶子上落下的蚜虫跑掉。这些试验单元在27℃、50%相对湿度下保持48h,然后记录死亡率读数。试验的化合物中,下列给出了80%或更高的死亡率水平:1、2、3、4、5、6、7、8、9、10、13、14*、15*和16*、19*、21*、22*、23*、24*、25*、26*、28*、29*、30*、31*、32*和34*。
*-在0.14kg/ha下测得的。
试验F 对大青叶蝉若虫的接触活性
将三颗1.5叶发育阶段和大约10cm高稻(Oryza sativa)幼苗移植到一个含有Kumiai Brown人工土壤的14mL(1/2盎司)塑料杯中。然后把七毫升蒸馏水加入杯中。试验化学品是通过首先把化学品溶解在丙酮中,然后加入水来制备的,得到最终的试验浓度为75∶25(丙酮∶水)。然后将四个塑料杯,每个杯子重复作一个同样的样品,放在一个喷室转台上。这些杯子然后用50mL此化学品溶液,在2.0kg/cm2压力下用气雾化喷头喷淋45秒钟。在此45秒钟喷雾间隔中,转台完成7.5转。应用化学品之后,将处理后的杯子放在一个带通气孔的罩中干燥大约2h。干燥之后,将杯子放入锥形试验单元中,并且土壤表面覆盖有2到3mm石英砂。将8至10个第三龄的大青叶蝉若虫(Nephotettixcineticeps)用一个吸管移入这些试验单元中。这些试验单元保持在27℃、65%相对湿度下。记录24和48小时侵蚀后活和死的若虫的数量。把不能走动的害虫列为死的一类。试验的化合物中,下列给出了在48h,用量相当于0.05千克/公顷下80%或更高的死亡率水平:1、2、 3、4、5、6、7和8。
试验G 对稻褐飞虱的接触活性
将三颗1.5叶发育阶段和大约10cm高稻(Oryza sativa)幼苗移植到一个含有Kumiai Brown人工土壤的14mL(1/2盎司)塑料杯中。然后往杯中加入七毫升蒸馏水。试验化学品是通过首先把化学品溶解在丙酮中,然后加入水制得的,得到最终试验浓度为75∶25(丙酮∶水)。然后将四个塑料杯,每个杯子重复作一个同样的样品,放在一个喷室转台上。这些杯子用50mL化学品溶液在2.0kg/cm2压力下用气雾化喷头喷淋45秒钟。转台在45秒喷雾间隔中完成7.5转。应用化学品后,将处理后的杯子放在一个带通气孔的罩中干燥大约2h。干燥之后,将杯子放入锥形试验单元中,并且土壤表面覆盖有2至3mm石英砂。然后将8至10个第三龄的稻褐飞虱(Nilaparvata lagens)若虫用一个吸管移入试验单元中。这些试验单元保持在27℃、65%相对湿度下。记录24和48h侵蚀后活和死的若虫的数量。把不能走动的害虫列为死的一类。试验的化合物中,下列给出了在48h,用量相当于0.05千克/公顷下80%或更高的死亡率水平:1、2、3、4、5、6、7、8和9。
Claims (8)
X选自Si和Ge;
A选自C1-C20亚烷基,C2-C20亚链烯基,C2-C20亚炔
基,C3-C8亚环烷基,C7-C10芳基亚烷基和亚苯基,每
个基团任意地被1-3个独立地选自W的取代基取代;或
者A是直接键。
R1和R3独立地选自H,C1-C10烷基,C2-C10链烯基或C2
-C10炔基,每个基团任意地被1-2个独立地选自卤素,
CN,C(O)R7,C(S)R7,NO2,OH,SC(O)R7,
SC(S)R7,OC(O)R7,OC(S)R7,NR8C(O)R7,
NR8C(S)R7,SH,Si(R8)(R9)(R10),C1
-C4烷氧基,C1-C4卤烷氧基,C1-C4烷基硫基,C1
-C4烷基氨基,C2-C8二烷基氨基,C3-C8环烷基和任
意地被1-3个独立地选自W1的取代基取代的苯基;任意地
被1-3个独立地选自卤素,C1-C2烷基和C1-C2卤烷
基取代的C3-C8环烷基;C(O)R11;C(S)R11;
任意地被1-3个独立地选自W1的取代基取代的苯基;被一
个通过C或N连接的,含有1-4个独立地选自0-4个氮,
0-1个氧和0-1个硫杂原子的5或6元芳香环取代的C1
-C3烷基,上述芳环任意地被1-3个独立地选自W1的取
代基取代;和一个通过C或N连接的、含有1至4个独立地
选自0-4个氮,0-1个氧和0-1个硫杂原子的5或6
元芳香环,该环任意地被1-3个独立地选自W1的取代基取
代;R2选自H,C1-C6烷基,C1-C6卤烷基,C2-C6链烯基,C2-C6卤代链烯基,C2-C6炔基,C2-C6卤代炔基,C3-C7环烷基,C3-C7卤代环烷基和C4-C7环烷基烷基,每个基团任意地被1-3个独立地选自W的取代基取代;或R2和R3可被一起看作CH2CH2和CH2CH2CH2,每个基团任意地被1-2个CH3取代;R4选自H和C3-C6三烷基甲硅烷基;或R4选自C1-C10烷基,C2-C10链烯基,C2-C10炔基,C1-C10烷氧基,C1-C10烷基硫基,苯基,苯氧基,苯基硫基和萘基,每个基团任意地被1-3个独立地选自W1的取代基取代;R5和R6独立地选自C1-C10烷基,C2-C10链烯基,C2-C10炔基,C1-C10烷氧基,C1-C10烷基硫基,苯基,苯氧基,苯基硫基和萘基,每个基团任意地被1-3个独立地选自W1的取代基取代;OH和C3-C6三烷基甲硅烷基;R7选自H,NH2,OH,C1-C6烷基、C1-C6卤代烷基,C1-C6烷氧基,C1-C6卤代烷氧基,C1-C6烷基硫基,C1-C4烷基氨基,C2-C8二烷基氨基和任意地被1-3个独立地选自W1的取代基取代的苯基;R8为H;或R8选自C1-C10烷基,C2-C10链烯基,C2-C10炔基,C1-C10烷氧基,苯氧基,苯基和萘基,每个基团任意地被1-3个独立地选自W1的取代基取代;R9和R10独立地选自C1-C10烷基,C2-C10链烯基,C2-C10炔基,C1-C10烷氧基,苯氧基,苯基和萘基,每个基团任意地被1-3个独立地选自W1的取代基取代;和OH;R11选自H,NH2,OH,C1-C6烷基,C1-C6卤代烷基,C1-C6烷氧基,C1-C6卤代烷氧基,C1-C2烷基硫基,C1-C4烷基氨基,C2-C8二烷基氨基和任意地被1-3个独立地选自W1的取代基取代的苯基;W选自卤素,CN,NO2,OH,C1-C6烷基,C1-C6卤代烷基,C1-C6烷氧基和C1-C6卤代烷氧基;和W1选自卤素,CN,NO2,C1-C2烷基和C1-C2卤代烷基,C1-C2烷氧基,C1-C2卤代烷氧基,C1-C2烷基硫基,
C1-C2卤代烷基硫基,C1-C2烷基磺酰基,C1-C2卤代
烷基磺酰基,C1-C4烷基氨基,C2-C8二烷基氨基和C3
-C6三烷基甲硅烷基;
2.按照权利要求1的化合物,其中:A是C1-C6亚烷基;R1是被一个通过C或N连结的、含有1至4个独立地选自0-4
个氮,0-1个氧和0-1个硫杂原子的5或6元芳香环取代
的C1-C3烷基,上述芳香环任意地被1-3个独立地选自W1
的取代基取代;R4选自C1-C10烷基和苯基,每个基团任意地被1-3个独立
地选自W1的取代基取代;R5和R6独立地选自C1-C10烷基和苯基,每个基团任意地被1
-3个独立地选自W1的取代基取代;和W1选自卤素和C1-C2卤代烷基。
3.按照权利要求2的化合物,其中:X是Si;R1是被吡啶基、噻唑或异噁唑取代的CH2,上述环任意地被1-
2个卤素或1-2个甲基取代;R2和R3被一起看作CH2CH2或CH2CH2CH2,每个基团任意地被1
-2个CH3取代;和R4、R5和R6是C1-C3烷基,C1-C3烷氧基和苯基。
4.按照权利要求2的化合物,其中:X是Si;R1是被吡啶基、噻唑或异噁唑取代的CH2,上述环任意地被1-
2个卤素取代;R2选自H和C1-C3烷基,和R4、R5和R6是C1-C3烷基,C1-C3烷氧基和苯基。
5.按照权利要求3的化合物,它是:1-[(6-氯-3-吡啶基)甲基]-1,2,3,5,6,7-六氢-2-甲
基-8-硝基-6-[(三甲基甲硅烷基)甲基]咪唑并[1,2-c]
嘧啶;
6.按照权利要求3的化合物,它是:
1-[(6-氯-3-吡啶基)甲基]-1,2,3,5,6,7-六氢-8-甲
硝基-6-[(三甲基甲硅烷基)甲基]咪唑并[1,2-c]嘧啶。
7.一种节肢动物的杀虫剂组合物,包括杀节肢动物有效量的按照权利要求1的化合物和其载体。
8.一种控制节肢动物的方法,包括使节肢动物或其环境与杀节肢动物有效量的按照权利要求1的化合物接触。
Applications Claiming Priority (4)
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US19421494A | 1994-02-09 | 1994-02-09 | |
US27859794A | 1994-07-21 | 1994-07-21 | |
US08/194,214 | 1994-07-21 | ||
US08/278,597 | 1994-07-21 |
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Publication Number | Publication Date |
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CN1140452A true CN1140452A (zh) | 1997-01-15 |
Family
ID=26889795
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Application Number | Title | Priority Date | Filing Date |
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CN95191561.4A Pending CN1140452A (zh) | 1994-02-09 | 1995-02-09 | 节肢动物杀虫剂四氢嘧啶 |
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EP (1) | EP0743947A1 (zh) |
JP (1) | JPH09507676A (zh) |
CN (1) | CN1140452A (zh) |
AU (1) | AU679350B2 (zh) |
BR (1) | BR9506960A (zh) |
HU (1) | HUT76814A (zh) |
IL (1) | IL112577A0 (zh) |
MX (1) | MX9603273A (zh) |
PL (1) | PL315813A1 (zh) |
WO (1) | WO1995021846A1 (zh) |
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US6828275B2 (en) | 1998-06-23 | 2004-12-07 | Bayer Aktiengesellschaft | Synergistic insecticide mixtures |
WO2012050141A1 (ja) * | 2010-10-14 | 2012-04-19 | 住友化学株式会社 | ヘテロ芳香環化合物およびその有害生物防除用途 |
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-
1995
- 1995-02-08 IL IL11257795A patent/IL112577A0/xx unknown
- 1995-02-09 AU AU19134/95A patent/AU679350B2/en not_active Ceased
- 1995-02-09 MX MX9603273A patent/MX9603273A/es unknown
- 1995-02-09 HU HU9602186A patent/HUT76814A/hu unknown
- 1995-02-09 BR BR9506960A patent/BR9506960A/pt not_active Application Discontinuation
- 1995-02-09 WO PCT/US1995/001616 patent/WO1995021846A1/en not_active Application Discontinuation
- 1995-02-09 EP EP95911641A patent/EP0743947A1/en not_active Withdrawn
- 1995-02-09 JP JP7521314A patent/JPH09507676A/ja active Pending
- 1995-02-09 CN CN95191561.4A patent/CN1140452A/zh active Pending
- 1995-02-09 PL PL95315813A patent/PL315813A1/xx unknown
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EP0743947A1 (en) | 1996-11-27 |
WO1995021846A1 (en) | 1995-08-17 |
HU9602186D0 (en) | 1996-10-28 |
AU679350B2 (en) | 1997-06-26 |
IL112577A0 (en) | 1995-05-26 |
AU1913495A (en) | 1995-08-29 |
MX9603273A (es) | 1997-03-29 |
BR9506960A (pt) | 1997-09-09 |
PL315813A1 (en) | 1996-12-09 |
HUT76814A (en) | 1997-11-28 |
JPH09507676A (ja) | 1997-08-05 |
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