CN1135211A - 苯基磺酰脲，其制备方法及其用作除草剂和植物生长调节剂 - Google Patents

苯基磺酰脲，其制备方法及其用作除草剂和植物生长调节剂 Download PDF

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CN1135211A
CN1135211A CN94194137A CN94194137A CN1135211A CN 1135211 A CN1135211 A CN 1135211A CN 94194137 A CN94194137 A CN 94194137A CN 94194137 A CN94194137 A CN 94194137A CN 1135211 A CN1135211 A CN 1135211A
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K·劳伦兹
L·威尔姆斯
K·保尔
H·比伦格
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Abstract

权利要求1中定义的式(I)化合物及其盐适合作为选择性除草剂，见式(1)，
其中R1为CO-Q-R8，其中R8＝H或R，R2和R3为H或(C1-C4)烷基，R4为H，R，RO，OH，RCO，RSO2，PhSO2，R5为RSO2，PhSO2，PhCO，RNHSO2，R2NSO2，RCO，CHO，COCOR′，CW-T-R9，CW-NR10R11，CW-N(R12)2，或R4和R5一起为(CH2)mB或-B1-(CH2)m1B-链，其中B＝SO2，CO；m＝3，4；m1＝2，3，；T和W＝O，S；Q＝O，S，NR13,其中R13＝H,R;R6＝H，R，RO，RCO，ROCO，Hal，NO2，CN；R7＝H,CH3;R9＝R;R10,R11＝H,R;N(R12)2＝杂环，Ａ＝嘧啶基和三嗪基或其类似的基团。可通过相似方法从式Ⅱ磺酰胺制备上述化合物，一些式(Ⅱ)化合物是新的(见权利要求４)。

Description

苯基磺酰脲，其制备方法及其 用作除草剂和植物生长调节剂
已知一些苯基磺酰脲具有除草和调节植物生长的性质；参见US-A-4,786,314，US-A-4,927,453和WO89/10921。可是在一些情况下上述苯基磺酰脲在应用上存在一些缺点，例如残效高或对重要的作物选择性差。
现已发现在苯环上具有一定基团的苯基磺酰脲可有效地用作除草剂或植物生长调节剂。本发明涉及式(I)的化合物或其盐，
Figure A9419413700121
其中R1为CO-Q-R8，R2和R3各自独立的为H或(C1-C4)烷基，R4为H，未取代或被一或多个下组包括的基团取代的(C1-C8)烷基，上述取代基团由卤素、(C1-C4)烷氧基、(C1-C4)烷硫基、(C1-C4)烷基亚磺酰基、(C1-C4)烷基磺酰基、[(C1-C4)烷氧基]羰基和CN组成，或为未被取代或被一至多个卤原子取代的(C3-C6)链烯基，或为未被取代或被一至多个卤原子取代的(C3-C6)链炔基，或为羟基，(C1-C4)烷氧基，[(C1-C4)烷基]羰基或(C1-C4)烷基磺酰基，后三个基团各自未被取代或在烷基部分被一至多个卤原子或被(C1-C4)烷氧基或(C1-C4)烷硫基取代，或为苯基磺酰基，其中苯基是未被取代或优选被一至多个下述基团取代，取代基由卤素、CN、NO2、(C1-C4)烷基、(C1-C4)卤代烷基和(C1-C4)烷氧基组成，和R5为(C1-C4)烷基磺酰基或(C3-C6)链烯基磺酰基，后两个基团各自未被取代或被一至多个卤原子或被(C1-C4)烷氧基或(C1-C4)烷硫基取代的，或为苯基磺酰基或苯基羰基，后两个基团的苯基各自未被取代或优选被一或多个下述基团取代，上述取代基由卤素、CN、NO2、(C1-C4)烷基、(C1-C4)卤代烷基和(C1-C4)烷氧基组成，或为单-或二-[(C1-C4)烷基]氨基磺酰基或[(C1-C6)烷基]羰基，后三个基团各自未被取代或被一或多个下述基团取代，上述取代基由卤素、(C1-C4)烷氧基、(C1-C4)烷硫基、(C1-C4)烷基亚磺酰基、(C1-C4)烷基磺酰基、[(C1-C4)烷基]羰基、[(C1-C4)烷氧基]羰基和CN组成，或为甲酰基，式-CO-CO-R’的基团其中R’＝H，OH，(C1-C4)烷氧基或(C1-C4)烷基，或为[(C3-C6)环烷基]羰基，[(C2-C6)链烯基]羰基或[(C2-C6)链炔基]羰基，后三个基团各自未被取代或被一或多个卤原子取代，或为下式的基团
Figure A9419413700141
或R4和R5一起为式(-CH2)mB-或-B1-(CH2)ml-B-的链，上述链是未被取代或被一个或多个，优选直至四个(C1-C3)烷基取代和m为3或4或m1为2或3，和W为氧或硫原子(即O或S)，B和B1各自独立为SO2或CO，Q为O，S或-NR13-，T为O或S，R6为H，(C1-C4)烷基，(C1-C4)烷氧基，[(C1-C4)烷基]羰基或[(C1-C4)烷氧基]羰基，后四个基团各自未被取代或在烷基部分被一至多个卤原子取代，或为卤素，NO2或CN，R7为H或CH3，R8为H，(C1-C4)烷基，(C3-C4)链烯基或(C3-C4)链炔基，后三个基团各自未被取代或被一或多个由卤素、(C1-C4)烷氧基、(C1-C4)烷硫基、[(C1-C4)烷基]羰基和[(C1-C4)烷氧基]羰基组成的一组基团取代，R9为(C1-C4)烷基，(C3-C4)链烯基或(C3-C4)链炔基，后三个基团各自未被取代或被一或多个由卤素、(C1-C4)烷氧基、(C1-C4)烷硫基、[(C1-C4)烷基]羰基和[(C1-C4)烷氧基]羰基组成的一组基团取代，R10和R11各自独立地为H，(C1-C4)烷基，(C3-C4)链烯基或(C3-C4)链炔基，后三个基团各自未被取代或被一或多个由卤素、(C1-C4)烷氧基、(C1-C4)烷硫基、[(C1-C4)烷基]羰基和[(C1-C4)烷氧基]羰基组成的一组基团取代，R12基团与氮原子一起为5或6元杂环，上述杂环在可能的氧化态中可含有一个其它N，O和S杂原子，且是未被取代或被(C1-C4)烷基或氧基取代，或被苯环稠和，R13为H，(C1-C4)烷基，(C3-C4)链烯基或(C3-C4)链炔基，后三个基团各自未被取代或被一或多个由卤素、(C1-C4)烷氧基、(C1-C4)烷硫基组成的一组基团取代，A为下式的基团
Figure A9419413700151
X和Y基团之一是氢，卤素，(C1-C3)烷基或(C1-C3)烷氧基，后两个基团是未被取代或被卤素单取代或多取代或被(C1-C3)烷氧基单取代，和X和Y基团的另一个是氢，(C1-C3)烷基，(C1-C3)烷氧基或(C1-C3)烷硫基，后三个含有烷基的基团是未被取代或被卤原子单或多取代或被(C1-C3)烷氧基或(C1-C3)烷硫基单取代或二取代，或为式NR14R15的基团，(C3-C6)环烷基，(C2-C4)链烯基，(C2-C4)链炔基，(C3-C4)链烯氧基，(C3-C4)链炔氧基，Z为CH或N，R14和R15各自彼此独立地为H，(C1-C3)烷基，(C3-C4)链烯基，X1为CH3、OCH3、OC2H5或OCHF2，Y1为-O-或-CH2-X2为CH3、C2H5或CH2CF3Y2为OCH3、OC2H5、SCH3、SCH2CH3、CH3或C2H5，X3为CH3或OCH3，Y3为H或CH3，X4为CH3、OCH3、OC2H5、CH2OCH3或Cl，Y4为CH3、OCH3、OC2H5或Cl和Y5为CH3、C2H5、OCH3或Cl。在式(I)和下文中，烷基、烷氧基、卤代烷基、烷基氨基和烷硫基以及相应的不饱和和/或取代的基团在碳架中各自可为直链和支链的基团。单独的烷基或作为如烷氧基、卤代烷基等的组成的烷基是甲基、乙基、正或异丙基、正-、异-、叔-或2-丁基；链烯基或链炔基具有相应于烷基可能的不饱和基团的定义，如2-丙烯基、2-或3-丁烯基、2-丙炔基、2-或3-丁炔基。卤素为氟、氯、溴或碘；卤代烷基是被一或多个卤原子取代的烷基；卤代烷基的实例为CF3、CHF2和CH2CF3。取代苯基优选为被一或多个，优选1，2或3个下组基团取代的苯基，上组取代基团由卤素，如F、Cl、Br和I，优选F、Cl和Br，以及烷基、卤代烷基、烷氧基、卤代烷氧基、羟基、氨基、硝基、氰基、烷氧羰基、烷基羰基、甲酰基、氨基甲酰基、单-和二烷基氨基羰基、单-和二烷基氨基、烷基亚磺酰基和烷基磺酰基组成，且对于含有碳原子的基团，上述含有一至四个碳原子、特别1或2碳原子的基团是优选的。在此一般优选的取代基为由卤素，例如氟和氯、C1-C4-烷基、优选甲基或乙基，C1-C4-卤代烷基、优选三氟甲基，C1-C4-烷氧基、优选甲氧基或乙氧基，C1-C4-卤代烷氧基，硝基和氰基组成的一组基团。
在需要时可被苯稠和和含有氮原子(例如，在N(R12)2的情况下)的5-或6-元杂环可以是饱和，不饱和或杂芳基，例如借助氮原子连接并选自下组的基团，上述基团由吡咯烷基、哌啶基、吡唑基、吗啉基、吲哚基、喹啉基、嘧啶基、三唑基、噁唑基、吡啶基、嘧啶基、哒嗪基、吡嗪基、噻唑基、噁唑基、吡咯基、咪唑基和苯并恶唑基。
本发明还涉及式(I)化合物的各种异构体，及其混合物。如在式(I)未具体指明的含有一或多个不对称碳原子或双键的式(I)化合物。式(I)包括通过具体空间构型确定的所有可能的立体异构体，如对映体、非对映体、E和Z异构体，上述所有的异构体都可通过常规方法从立体异构体的混合物或通过立体选择性反应结合应用立体化学纯的起始物而制备。
式(I)化合物可形成盐，其中-SO2-NH-基的氢原子被适于农用的阳离子置换。例如上述盐是金属盐、特别是碱金属盐或碱土金属盐、特别是钠和钾盐、或铵盐或与有机胺形成的盐。
特别令人感兴趣的是根据本发明的式(I)化合物或其盐其中R4为H，未取代或被一或多个下组包括的基团取代的(C1-C4)烷基，上述取代基团由卤素、(C1-C4)烷氧基、(C1-C4)烷硫基、(C1-C4)烷基磺酰基、[(C1-C4)烷氧基]羰基和CN组成，或为(C3-C4)链烯基、(C3-C4)链炔基、羟基，(C1-C4)烷氧基，[(C1-C4)烷基]羰基或(C1-C4)烷基磺酰基，后五个基团各自未被取代或在烷基部分被一至多个卤原子取代，或为苯基磺酰基，其中苯基是未被取代或被一或多个下述基团取代的，取代基由卤素、(C1-C4)烷基和(C1-C4)烷氧基组成，和R5为(C1-C4)烷基磺酰基、(C1-C4)卤代烷基磺酰基、苯基磺酰基或苯基羰基，后两个基团中的苯基各自未被取代或被一至多个选自卤原子、(C1-C4)烷基和(C1-C4)烷氧基的基团取代，或为单-或二-[(C1-C4)烷基]氨基磺酰基，未被取代或被一或多个卤原子或(C1-C4)烷氧基或(C1-C4)烷硫基取代的[(C1-C6)烷基]羰基，或为甲酰基、OHC-CO-、2-氧-(C3-C5)链烷酰基、[(C1-C4)烷氧基]草酰基、[(C3-C6)环烷基]羰基，[(C2-C4)链烯基]羰基或[(C2-C4)链炔基]羰基、或为下式的基团W为O或SR6为H、(C1-C4)烷基、(C1-C4)卤代烷基、(C1-C4)烷氧基、(C1-C4)卤代烷氧基或卤素，R8各自为未被取代或被一或多个卤原子取代的(C1-C4)烷基，或为(C3-C4)链烯基或(C3-C4)链炔基，R9为H、未被取代或被一或多个卤原子或被(C1-C4)烷氧基、(C1-C4)烷硫基、[(C1-C4)烷氧基]羰基和[(C1-C4)烷基]羰基取代的(C1-C4)烷基，R10和R11各自独立地为H、未被取代或被一或多个卤原子取代的(C1-C4)烷基、或为(C3-C4)链烯基或(C3-C4)链炔基、其中R10和R11至少一个不是氢，R12基团与氮原子一起为5或6元杂环，上述杂环在不同的氧化态中可含有一个其它N，O和S杂原子，且是未被取代或被(C1-C4)烷基或氧基取代，R13为H，未被取代或被一或多个由卤素原子取代的(C1-C4)烷基、或为(C3-C4)链烯基或(C3-C4)链炔基。
优选的式(I)化合物及其盐是其中W为氧原子和A为下式的基团的式(I)化合物
Figure A9419413700201
其中X、Y和Z如上述定义。特别优选的式(I)化合物或其盐，其中R4为H、(C1-C4)烷基、羟基或(C1-C4)烷氧基，R5为(C1-C4)烷基磺酰基、CHO、未被取代或被一或多个卤原子取代的[(C1-C4)烷基]羰基、或为[(C1-C4)烷氧基]草酰基、[(C3-C6)环烷基]羰基或下式的基团
Figure A9419413700202
其中W，T和R9至R12如上面式(I)中的定义，R6为H、(C1-C3)烷基、(C1-C3)烷氧基或卤素，A为下式的基团
Figure A9419413700203
Z为CH或N，优选为CH，和X和Y基团之一为卤素、(C1-C2)烷基、(C1-C2)烷氧基、OCF2H、CF3或OCH2CF3和X和Y的另一个为(C1-C2)烷基、(C1-C2)烷氧基或(C1-C2)卤代烷氧基。
鉴于便于制备或具有较好的生物活性的原因，其中基团-CR2R3-NR4R5相对于R1基团为邻位或对位或相对于磺基为邻位的根据本发明的式(II)化合物及其盐是特别令人感兴趣的；-CR2R3-NR4R5基优选的位置是R1基的对位。
本发明还涉及制备式(I)化合物及其盐的方法，其中包括a)式(II)的化合物与式(III)杂环氨基甲酸酯反应
Figure A9419413700211
R*-O-CO-NR7-A    (III)其中R*是必要时被取代的苯基或(C1-C4)烷基，或b)式(IV)的苯基磺酰基氨基甲酸酯与式(V)的氨基杂环反应H-NR7-A    (V)或c)式(VI)的磺酰基异氰酸酯与式(V)H-NR7-A的氨基杂或d)在一个单釜反应(Eintopfreaktion)中，首先在碱存在下使式(V)H-NR7-A的氨基杂环化物与光气反应，然后反应的中间体与式(II)的苯基磺酰胺反应，或e)在碱存在下式(VII)的磺酰氯与其中M＝NH4、Na或K的氰酸酯M-OCN以及式(V)H-NR7-A的氨基杂环化物反
Figure A9419413700223
f)在碱存在下上述式(II)的磺酰胺与式(V’)的(硫代)异氰酸酯反应
W＝C＝N-A    (V’)，在式(II)-(VII)和(V’)中的基团R1-R7、A或W如在式(I)中的定义，在方法a)-e)中，最初获得的是W＝O的式(I)化合物。
式(II)化合物和式(III)化合物的反应优选在碱催化下，在惰性有机溶剂，例如二氯甲烷、乙腈、二噁烷或THF存在下，在0℃和溶剂沸点之间进行。使用的碱的实例为有机胺碱，如特别是R*＝(取代)苯基(参见EP-A-44 807)时，碱为1，8-二氮杂二环[5.4.0]十一-7-烯(DBU)，或特别是R*＝烷基(参见EP-A-166 516)时，碱为三甲基铵或三乙基铵。式(II)的磺酰胺是新化合物。其和其制备方法也是本发明的主题。以其中R2＝R3＝H和Q＝O的式(II)化合物为例，对其可能的制备方法在下面进行了详细的描述，且只要作一点改动就可将上述方法用于其中R2和R3不是氢和/或Q不是O的化合物的制备。
采用文献中已知的相似方法，以取代和未取代的甲基氨基苯磺酸(VIII)作为起始物(参见德国专利48 583,242页)时，最初通过重氮化作用和按Sandmeyer反应用KCN/CuCN将其转化成腈(IX)，将腈皂化，通过羧基的酯化作用和将磺基转化成叔丁基-保护的磺酰胺基后得到作为中间体的磺酰胺(X)(见图1)。
图1此外，以取代或未取代的甲基硝基苯甲酸(XI)作为起始物，通过酯化作用、硝基的还原、重氮化作用和与SO2/CuCl偶联(见H.Meerwein等人，Chem.Ber.90，841-1178(1957))和用叔丁基胺氨解可获得式(X)的磺酰胺(见图2)。
图2
Figure A9419413700242
同样磺酰胺(X)的制备可以取代或未取代的甲基硝基苯胺(XII)作为起始物。通过重氮化作用和与KCN/CuCN偶联得到相应的腈，其可通过氰基的水解并酯化成硝基苯甲酸酯(XIII)。然后可将图2中所述的硝基转化成叔丁基氨基磺酰基(见图3)。
图3
为了制备式(II)的磺酰胺，可在式(X)化合物的侧链进行卤化作用得到(XIV)，然后用胺或叠氮化物取代(XIV)上的卤原子，接着还原得到苄基胺(XV’)，再对氨基官能化并通过已知的相似方法(例如用CF3COOH)除去叔丁基保护基得到磺酰胺(II’)(见图4)。
图4
Figure A9419413700261
类似地，该方法步骤还可用于制备其它式(II)化合物，其中在最后一步中使用式(XV)化合物
式(III)氨基甲酸酯可通过描述在南非专利申请82/5671和82/5045或EP-A-70 804(US-A-4,480101)或RD275056中的方法制备。
式(IV)化合物与氨基杂环(V)的反应优选在如二噁烷、乙腈或四氢呋喃的惰性的、质子惰性溶剂中，在0℃至溶剂的沸点之间的温度下进行。所需的起始物(V)是文献中已知的或可通过文献中已知的方法制备的。式(IV)的苯基磺酰基氨基甲酸酯可通过类似于US-A-4,684,393或US-A-4,743,290的方法获得。
式(VI)的苯基磺酰基异氰酸酯可通过类似于US-A-4,481,029的方法制备并可与氨基杂环(V)反应。
根据方法d)的式(V)化合物的光气化作用优选在如空间位阻的有机胺碱，例如三乙胺的存在下进行。根据方法d)与式(II)化合物随后进行的反应可通过类似于已知的方法进行(参见：EP-A-232067)。
式(VII)的磺酰氯可通过常规方法从相应的磺酸获得，例如，在如乙腈和/或环丁砜的惰性溶剂中或不在溶剂中通过加热至回流使钾盐与磷酰氯或亚硫酰氯反应得到(参见：Houben-Weyl-Klamann，“Methoden der organischen Chemie”，[有机化学方法]，第四版，E XI/2卷，1067-1073页，ThiemeVerlag，Stuttgart，1985)。
通过类似于化合物(XI)的反应，相应的磺酸可从适当的硝基化合物获得。
可选择地，在个别的情况下，磺酰氯(VII)可通过适当取代的苯甲酸酯的磺化作用(+氯化作用)或氯磺化作用制备；氯磺化作用是采用Houben-Weyl-Klamann，“Methoden der organischenChemie”，[有机化学方法]，第四版，E XI/2卷，1067页，ThiemeVerlag，Stuttgart，1985)；Houben-Weyl-Muller，“Methoden derorganischen Chemie”，[有机化学方法]，第四版，XI卷，563页，Thieme Verlag，Stuttgart，1955)的类似方法；磺化作用是采用Houben-Weyl-Klamann，“Methoden der organischenChemie”，[有机化学方法]，第四版，E XI/2卷，1055页，ThiemeVerlag，Stuttgart，1985)；Houben-Weyl-Muller，“Methoden derorganischen Chemie”，[有机化学方法]，第四版，IX卷，435页，Thieme Verlag，Stuttgart，1955)的类似方法。
采用文献中的已知方法(EP-A-232067，EP-A-166516)可获得式(V’)的(硫代)异氰酸酯。(硫代)异氰酸酯(V’)与化合物(II)的反应在-10℃至100℃，优选20至200℃下，在诸如丙酮或乙腈的惰性的质子惰性溶剂中，在适合的碱，例如N(C2H5)3或K2CO3的存在下进行。
优选于诸如水、甲醇或丙酮的惰性极性溶剂中，在0-100℃下制备式(I)化合物的盐。根据本发明，适合制备盐的碱的实例为碱金属碳酸盐，如碳酸钾，碱金属氢氧化物和碱土金属氢氧化物，例如NaOH或KOH，或氨或乙醇胺。
在上述方法中所指的“惰性溶剂”为各种在各自的反应条件下惰性的溶剂，但其不需要在所有的反应条件下呈惰性。
根据本发明的式(I)化合物对多种经济上重要的单子叶和双子叶有害植物具有极好的除草活性。本活性物质还对从根茎、砧木根或其它多年生器官萌生的而且难于防治的多年生杂草具有有效的作用。在本文中，无论活性物质在播种前、苗前或苗后使用都可以。
下面具体但非限定性地述及了根据本发明化合物可以防治的一些代表性的单子叶和双子叶杂草的谱系。
活性物质对其能有效发挥作用的杂草的实例为：单子叶杂草：一年生中的燕麦、黑麦草、看麦娘、虉草、稗、马唐、狗尾草以及莎草属和多年生冰草、狗牙根、白茅和蜀黍属，以及多年生莎草属。
对双子叶杂草能发挥作用的是，例如一年生的：猪殃殃、堇菜、婆婆纳、野芝麻、繁缕、苋、白芥、牵牛、母菊、麻和黄花稔属，和多年生的旋花、蓟、酸模和蒿属。
根据本发明的活性物质防治水稻生长条件下的杂草非常有效，上述杂草如：慈菇、泽泻、荸荠、藨草和莎草属。
如果在萌发前将根据本发明化合物施用到土壤表面，则或是能完全防止杂草幼苗萌发，或是杂草生长到子叶阶段后生长停止且最终在三至四周后，杂草全部死亡。
如果将活性物质在苗后施用到植物的绿色部分，在处理后短期内植物生长马上停止且杂草植物停留在施药时的生长期，或一段时间后完全死亡，因此以这种方式将对作物有害的杂草竞争及早、持继地加以消除。
尽管对单子叶和双子叶杂草具有极好所除草活性，根据本发明的化合物完全不损害经济作物或其损害很小，经济作物如小麦、大麦、黑麦、水稻、玉米、甜菜、棉花和大豆。根据上述原因，本发明的化合物非常适合在农作物中选择性地防治有害植物生长。
另外，根据本发明的物质对作物存在明显的调节植物生长的性质。它们介入代谢的调节并因此可用来有针对性地影响植物中含有的物质，和方便收获，例如通过最初的干燥和生长紧密。而且，它们可在不杀死植物的情况下，系统的防治和抑制不需要的植物生长。在许多单子叶和双子叶作物中，抑制植物生长具有很大作用，这是因为这样能减少或完全防止倒伏。
根据本发明的化合物可用于常规的制剂形式，如可湿性粉剂、可乳化浓缩物、可喷雾溶液、粉剂或颗粒剂。因此本发明还涉及含有式(I)化合物的除草和植物生长调节组合物。
根据预定的生物和/或物理化学参数，可以多种方式配制式(I)化合物。因此可能的制剂为：可湿性粉剂(WP)、水溶性粉剂(SP)、水溶性浓缩物、可乳化浓缩液(EC)、乳液(EW)如水包油型和油包水型乳液、可喷雾溶液、浓悬浮液(SC)、油基或水基分散液、油混溶液剂、胶囊悬浮液(CS)、粉剂(DP)、种子包衣剂、散播和土壤施用颗粒剂、微胶囊形式的颗粒剂(GR)、喷洒颗粒剂、包覆颗粒剂和吸收颗粒剂、水分散颗粒剂(WG)、水溶颗粒剂(SG)、ULV制剂、微胶囊和蜡剂。
上述单独的制剂类型原则上是已知的且描述在：Winnacker-Kuchler，“Chemische Technologie”[化学技术]，7卷C.HauserVerlag Munich，第4版，1986；Wade van Valkenburg，“Pesticide Formulation”，Marcel Dekker N.Y.1973；K.Martens，“Spary Drying”手册，第3版，1979，G.Goodwin Ltd.London。
制剂中所需要的助剂如惰性材料、表面活性剂、溶剂和其它添加剂也是已知的并描述在：例如(Watkins，“Handbook ofInsecticide Dust Diluents and Carriers”，第二版，Darland Books，Caldwell N.J.，H.v.Olphen，“Introduction to Clay ColloidChemistry”，第二版，J.Wiley & Sons，N.Y.；C.Marsden，“Solvents Guide”，第二版，Interscience，N.Y.1963；McCutcheon’s“Detergents and Emulsifiers Annual”，MC Publ.Corp.，Ridgewood N.J.；Sisley and Wood，“Encyclopedia of SurfaceActive Agents”，Chem.Publ.Co.Inc.，N.Y.1964；Schonfeldt，“Grenzflchenaktive thylenoxidaddukte”[表面活性的环氧乙烷加成物]，Wiss.Verlagsgesell.，Stuttgart 1976；Winnacker-Küchler，“Chemische Technologie”[化学技术]，Volume 7，C.Hauser VerlagMunich，第4版，1986。
与其它已知农药活性成分如杀虫剂、杀螨剂、除草剂、杀菌基的组合物，以及与安全剂、肥料和/或生长调节剂的组合物也可以上述制剂为基础制备，例如以现用制剂或桶混合物的形式。
可湿性粉剂是能均匀分散于水中的制剂，且除了活性物质外，其中还含有一些离子和/或非离子型表面活性剂(湿润剂，分散剂)，例如聚乙氧基化烷基酚、聚乙氧基化脂肪醇、聚乙氧基化脂肪胺、脂肪醇聚乙二醇醚硫酸盐、烷基磺酸盐、烷基苯磺酸盐、木质素磺酸钠、2，2’-二萘基甲烷-6，6’-二磺酸钠、二丁基萘磺酸钠，或油酰基经济牛酯酸钠(OleoylmethyltaurinsauresNatrium)，以及稀释剂或惰性物质。可湿性粉剂的制备是通过精细研磨除草活性物质，例如在常规的设备如锤磨、吹磨和气流磨中研磨，并在同时或随后将其与制剂助剂混合。
可乳化浓缩液的制备是通过在添加一种或多种离子型和/或非离子型表面活性剂的条件下将活性物质溶于有机溶剂中，有机溶剂例如：丁醇、环己酮、二甲基甲酰胺、二甲苯和高沸点的芳香化合物或烃类或有机溶剂的混合物。可使用的乳化剂的实例为：烷基芳基磺酸钙盐如十二烷基苯磺酸钙、或非离子型乳化剂，如脂肪酸聚乙二醇酯、烷基芳基聚乙二醇醚、脂肪醇聚乙二醇醚、环氧丙烷/环氧乙烷缩合产物、烷基聚醚、脱水山梨醇酯、如脱水山梨醇脂肪酸酯或“聚氧乙烯脱水山梨醇酯，诸如聚氧乙烯脱水山梨醇脂肪酸酯。
粉剂的制备是通过将活性物质与细分离的固体物质研磨而制备，固体物质例如：滑石或天然粘土，如高岭土、膨润土、叶蜡石或硅藻土。
浓悬浮剂是以水或油为基础的。它们的制备是例如通过借取常规的球磨湿磨和必要时加入上述其它类型制剂中使用的表面活性剂来进行的。
乳液，例如水包油型乳液(EW)的制备例如：通过搅拌器、胶体磨和/或静电磨的方式，使用含水的有机溶剂和如果需要的表面活性剂来制备，表面活性剂如上述其它类型制剂中使用的表面活性剂。
颗粒剂的生产或是通过将活性物质喷布在吸收性、造粒惰性材料上，或是借助于粘合剂将活性物质的浓缩物涂敷在载体的表面，制备，载体如砂土、高岭土和造粒惰性材料，粘合剂例如聚乙烯醇、聚丙烯酸钠或矿物油。也可按常规的生产肥料颗粒的方法将活性物质造粒，如果需要可为与肥料的混合物。
水分散颗粒剂通常是通过常规的方法制备，如喷雾干燥、流化床造粒、平板(Teller)造粒、用高速混合器混合和不需要固体惰性载体的挤压。对于平板、流化床、挤压器和喷布颗粒的制备，可参见“Spary Drying Handbook”第3版，1979，G.GoodwinLtd.，”London；J.E.Browning，“Agglomeration”，Chemical andEngineering 1967，147等页；“Perry’s Chemical Engineer’sHandbook””，第5版，McGraw-Hill，New York 1973，8-57页。
对于作物保护组合物制剂的详细内容例如参见G.C.Klingman，“Weed Control sa a Science”，John Wiley和Sons，Inc.，New York，1961，81-96页和J.D.Freyer，S.A.Evans，“Weed ControlHandbook”，第5版，Blackweel ScientificPublications，Oxford，1968，101-103页。
本农用化学制剂通常含有0.1至99％重量和特别含有0.1至95％重量的式(I)活性物质。活性物质在可湿性粉剂中的浓度例如为大约10至90％重量；100％重量的剩余物由常规的制剂成分组成。在可乳化浓缩液的情况下，活性物质的浓度可为大约1至90％重量，优选5至80％重量。粉剂的制剂形式中含有1至30％重量，通常优选5-20％重量的活性物质，可喷雾液剂含有大约0.05至80，优选2至50％重量的活性成分。在水分散颗粒剂的情况下活性物质的含量部分的依赖于活性化合物为液体或固体和使用的造粒助剂、填料等。在水分散颗粒剂的情况下活性物质的含量为：例如1至95％重量，优选10至80％重量。
另外，已述及的活性物质的制剂如果适合可含有在各种情况下常规使用的粘着剂、湿润剂、分散剂、乳化剂、渗透剂、防腐剂、防冻剂、溶剂、填料、载体和着色剂、防泡剂、蒸发抑制剂和PH和粘度调节剂。
在混合制剂或桶混合物中的本发明活性物质的混用组合物中可使用，例如描述在如Weed Research 26，441-445(1986)或“ThePesticide Manual”，第9版，The British Crop ProtectionCouncil，1990/91，Bracknell，England，和其中所引文献描述的已知活性物质。可与式(I)化合物混用的文献中已知的除草剂的实例为下述活性物质(注意：化合物或是以其根据国际标准化组织(ISO)提供的通用名给出或是以化学名给出，如果需要还连带通用编码)：乙草胺、三氟羧草醚、苯草醚、氟草醚酯，即[[[1-[5-[2-氯-4-(三氟甲基)苯氧基]-2-硝基苯基]-2-甲氧基亚乙基]氨基]氧]乙酸及其甲基酯、甲草胺、枯杀达、莠灭津、amidosulfuron、amitrol、AMS，即氨基磺酸铵、莎稗磷、黄草灵、莠去津、azimsulfurone(DPX-A8947)、叠氮津、燕麦灵、BAS516H，即5-氟-2-苯基-4H-3，1-苯并恶嗪-4-酮、草除灵、氟草胺、呋草黄、苄嘧磺隆、地散磷、灭草松、吡草酮、benzofluor、新燕灵、噻草隆、双丙氨酰膦、甲羧除草醚、除草定、溴丁酰草胺、杀草全、溴苯腈、bromuron、buminafos、busoxinone、丁草胺、草胺磷、丁烯草胺、草噻醚、地乐胺、丁草特、cafenstrole(CH-900)、卡草胺、碘草酮(ICI-A0051)、草毒死，即2-氯-N，N-二-2-丙烯基乙酰胺、草克死，即2-氯烯丙基二乙基二硫代氨基甲酸酯、氟硝醚、草灭平、chlorazifop-butyl、Chlormesulon(ICI-A0051)、氯溴隆、氟草灵、伐克草、氯甲丹、杀草敏、氯嘧磺隆、草枯醚、绿麦隆、枯草隆、氯苯胺灵、绿磺隆、敌草索、草克乐、恶庚草烷、醚磺隆、烯草酮、clodinafop及其酯衍生物(例如clodinafop-propargyl)、广灭灵、稗草胺、Cloproxydim、clopyralid、cumyluron(JC 940)、氰草津、环莠特、cyclosulfamuron(AC 104)、噻草酮、环莠隆、cyhalofop及其酯衍生物(例如丁基酯，DEH-112)、对草快、环草津、环唑草胺、daimuron、2，4-滴丁酸、茅草枯、异苯敌草、敌草净、燕麦敌、麦草畏、敌草腈、2，4-滴丙酸、禾草灵、及其酯如甲基禾草灵、安塔、枯莠隆、野燕枯、吡氟草胺、dimefuron、克草胺、戊草津、dimethenamide(SAN-582H)、敌苯达松、dimethipin、dimetrasulfuron、敌乐胺、地乐散、地乐硝酚、双苯酰草胺、杀草净、敌草快、氟硫草定、敌草隆、二硝甲酚、草止津、氟草酮，即5-氰基-1-(1，1-二甲基乙基)-N-甲基-1H-吡唑-4-甲酰胺、草藻灭、扑草灭、禾草畏、丁氟硝草、ethametsulfuron-methyl、噻二唑隆、乙嗪草酮、唑啶草、F5231，即N-[2-氯-4-氟-5-[4-(3-氟丙基)-4，5-二氢-5-氧-1H-四唑-1-基]苯基]乙烷磺酰胺、ethoxyfen及其酯(例如乙基酯，HN-252)、etobenzanid(HW52)、2，4，5-滴丙酸、fenoxan、噁唑禾草灵和高噁唑禾草灵及其酯，例如fenoxaprop-P-ethyl和fenoxaprop-ethyl、fenoxydim、黄草隆、甲氟燕灵、啶嘧磺隆、吡氟禾草灵和精吡氟禾草灵及其酯，例如fluazifop-butyl和fluazifop-P-butyl、氟消草、flumetsulam、伏草隆、flumiclorac及其酯(例如苯基酯，S-23031)、flumioxazin(S-482)、flumipropyn、flupoxam(KNW-739)、fluorodifen、fluoroglycofen-ethyl、氟胺磺隆(UBIC-4243)、氟草同、fluroehloridone、fluroxypyr、flurtamone、氟磺胺草醚、膦铵素、氟呋草醚、草胺膦、草甘膦、halosaten、halosulfuron及其酯(例如甲基酯，NC-319)、吡氟乙草灵及其酯、吡氟氯禾灵(＝R-haloxyfop)及其酯、环嗪酮、咪草酯、灭草烟、灭草喹、及其盐如铵盐、imazethamethapyr、咪草胺、imazosulfuron、碘苯腈、丁环隆、异乐灵、异丙隆、异噁隆、异恶草胺、isoxapyrifop、卡草灵、克阔乐、环草定、利谷隆、二甲四氯、二甲四氯丁酸、二甲四氯丙酸、苯噻草胺、氟草磺、苯嗪草、吡草胺、噻唑隆、威百亩、灭草定、去草酮、methyldymron、metabenzuron、methobenzuron、秀谷隆、丙草胺、metosulam(XRD 511)、甲氧隆、赛克津、甲黄隆、抑草丹、禾草特、杀草利、二氢硫酸单脲、绿谷隆、灭草隆、MT128，即6-氯-N-(3-氯-2-丙烯基)-5-甲基-N-苯基-3-哒嗪胺(pyridazinamin)、MT 5959，即N-[3-氯-4-(1-甲基乙基)-苯基]-2-甲基戊酰胺、草萘胺、抑草生、NC310，即4-(2，4-二氯苯甲酰基)-1-甲基-5-苄基氧吡唑、草不隆、烟嘧磺隆、吡氯草胺、nitralin、除草醚、nitroflurofen、norflurazon、orbencarb、磺禾灵、恶霜灵(RP-020630)、恶草灵、氟消草醚、对草快、克草猛、胺硝草、氟草磺胺、敌克草、二苯乙草、毒莠定、哌草磷、piributicarb、pirifenop-butyl、丙草胺、氟嘧磺隆、环氰津、prodiamine、卡乐施、丙草止津、2，4，5-涕、扑草净、metryn、扑草胺、敌稗、喔草酯及其酯、扑灭津、苯胺灵、propisoehlor、拿草特、prosulfalin、杀草丹、prosulfuron(CGA-152005)、广草胺、pyrazolinate、杀草敏、吡嘧磺隆、苄草唑、达草酯、pyrithiobac(KIH-2031)、pyroxofop及其酯(即炔丙基酯)、二氯喹啉酸、喹草酸、quinofop及其酯衍生物、喹禾灵和quizalofop及其酯衍生物、即quizalofop-ethyl、quizalofop-P-tefuryl和-ethyl、renriduron、rimsulfuron(DPX-E 9636)、S275，即2-[4-氯-2-氟-5-(2-丙炔氧基)-苯基]4，5，6，7-私氢-2H-吲唑、密草通、烯禾定、环莠隆、西马津、西草净、氟萘草酯、即2-[[7-[2-氯-4-(三氟甲基)-苯氧基]-2-萘基]氧]丙酸及其甲基酯、sulfentrazon(FMC-97385，f-6285)、sultazuron、嘧磺隆、sulfosate(ICI-A0224)、三氟醋酸、tebutam(GCP-5544)、丁唑隆、特草定、牙根灵、猛杀草、甲氧去草净、特丁津、去草净、TFH450，即N，N-二乙基-3-[(2-乙基-6-甲基苯基)-磺酰基]-1H-1，2，4-三唑-1-甲酰胺、thenylchlor(NSK-850)、噻唑隆、thizopyr(Mon-13200)、thidiazimin(SN-124085)、嘧黄隆、杀草丹、丁草威、肟草酮、野麦畏、triasulfuron、triazofenamide、teibenuron-methyl、定草酯、tridiphane、草达津、氟乐灵、醚苯黄隆及其酯(例如甲基酯，DPX-66037)、三甲隆、tsitodef、灭草猛、WL 110547，即5-苯氧基-1-[3-(三氟甲基)-苯基]-1H-四唑、UBH-509、D-489、LS82-556、KPP-300、NC-324、NC-330、KH-218、DPX-N8189、SC-0774、DOWCO-535、DK-8910、V-53482、PP-600、MBH-001、KIH-9201、ET-751、KIH-6127和KIH-2023。
在使用时如果需要可以常规方式将市售形式的制剂稀释，例如用水稀释可湿性粉剂、可乳化浓缩液、分散和水分散颗粒剂，粉剂、用于土壤施用和撒播的颗粒剂以及可喷雾液剂，在使用前通常不需要用其它惰性物质稀释。
式(I)化合物的所需施用剂量可根据外部条件如温度、湿度、和使用除草剂的性质而变化。使用剂量可在很宽的范围内变化，例如0.001至10.0kg/ha或更多的活性物质；可是优选0.005至5kg/ha。A.化学实施例缩写：除非另外指明，百分比和量比指的是重量。
  i.v.＝在减压条件下
  h＝小时
实施例A1N-叔丁基-5-溴甲基-2-甲氧基羰基苯磺酰胺
将在420ml四氯甲烷中的54.8g(192mmol)的N-叔丁基-2-甲氧羰基-5-甲基苯磺酰胺在氮保护气下在加入36g(202mmol)的N-溴琥珀酰亚胺和0.5g的偶氮二异丁腈(AIBN)之后，在用日光灯照射的同时加热回流6-8小时。然后过滤溶液，并依次用亚硫酸氢钠溶液、碳酸氢钠溶液和水冲洗，用Na2SO4充分干燥并蒸发至干i.v.。从二异丙基醚/乙酸乙酯结晶剩余物，得到41.9g(57％)的N-叔丁基-5-溴甲基-2-甲氧基羰基苯磺酰胺，Fp.88-90℃。
实施例A2N-叔丁基-5-叠氮基甲基-2-甲氧基羰基苯磺酰胺
将25.5g(70mmol)的N-叔丁基-5-溴甲基-2-甲氧基羰基苯磺酰胺和5.9g(90mmol)的叠氮化钠在240ml乙醇中的溶液加热回流6小时。然后将溶液蒸发至干并用水/乙酸乙酯提取剩余物。用二异丙醚浸提粗产物，得到16.6g(72.5％)的N-叔丁基-5-叠氮基甲基-2-甲氧基羰基苯磺酰胺，Fp.63-65℃。
实施例A3N-叔丁基-5-氨基甲基-2-甲氧基羰基苯磺酰胺
将16.3g(50mmol)的N-叔丁基-5-叠氮基甲基-2-甲氧基羰基苯磺酰胺溶于300ml甲醇中并经Pd/C(5％)氢化。将混合物过滤并蒸发至干。将获得所粗产物通过硅胶粒洗脱纯化，用乙酸乙酯/甲醇4∶1作为洗脱液。获得粘稠油状的11.2g(74％)N-叔丁基-5-氨基甲基-2-甲氧基羰基苯磺酰胺。
1H NMR(100MHz，CDCl3)：δ＝1,25(s，9H，C(CH3)3)，
                           1,80 (bs，2H，NH2)，
                           3,95(s，3H，OCH3)，
                           4,00(s，2H，Ar-CH2)，
                           6,20(bs，1H，SO2NH)，
                           7,58(dd，1H，Ar-H)，
                           7,80(d，1H，Ar-H)，
                           8,10(dd，1H，Ar-H).
实施例A4N-叔丁基-5-乙酰氨基甲基-2-甲氧基羰基苯磺酰胺
将0.63g(8mmol)的乙酰氯溶于10ml二氯甲烷中并滴加到冷却到0℃的、2.01g(6.7mmol)N-叔丁基-5-氨基甲基-2-甲氧基羰基苯磺酰胺和0.93ml(6.7mmol)三乙胺的30ml二氯甲烷溶液中，在室温下搅拌混合物2小时。用水洗涤反应溶液，干燥并蒸发至干i.v.。获得粘稠油状的2.1g(91％)的N-叔丁基-5-乙酰氨基甲基-2-甲氧基羰基苯磺酰胺。
1H NMR(100MHz，CDCl3)：δ＝1,25(s，9H，C(CH3)3)，
                          2,05(s，3H，COCH3)，
                          3,95(s，3H，OCH3)，
                          4,50(s，2H，Ar-CH2)，
                          6,15(s，1H，SO2NH)，
                          6,38(bt，1H，NH)，
                          7,47(dd，1H，Ar-H)，
                          7,75(d，1H，Ar-H)，
                          7,95(dd，1H，Ar-H).
实施例A55-乙酰氨基甲基-2-甲氧基羰基苯磺酰胺
将2.09g(6.1mmol)N-叔丁基-5-乙酰氨基甲基-2-甲氧基羰基苯磺酰胺的25ml三氟乙酸溶液在室温下搅拌14小时，然后蒸发至干。从乙酸乙酯中结晶剩余物，得到1.33g(76％)的5-乙酰氨基甲基-2-甲氧基羰基苯磺酰胺，Fp.173-175℃。
实施例A6N-[4，6-(二甲氧基嘧啶-2-基)氨基羰基]-5-乙酰氨基甲基-2-甲氧基羰基苯磺酰胺
将0.69g(4.54mmol)的1，8-二氮杂二环[5.4.0]十一-7-烯(DBU)在0℃加入到1.3g(4.54mmol)的5-乙酰氨基甲基-2-甲氧羰基苯磺酰胺和1.25g(4.54mmol)的N-(4，6-二甲氧基嘧啶-2-基)苯基氨基甲酸酯的20ml乙腈悬浮液中。在室温下2小时后，用水和乙醚稀释混合物，用盐酸酸化到pH 1-2，过滤出所得沉淀并干燥。获得1.32g(62％)的N-[4，6-(二甲氧基嘧啶-2-基)氨基羰基]-5-乙酰氨基甲基-2-甲氧基羰基苯磺酰胺，mp.149-150℃。
采用实施例A1-A6的类似方法，可获得例示于下述表1-4中的式(I)化合物(W＝O，A＝嘧啶基或三嗪基)。在表中：Fp.＝熔点℃Vb＝化合物号＝实施例号Me＝甲基＝CH3Et＝乙基Bu＝n-Bu＝n-丁基＝n-C4H9Ph＝苯基
表1
Figure A9419413700411
Vb.   R1       R4   R5   R7   X         Y            Z   Fp.℃1    CO2CH3   H     CHO   H   OCH3      OCH3        CH  124-1252    ″         ″    ″    H   OCH3      CH3         CH3    ″         ″    ″    H   CH3       CH3         CH4    ″         ″    ″    H   CH3       OC2H5      CH5    ″         ″    ″    H   OCH3      OCH3        N6    ″         ″    ″    H   OCH3      CH3         N7    ″         ″    ″    H   OCH3      Cl           CH8    ″         ″    ″    H   OCF2H     CH3         CH9    ″         ″    ″    H   OCF2H     OCF2H       CH10   ″         ″    ″    H   OCH3      Br           CH11   ″         ″    ″    H   OCH3      OC2H5      CH12   ″         ″    ″    H   OCH3      SCH3        CH13   ″         ″    ″    H   OCH3      OC2H5      N14   ″         ″    ″    H   OCH3      OC3H7      CH15   ″         ″    ″    H   CH3       Cl           CH16   ″         ″    ″    H   Cl         OC2H5      CH17   ″         ″    ″    H   OC2H5    OC2H5      CH18   ″         ″    ″    H   C2H5     OCH3        CH19   ″         ″    ″    H   CF3       OCH3        CH20   ″         ″    ″    H   OCH2CF3  CH3         CH21   ″         ″    ″    H   OCH2CF3  OCH3        CH22   ″         ″    ″    H   OCH2CF3  OCH2CF3    CH23   ″         ″    ″    H   OCH2CF3  OCH3        N Vb.   R1   R4    R5     R7      X         Y       Z    Fp.C24    ″    ″    ″      H       OCH3      CH(OCH3)2  CH25    ″    ″    ″      CH3    OCH3      OCH3        CH26    ″    ″    ″      CH3    OCH3      CH3         N27    ″    H     COCH3  H       OCH3      OCH3        CH 149-15028    ″    ″    ″      H       OCH3      CH3         CH29    ″    ″    ″      H       CH3       CH3         CH30    ″    ″    ″      H       CH3       OC2H5      CH31    ″    ″    ″      H       OCH3      OCH3        N32    ″    ″    ″      H       OCH3      CH3         N33    ″    ″    ″      H       OCH3      Cl           CH34    ″    ″    ″      H       OCF2H     CH3         CH35    ″    ″    ″      H       OCF2H     OCF2H       CH36    ″    ″    ″      H       OCH3      Br           CH37    ″    ″    ″      H       OCH3      OC2H5      CH38    ″    ″    ″      H       OCH3      SCH3        CH39    ″    ″    ″      H       OCH3      OC2H5      N40    ″    ″    ″      H       OCH3      OC3H7      CH41    ″    ″    ″      H       CH3       Cl           CH42    ″    ″    ″      H       Cl         OC2H5      CH43    ″    ″    ″      H       OC2H5    OC2H5      CH44    ″    ″    ″      H       C2H5     OCH3        CH45    ″    ″    ″      H       CF3       OCH3        CH46    ″    ″    ″      H       OCH2CF3  CH3         CH47    ″    ″    ″      H       OCH2CF3  OCH3        CH48    ″    ″    ″      H       OCH2CF3  OCH2CF3    CH49    ″    ″    ″      H       OCH2CF3  OCH3        N50    ″    ″    ″      H       OCH3      CH(OCH3)2  CH51    ″    ″    ″      CH3    OCH3      OCH3        CH52    ″    ″    ″      CH3    OCH3      CH3          N53    ″    CH3  CHO     H       OCH3      OCH3        CH 171-17554    ″    ″    ″      H       OCH3      CH3         CH 135-14055    ″    ″    ″      H       CH3       CH3         CH 123-12656    ″    ″    ″      H       CH3       OC2H5      CH57    ″    ″    ″      H       OCH3      OCH3        N58    ″    ″    ″      H       OCH3      CH3         N  105 Vb.   R1   R4   R5     R7    X         Y            Z    Fp.C59    ″    ″    ″      H     OCH3      Cl           CH 125-13060    ″    ″    ″      H     OCF2H     CH3         CH61    ″    ″    ″      H     OCF2H     OCF2H       CH62    ″    ″    ″      H     OCH3      Br           CH63    ″    ″    ″      H     OCH3      OC2H5      CH64    ″    ″    ″      H     OCH3      SCH3        CH65    ″    ″    ″      H     OCH3      OC2H5      N66    ″    ″    ″      H     OCH3      OC3H7      CH67    ″    ″    ″      H     CH3       Cl           CH68    ″    ″    ″      H     Cl         OC2H5      CH69    ″    ″    ″      H     OC2H5    OC2H5      CH70    ″    ″    ″      H     C2H5     OCH3        CH71    ″    ″    ″      H     CF3       OCH3        CH72    ″    ″    ″      H     OCH2CF3  CH3         CH73    ″    ″    ″      H     OCH2CF3  OCH3        CH74    ″    ″    ″      H     OCH2CF3  OCH2CF3    CH75    ″    ″    ″      H     OCH2CF3  OCH3        N76    ″    ″    ″      H     OCH3      CH(OCH3)2  CH77    ″    ″    ″      CH3  OCH3      OCH3        CH78    ″    ″    ″      CH3  OCH3      CH3         N79    ″    CH3  COCH3  H     OCH3      OCH2       CH 146-14980    ″    ″    ″      H     OCH3      CH3         CH81    ″    ″    ″      H     CH3       CH3         CH82    ″    ″    ″      H     CH3       OC2H5      CH83    ″    ″    ″      H     OCH3      OCH3        N84    ″    ″    ″      H     OCH3      CH3         N85    ″    ″    ″      H     OCH3      Cl           CH86    ″    ″    ″      H     OCF2H     CH3         CH87    ″    ″    ″      H     OCF2H     OCF2H       CH88    ″    ″    ″      H     OCH3      Br           CH89    ″    ″    ″      H     OCH3      OC2H5      CH90    ″    ″    ″      H     OCH3      SCH3        CH91    ″    ″    ″      H     OCH3      OC2H5      N92    ″    ″    ″      H     OCH3      OC3H7      CH93    ″    ″    ″      H     CH3       Cl            CH Vb.   R1   R4   R5     R7      X          Y            Z  Fp.℃94    ″    ″    ″       H       Cl         OC2H5      CH95    ″    ″    ″      H       OC2H5    OC2H5      CH96    ″    ″    ″      H       C2H5     OCH3        CH97    ″    ″    ″      H       CF3       OCH3        CH98    ″    ″    ″      H       OCH2CF3  CH3         CH99    ″    ″    ″      H       OCH2CF3  OCH3        CH100   ″    ″    ″      H       OCH2CF3  OCH2CF3    CH101   ″    ″    ″      H       OCH2CF3  OCH3        N102   ″    ″    ″      H       OCH3      CH(OCH3)2  CH103   ″    ″    ″      CH3    OCH3      OCH3        CH104   ″    ″    ″      CH3    OCH3      CH3         N105   ″    H    SO2CH3H       OCH3      OCH3        CH 192-194106   ″    ″    ″      H       OCH3      CH3         CH107   ″    ″    ″      H       CH3       CH3         CH108   ″    ″    ″      H       OCH3      OCH3        N109   ″    ″    ″      H       OCH3      CH3         N110   ″    ″    ″      H       OC2H5    NHCH3       N111   ″    ″    ″      CH3    OCH3      OCH3        CH112   ″    ″    ″      CH3    OCH3      CH3         N113   ″    CH3 SO2CH3H       OCH3      OCH3        CH 107-109114   ″    ″    ″      H       OCH3      CH3         CH115   ″    ″    ″      H       CH3       CH3         CH116   ″    ″    ″      H       OCH3      OCH3        N117   ″    ″    ″      H       OCH3      CH3         N118   ″    ″    ″      H       OC2H5    NHCH3       N119   ″    ″    ″      CH3    OCH3      OCH3        CH120   ″    ″    ″      CH3    OCH3      CH3         N121   ″    OH    CHO     H       OCH3      OCH3        CH122   ″    ″    ″      H       OCH3      CH3         CH123   ″    ″    ″      H       CH3       CH3         CH124   ″    ″    ″      H       OCH3      OCH3        N125   ″    ″    ″      H       OCH3      CH3         N126   ″    ″    ″      H       OC2H5    NHCH3       N127   ″    ″    ″      CH3    OCH3      OCH3        CH128   ″    ″    ″      CH3    OCH3      CH3         N Vb.    R1   R4   R5          R7   X       Y       Z    Fp.℃129    ″    OCH3 CHO          H    OCH3   OCH3    CH 142-145130    ″    ″    ″           H    OCH3   CH3     CH131    ″    ″    ″           H    CH3    CH3     CH132    ″    ″    ″           H    OCH3   OCH3    N133    ″    ″    ″           H    OCH3   CH3     N134    ″    ″    ″           H    OC2H5 NHCH3   N135    ″    ″    ″           CH3 OCH3   OCH3    CH136    ″    ″    ″           CH3 OCH3   CH3     N137    ″    OH    COCH3       H    OCH3   OCH3    CH138    ″    ″    ″           H    OCH3   CH3     CH139    ″    ″    ″           H    CH3    CH3     CH140    ″    ″    ″           H    OCH3   OCH3    N141    ″    ″    ″           H    OCH3   CH3     N142    ″    ″    ″           H    OC2H5 NHCH3   N143    ″    ″    ″           CH3 OCH3   OCH3    CH144    ″    ″    ″           CH3 OCH3   CH3     N145    ″    OCH3 COCH3      H    OCH3   OCH3    CH 195-196146    ″    ″    ″           H    OCH3   CH3      CH147    ″    ″    ″           H    CH3    CH3     CH148    ″    ″    ″           H    OCH3   OCH3    N149    ″    ″    ″           H    OCH3   CH3     N150    ″    ″    ″           H    OC2H5 NHCH3   N151    ″    ″    ″           CH3 OCH3   OCH3    CH152    ″    ″    ″           CH3 OCH3   CH3     N153    ″    H     COC2H5    H    OCH3   OCH3    CH 150-152154    ″    ″    ″           H    OCH3   CH3     CH155    ″    ″    ″           H    OCH3   OCH3    N156    ″    ″    ″           H    OCH3   CH3     N157    ″   CH3   ″          H    OCH3    OCH3    CH158    ″    ″    ″           H    OCH3   CH3     CH159    ″    ″    ″           H    OCH3   OCH3    N160    ″    ″    ″           H    OCH3   CH3     N161    ″    H     COCH2OCH3 H    OCH3   OCH3    CH162    ″    ″    ″           H    OCH3   CH3     CH163    ″    ″    ″           H    OCH3   OCH3    N Vb.    R1   R4   R5         R7   X       Y     Z  Fp.℃164    ″    ″    ″            H    OCH3   CH3   N165    ″    CH3 ″             H    OCH3   OCH3  CH166    ″    ″    ″            H    OCH3   CH3   CH167    ″    ″    ″            H    OCH3   OCH3  N168    ″    ″    ″            H    OCH3   CH3   N169    ″    H     COCO2C2H5 H    OCH3   OCH3  CH170    ″    ″    ″            H    OCH3   CH3   CH171    ″    ″    ″            H    OCH3   OCH3  N172    ″    ″    ″            H    OCH3   CH3   N173    ″    CH3  ″           H    OCH3   OCH3  CH174    ″    ″    ″            H    OCH3   CH3   CH175    ″    ″    ″            H    OCH3   OCH3  N176    ″    ″    ″            H    OCH3   CH3   N177    ″    H     COCF3        H    OCH3   OCH3  CH 158178    ″    ″    ″            H    OCH3   CH3   CH179    ″    ″    ″            H    OCH3   OCH3  N180    ″    ″    ″            H    OCH3   CH3   N181    ″    CH3  ″            H    OCH3   OCH3  CH 144-147182    ″    ″    ″            H    OCH3   CH3   CH183    ″    ″    ″            H    OCH3   OCH3  N184    ″    ″    ″            H    OCH3   CH3   N185    ″    H     COOCH3       H    OCH3   OCH3  CH 160-161186    ″    ″    ″            H    OCH3   CH3   CH187    ″    ″    ″            H    OCH3   OCH3  N188    ″    ″    ″            H    OCH3   CH3   N189    ″    CH3  ″            H    OCH3   OCH3  CH 157-159190    ″    ″    ″            H    OCH3   CH3   CH191    ″    ″    ″            H    OCH3   OCH3  N192    ″    ″    ″            H    OCH3   CH3   N193    ″    H     CONHC2H5    H    OCH3   OCH3  CH194    ″    ″    ″            H    OCH3   CH3   CH195    ″    ″    ″            H    OCH3   OCH3  N196    ″    ″    ″            H    OCH3   CH3   N197    ″    CH3  ″            H    OCH3   OCH3  CH198    ″    ″    ″            H    OCH3   CH3   CH Vb.    R1   R4   R5         R7   X       Y      Z Fp.℃199    ″    ″    ″          H    OCH3   OCH3   N200    ″    ″    ″          H    OCH3   CH3    N201    ″    H  CSNHC2H5    H    OCH3   OCH3   CH202    ″    ″    ″          H    OCH3   CH3    CH203    ″    ″    ″          H    OCH3   OCH3   N204    ″    ″    ″          H    OCH3   CH3    N205    ″    CH3  ″          H    OCH3   OCH3   CH206    ″    ″    ″          H    OCH3   CH3    CH207    ″    ″    ″          H    OCH3   OCH3   N208    ″    ″    ″          H    OCH3   CH3    N209    ″    H  SO2NHCH3    H    OCH3   OCH3   CH210    ″    ″    ″          H    OCH3   CH3    CH211    ″    ″    ″          H    OCH3   OCH3   N212    ″    ″    ″          H    OCH3   CH3    N213    ″   CH3   ″          H    OCH3   OCH3   CH 171-173214    ″    ″    ″          H    OCH3   CH3    CH215    ″    ″    ″          H    OCH3   OCH3   N216    ″    ″    ″          H    OCH3   CH3    N217    ″    H SO2N(CH3)2  H    OCH3   OCH3   CH 162218    ″    ″    ″          H    OCH3   CH3    CH219    ″    ″    ″          H    OCH3   OCH3   N220    ″    ″    ″          H    OCH3   CH3    N221    ″   CH3   ″          H    OCH3   OCH3   CH 127-129222    ″    ″    ″          H    OCH3   CH3    CH223    ″    ″    ″          H    OCH3   OCH3   N224    ″    ″    ″          H    OCH3   CH3    N225    ″-CH2CH2CH2CO-     H    OCH3   OCH3   CH226    ″       ″             H    OCH3   CH3    CH227    ″       ″             H    OCH3   OCH3   N228    ″       ″             H    OCH3   CH3    N229    ″-CH2CH2CH2SO2-   H    OCH3   OCH3   CH230    ″       ″             H    OCH3   CH3    CH231    ″       ″             H    OCH3   OCH3   N232    ″       ″             H    OCH3   CH3    N233    ″-CH2CH2CH2CH2CO- H    OCH3   OCH3   CH Vb.    R1   R4   R5              R7   X       Y     Z    Fp.℃234    ″          ″               H    OCH3   CH3   CH235    ″          ″               H    OCH3   OCH3  N236    ″          ″               H    OCH3   CH3   N237    ″    -CH2CH2CH2CH2SO2- H  OCH3   OCH3  CH238    ″          ″               H    OCH3   CH3   CH239    ″          ″               H    OCH3   OCH3  N240    ″          ″               H    OCH3   CH3   N241    ″    -CH2CH2OCH2CH2-  H    OCH3   OCH3  CH242    ″          ″               H    OCH3   CH3   CH243    ″          ″               H    OCH3   OCH3  N244    ″          ″               H    OCH3   CH3   N245    ″    H          COC3H7    H    OCH3   OCH3  CH246    ″    ″         ″          H    OCH3   CH3   CH247    ″    ″         ″          H    OCH3   OCH3  N248    ″    ″         ″          H    OCH3   CH3   N249    ″    CH3       ″          H    OCH3   OCH3  CH250    ″    ″         ″          H    OCH3   CH3   CH251    ″    ″         ″          H    OCH3   OCH3  N252    ″    ″         ″          H    OCH3   CH3   N253    ″    H          COCH2Cl    H    OCH3   OCH3  CH 144-145254    ″    ″         ″          H    OCH3   CH3   CH255    ″    ″         ″          H    OCH3   OCH3  N256    ″    ″         ″          H    OCH3   CH3   N257    ″    CH3       ″          H    OCH3   OCH3  CH 138-140258    ″    ″         ″          H    OCH3   CH3   CH259    ″    ″         ″          H    OCH3   OCH3  N260    ″    ″         ″          H    OCH3   CH3   N261    ″    H          COCHCl2    H    OCH3   OCH3  CH262    ″    ″         ″          H    OCH3   CH3   CH263    ″    ″         ″          H    OCH3   OCH3  N264    ″    ″         ″          H    OCH3   CH3   N265    ″    CH3       ″          H    OCH3   OCH3  CH266    ″    ″         ″          H    OCH3   CH3   CH267    ″    ″         ″          H    OCH3   OCH3  N268    ″    ″         ″          H    OCH3   CH3   N Vb.    R1   R4         R5         R7   X      Y      Z Fp.℃269    ″    H           COCCl3    H    OCH3   OCH3  CH270    ″    ″          ″         H    OCH3   CH3   CH271    ″    ″          ″         H    OCH3   OCH3  N272    ″    ″          ″         H    OCH3   CH3   N273    ″    CH3        ″         H    OCH3   OCH3  CH274    ″    ″          ″         H    OCH3   CH3   CH275    ″    ″          ″         H    OCH3   OCH3  N276    ″    ″          ″         H    OCH3   CH3   N277    ″    H           COCH＝CH2 H    OCH3   OCH3  CH278    ″    ″          ″         H    OCH3   CH3   CH279    ″    ″          ″         H    OCH3   OCH3  N280    ″    ″          ″         H    OCH3   CH3   N281    ″    CH3        ″         H    OCH3   OCH3  CH282    ″    ″          ″         H    OCH3   CH3   CH283    ″    ″          ″         H    OCH3   OCH3  N284    ″    ″          ″         H    OCH3   CH3   N285    ″    H           COC＝CH    H    OCH3   OCH3  CH286    ″    ″          ″         H    OCH3   CH3   CH287    ″    ″          ″         H    OCH3   OCH3  N288    ″    ″          ″         H    OCH3   CH3   N289    ″    CH3        ″         H    OCH3   OCH3  CH290    ″    ″          ″         H    OCH3   CH3   CH291    ″    ″          ″         H    OCH3   OCH3  N292    ″    ″          ″         H    OCH3   CH3   N293    ″    H           COC6H5  H    OCH3   OCH3  CH294    ″    ″          ″         H    OCH3   CH3   CH295    ″    ″          ″         H    OCH3   OCH3  N296    ″    ″          ″         H    OCH3   CH3   N297    ″    CH3        ″         H    OCH3   OCH3 CH298    ″    ″          ″         H    OCH3   CH3   CH299    ″    ″          ″         H    OCH3   OCH3  N300    ″    ″          ″         H    OCH3   CH3   N301    ″    SO2C6H5 SO2C6H5H    OCH3   OCH3  CH302    ″    ″          ″         H    OCH3   CH3   CH303    ″    ″          ″         H    OCH3   OCH3  N Vb.    R1   R4      R5          R7   X       Y     Z Fp.℃304    ″    ″       ″           H    OCH3   CH3   N305    ″    SO2CH3 SO2CH3    H    OCH3   OCH3  CH306    ″    ″       ″           H    OCH3   CH3   CH307    ″    ″       ″           H    OCH3   OCH3  N308    ″    ″       ″           H    OCH3   CH3   N309    ″    H        COCH2Br     H    OCH3   OCH3  CH310    ″    ″       ″           H    OCH3   CH3   N311    ″    CH3     ″           H    OCH3   OCH3  CH312    ″    ″       ″           H    OCH3   CH3   N313    ″    H        COCH2F      H    OCH3   OCH3  CH314    ″    ″       ″           H    OCH3   CH3   N315    ″    CH3     ″           H    OCH3   OCH3  CH316    ″    ″       ″           H    OCH3   CH3   N317    ″    H        COCH2C＝CH  H    OCH3   OCH3  CH318    ″    ″       ″           H    OCH3   CH3   N319    ″    CH3     ″           H    OCH3   OCH3  CH320    ″    ″       ″           H    OCH3   CH3   N321    ″    H        COCO2CH3   H    OCH3   OCH3  CH322    ″    ″       ″           H    OCH3   CH3   N323    ″    CH3     ″           H    OCH3   OCH3  CH324    ″    ″       ″           H    OCH3   CH3   N325    ″    H        CO2C2H5  H    OCH3    OCH3  CH326    ″    ″       ″           H    OCH3   CH3   N327    ″    CH3     ″           H    OCH3   OCH3  CH328    ″    ″       ″           H    OCH3   CH3   N329    ″    H        COSCH3      H    OCH3   OCH3  CH330    ″    ″       ″           H    OCH3   CH3   N331    ″    CH3     ″           H    OCH3   OCH3  CH332    ″    ″       ″           H    OCH3   CH3   N333    ″    H        CSOCH3      H    OCH3   OCH3  CH334    ″    ″       ″           H    OCH3    CH3   N335    ″    CH3     ″           H    OCH3   OCH3  CH336    ″    ″       ″           H    OCH3   CH3   N337    ″    H        CSSCH3      H    OCH3   OCH3  CH338    ″    ″       ″           H    OCH3   CH3   N Vb.   R1   R4   R5              R7 X       Y     Z Fp.℃339   ″    CH3  ″               H  OCH3   OCH3  CH340   ″    ″    ″               H  OCH3   CH3   N341   ″    H     COCH(CH3)2    H  OCH3   OCH3  CH342   ″    ″    ″               H  OCH3   CH3   N343   ″    CH3  ″               H  OCH3   OCH3  CH344   ″    ″    ″               H  OCH3   CH3   N345   ″    H     COC(CH3)3     H  OCH3   OCH3  CH346   ″    ″    ″               H  OCH3   CH3   N347   ″    CH3  ″               H  OCH3   OCH3  CH348   ″    ″    ″               H  OCH3   CH3   N349   ″    H     CO-环丙基        H  OCH3   OCH3  CH350   ″    ″    ″               H  OCH3   CH3   N351   ″    CH3  ″               H  OCH3   OCH3  CH352   ″    ″    ″               H  OCH3   CH3   N353   ″    H     CO环丁基         H  OCH3   OCH3  CH354   ″    ″    ″               H  OCH3   CH3   N355   ″    CH3  ″               H  OCH3   OCH3  CH356   ″    ″    ″               H  OCH3   CH3   N357   ″    H     CO-环戊基        H  OCH3   OCH3  CH358   ″    ″    ″               H  OCH3   CH3   N359   ″    CH3  ″               H  OCH3   OCH3  CH360   ″    ″    ″               H  OCH3   CH3   N361   ″    H     CO-环己基        H  OCH3   OCH3  CH362   ″    ″    ″               H  OCH3   CH3   N363   ″    CH3  ″               H  OCH3   OCH3  CH364   ″    ″    ″               H  OCH3   CH3   N365   ″    H     CONHCH2CH2Cl  H  OCH3   OCH3  CH366   ″    ″    ″               H  OCH3   CH3   N367   ″    CH3  ″               H  OCH3   OCH3 CH368   ″    ″    ″               H  OCH3   CH3   N369   ″    H     CSNHCH2CH2Cl  H  OCH3   OCH3  CH370   ″    ″    ″               H  OCH3   CH3   N371   ″    CH3  ″               H  OCH3   OCH3  CH372   ″    ″    ″               H  OCH3   CH3   N373   ″    H     CONH-n-C4H9   H  OCH3   OCH3  CH Vb.    R1   R4            R5                 R7       X        Y     Z     Fp.℃374    ″    ″             ″                   H         OCH3   CH3   N375    ″    CH3           ″                  H         OCH3   OCH3  CH376    ″    ″             ″                  H         OCH3   CH3   N377    ″    H              CSNHCH3           H         OCH3   OCH3  CH378    ″    ″             ″                  H         OCH3   CH3   N379    ″    CH3           ″                  H         OCH3   OCH3  CH380    ″    ″             ″                  H         OCH3   CH3   N381    ″    H              CSNHCH2CH＝CH2   H         OCH3   OCH3  CH382    ″    ″             ″                  H         OCH3   CH3   N383    ″    CH3           ″                  H         OCH3   OCH3  CH384    ″    ″             ″                  H         OCH3   CH3   N385    ″    CH3           CSNHCH2COCH3     H         OCH3   OCH3  CH386    ″    ″             ″                  H         OCH3   CH3   N387    ″    CH3           CSNHCH2COC2H5   H         OCH3   OCH3  CH388    ″    ″             ″                  H         OCH3   CH3   N389    ″    CH3           CONHCH2COCH3     H         OCH3   OCH3  CH390    ″    ″             ″                  H         OCH3   CH3   N391    ″    CH3           CONHCH2COC2H5   H         OCH3   OCH3  CH392    ″    ″             ″                  H         OCH3   CH3   N393    ″    -CONHCH2CO-                       H         OCH3   OCH3  CH394    ″    ″                                 H         OCH3   CH3   N395    ″    H              SO2CH2F          H         OCH3   OCH3  CH396    ″    ″             ″                  H         OCH3   CH3   N397    ″    CH3           ″                  H         OCH3   OCH3  CH398    ″    ″             ″                  H         OCH3   CH3   N399    ″    H              SO2CF3           H         OCH3   OCH3  CH400    ″    ″             ″                  H         OCH3   CH3   N401    ″    CH3           ″                  H         OCH3   OCH3  CH402    ″    ″             ″                  H         OCH3   CH3   N403    ″    H              SO2C2H5         H         OCH3   OCH3  CH404    ″    ″             ″                  H         OCH3   CH3   N405    ″    CH3           ″                  H         OCH3   OCH3  CH406    ″    ″             ″                  H         OCH3   CH3   N407    ″    H              SO2-n-C3H7      H         OCH3   OCH3  CH408    ″    ″             ″                  H         OCH3   CH3   N Vb.    R1   R4    R5            R7    X       Y     Z  Fp.℃409    ″    CH3   ″              H    OCH3   OCH3  CH410    ″    ″     ″              H    OCH3   CH3   N411    ″    OH     COC2H5       H    OCH3   OCH3  CH412    ″    ″     ″              H    OCH3   CH3   N413    ″    OCH3  ″              H    OCH3   OCH3  CH414    ″    ″     ″              H    OCH3   CH3   N415    ″    OH     COCH2Cl        H    OCH3   OCH3  CH416    ″    ″     ″              H    OCH3   CH3   N417    ″    OCH3  ″              H    OCH3   OCH3  CH418    ″    ″     ″              H    OCH3   CH3   N419    ″    OH     COCF3          H    OCH3   OCH3  CH420    ″    ″     ″              H    OCH3   CH3   N421    ″    OCH3  ″              H    OCH3   OCH3  CH 159-161422    ″    ″     ″              H    OCH3   CH3   N423    ″    OH     COCH2OCH3     H    OCH3   OCH3  CH424    ″    ″     ″              H    OCH3   CH3   N425    ″    OCH3  ″              H    OCH3   OCH3  CH 130-131426    ″    ″     ″              H    OCH3   CH3   N427    ″    OH     COCO2C2H5   H    OCH3   OCH3  CH428    ″    ″     ″              H    OCH3   CH3   N429    ″    OCH3  ″              H    OCH3   OCH3  CH 158-159430    ″    ″     ″              H    OCH3   CH3   N431    ″    OH     COOCH3        H    OCH3   OCH3  CH432    ″    ″     ″              H    OCH3   CH3   N433    ″    OCH3  ″              H    OCH3   OCH3  CH 137-138434    ″    ″     ″              H    OCH3   CH3   N435    ″    OH     Cyclopropyl     H    OCH3   OCH3  CH436    ″    ″     ″              H    OCH3   CH3   N437    ″    OCH3  ″              H    OCH3   OCH3  CH 118-120438    ″    ″     ″              H    OCH3   CH3   N439    ″    OH     COC6H5       H    OCH3   OCH3  CH440    ″    ″     ″              H    OCH3   CH3   N441    ″    OCH3  ″              H    OCH3   OCH3  CH442    ″    ″     ″              H    OCH3   CH3   N443    ″    OH     COCH(CH3)2   H    OCH3   OCH3  CH Vb.    R1   R4   R5           R7X      Y     Z    Fp.℃444    ″    ″    ″             H OCH3   CH3   N445    ″    OCH3 ″            H OCH3   OCH3  CH  126-128446    ″    ″    ″            H OCH3   CH3   N447    ″    OH    COCH＝CH2    H OCH3   OCH3  CH448    ″    ″    ″            H OCH3   CH3   N449    ″    OCH3 ″            H OCH3   OCH3  CH450    ″    ″    ″            H OCH3   CH3   N451    ″    OH    COC＝CH       H OCH3   OCH3  CH452    ″    ″    ″            H OCH3   CH3   N453    ″    OCH3 ″            H OCH3   OCH3  CH454    ″    ″    ″            H OCH3   CH3   N455    ″    OH    SO2CH3     H OCH3    OCH3  CH456    ″    ″    ″            H OCH3   CH3   N457    ″    OCH3 ″            H OCH3   OCH3  CH  146-148458    ″    ″    ″            H OCH3   CH3   N459    ″    OH    SO2NHCH3   H OCH3   OCH3  CH460    ″    ″    ″            H OCH3   CH3   N461    ″    OCH3 ″            H OCH3   OCH3  CH  179-180462    ″    ″    ″            H OCH3   CH3   N463    ″    OH    SO2N(CH3)2H OCH3   OCH3  CH464    ″    ″    ″            H OCH3   CH3   N465    ″    OCH3 ″            H OCH3   OCH3  CH  179-180466    ″    ″    ″            H OCH3   CH3   N467    ″    C2H5CHO          H OCH3   OCH3  CH  168-170468    ″    ″    ″            H OCH3   CH3   N469    ″    ″    COCH3        H OCH3   OCH3  CH470    ″    ″    ″            H OCH3   CH3   N471    ″    ″    环丙基        H OCH3   OCH3  CH472    ″    ″    ″            H OCH3   CH3   N473    ″    ″    COCH2Cl      H OCH3   OCH3  CH474    ″    ″    ″            H OCH3   CH3   N475    ″    ″    COCF3        H OCH3   OCH3  CH476    ″    ″    ″            H OCH3   CH3   N477    ″    ″    COOCH3       H OCH3   OCH3  CH478    ″    ″    ″            H OCH3   CH3   N Vb.    R1         R4     R5           R7   X       Y     Z  Fp.℃479    ″          ″      COC6H5      H    OCH3   OCH3  CH480    ″          ″      ″            H    OCH3   CH3   N481    ″          ″      CONHC2H5   H    OCH3   OCH3  CH482    ″          ″      ″            H    OCH3   CH3   N483    ″          ″      CSNHC2H5   H    OCH3   OCH3  CH484    ″          ″      ″            H    OCH3   CH3   N485    ″          ″      SO2CH3     H    OCH3   OCH3  CH 154-155486    ″          ″      ″            H    OCH3   CH3   N487    ″          ″      SO2NHCH3   H    OCH3   OCH3  CH 150-152488    ″          ″      ″            H    OCH3   CH3   N489    ″          ″      SO2N(CH3)2H    OCH3   OCH3  CH490    ″          ″      ″            H    OCH3   CH3   N491    ″          ″      SO2C6H5   H    OCH3   OCH3  CH492    ″          ″      ″            H    OCH3   CH3   N493    CO2C2H5  H       CHO          H    OCH3   OCH3  CH494    ″          ″      ″            H    OCH3   CH3   N495    ″          ″      COCH3       H    OCH3   OCH3  CH496    ″          ″      ″            H    OCH3   CH3   N497    ″          ″      SO2CH3     H    OCH3   OCH3  CH498    ″          ″      ″            H    OCH3   CH3   N499    ″          CH3    CHO           H    OCH3   OCH3  CH500    ″          ″      ″            H    OCH3   CH3   N501    ″          ″      COCH3        H    OCH3   OCH3  CH502    ″          ″      ″            H    OCH3   CH3   N503    ″          ″      SO2CH3     H    OCH3   OCH3  CH504    ″          ″      ″            H    OCH3   CH3   N505    ″          C2H5  CHO          H    OCH3   OCH3  CH506    ″          ″      ″            H    OCH3   CH3   N507    ″          ″      COCH3       H    OCH3   OCH3  CH508    ″          ″      ″            H    OCH3   CH3   N509    ″          ″      SO2CH3     H    OCH3   OCH3  CH510    ″          ″      ″            H    OCH3   CH3   N511    ″          OH      CHO           H    OCH3   OCH3  CH512    ″          ″      ″            H    OCH3   CH3   N513    ″          ″      COCH3       H    OCH3   OCH3  CH Vb.    R1          R4       R5       R7  X        Y         Z  Fp.℃514    ″            ″      ″          H  OCH3      CH3      N515    ″           ″      SO2CH3   H  OCH3      OCH3     CH516    ″           ″      ″          H  OCH3      CH3      N517    ″           OCH3   CHO         H  OCH3      OCH3     CH518    ″           ″      ″          H  OCH3      CH3      N519    ″           ″      COCH3      H  OCH3      OCH3     CH520    ″           ″      ″          H  OCH3      CH3      N521    CO2-n-Bu    H       CHO         H  OCH3      OCH3     CH522    CON(CH3)2 CH3    CHO         H  OCH3      CH3      N523    CONHCH3     H       CHO         H  OCH3      OCH3     CH524    COSCH3     CH3    COCH3      H  OCH3      CH3      N525    CO2CH3     n-Bu    CHO        H  OCH3      OCH3     CH526    ″           ″      ″          H  OCH3      CH3      N527    ″           H       ″          H  OCH2CF3  N(CH3)2 N528    ″           CH3    ″          H  ″         ″        N529    ″           H       COCH3      H  ″         ″        ″530    ″           CH3    ″          H  ″         ″        ″531    ″           ″      SO2CH3    H  OCH3      OCH3     CH532    ″           ″      ″          H  OCH3      CH3      N533    CO2CH3
Figure A9419413700561
H OCH3       OCH3     CH534    ″           ″                  H  OCH3      CH3      N535    CO2CH3     CH3    CHO        H  OCH3      OCH3     CH  钠盐236-238536    CO2CH3     H       SO2CH3   H  OCH3      OCH3     CH  钠盐170-173537    CO2CH3     CH3    SO2CH3   H  OCH3      OCH3     CH  钠盐191538    CO2CH3     OCH3   CHO        H  OCH3      OCH3     CH  钠盐215-216539    CO2CH3     OCH3   COCH3     H  OCH3       OCH3    CH  钠盐 Vb.    R1    R4     R5          R7 X        Y   Z    Fp.℃540 CO2CH3  H      COOCH3         H  OCH3   OCH3   CH  钠盐203-205541 CO2CH3  CH3   SO2N(CH3)2  H  OCH3   OCH3   CH  钠盐122542 CO2CH3  CH3   CONHEt         H  OCH3   OCH3   CH   钠盐190-192543 CO2CH3  CH3   CONHEt         H  OCH3   OCH3   CH    150-152544 CO2CH3  CH3   CONHEt         H  OCH3   CH3    N545 CO2CH3  H      CONHEt         H  OCH3   OCH3   CH546 CO2CH3  H      CONHEt         H  OCH3   CH3    N547 CO2CH3    -CO-CH2CH2-CO-   H  OCH3   OCH3   CH    220-221548 CO2CH3    -CO-CH2CH2-CO-   H  OCH3   OCH3   N549 CO2CH3    -CO-CH2CH2-CO-   H  OCH3   CH3    CH550 CO2CH3    -CO-CH2CH2-CO-   H  OCH3   CH3    N551 CO2CH3    -CO-CH2CH2-CO-   H  OCH3   OCH3   CH    钠盐210-212552 CO2CH3  OCH3  COCF3        H  OCH3   OCH3   CH    钠盐228-229553 CO2CH3  OCH3  COOCH3       H  OCH3   OCH3   CH    钠盐184-185554 CO2CH3  OCH3  Cyclopropyl   H  OCH3   OCH3   CH    钠盐216555 CO2CH3  OCH3  SO2CH3      H  OCH3   OCH3   CH   钠盐183-185556 CO2CH3  C2H5 CHO           H  OCH3   OCH3   CH    钠盐237-239557 CO2CH3  C2H5 Cyclopropyl   H  OCH3   OCH3   CH    钠盐178-180558 CO2CH3  C2H5 COCCl3       H  OCH3   OCH3   CH    109-111559 CO2CH3  C2H5 COCCl3       H  OCH3   OCH3   CH    钠盐174-176560 CO2CH3  C2H5 COCCl3       H  OCH3   CH3    N561 CO2CH3  C2H5 COCOOCH3     H  OCH3   CH3    N562 CO2CH3  C2H5 COCOOCH3     H  OCH3   OCH3   CH    138-140563 CO2CH3  C2H5 COCH2OCH3   H  OCH3   OCH3   CH    121-123Vb.  R1        R4     R5            R7 X       Y      Z    Fp.℃564 CO2CH3   C2H5  COCH2OCH3   H   OCH3   CH3    N565 CO2CH3   C2H5  SO2CH3      H   OCH3   OCH3   CH   154-155566 CO2CH3   C2H5  SO2CH3      H   OCH3   OCH3   CH   钠盐161567 CO2CH3   C2H5  SO2NHCH3    H   OCH3   OCH3   CH   150-152568 CO2CH3   C2H5  SO2NHCH3    H   OCH3   OCH3   CH   钠盐165-168569 CO2CH3   OC2H5 SO2CH3      H   OCH3   OCH3   CH   163-164570 CO2CH3   OC2H5 SO2CH3      H   OCH3   OCH3   CH   钠盐166-168571 CO2CH3   OC2H5 CHO           H   OCH3   OCH3   CH   165-166572 CO2CH3   OC2H5 CHO           H   OCH3   OCH3   CH   钠盐207-208573 CO2CH3   OCH3   CONHPh        H   OCH3   OCH3   CH   178-179574 CO2CH3   OCH3   CONHEt        H   OCH3   OCH3   CH   155-157575 CO2CH3   OCH3   COCCl3       H   OCH3   OCH3   CH   165-168576 CO2CH3   OCH3   COCCl3       H   OCH3   OCH3   CH   钠盐100577 CO2CH3   OCH3   COCHCl2      H   OCH3   OCH3   CH   145-150578 CO2CH3   OCH3   COCHCl2      H   OCH3   OCH3   CH   钠盐235表2
Figure A9419413700591
Vb.    R1       R4   R5   R7   X         Y          Z  Fp.℃1     CO2CH3  H     CHO   H    OCH3      OCH3      CH 142-1442     ″        ″    ″    H    OCH3      CH3       CH3     ″        ″    ″    H    CH3       CH3       CH4     ″        ″    ″    H    CH3       OC2H5    CH5     ″        ″    ″    H    OCH3      OCH3      N6     ″        ″    ″    H    OCH3      CH3       N7     ″        ″    ″    H    OCH3      Cl         CH8     ″        ″    ″    H    OCF2H     CH3       CH9     ″        ″    ″    H    OCF2H     OCF2H     CH10    ″        ″    ″    H    OCH3      Br         CH11    ″        ″    ″    H    OCH3      OC2H5    CH12    ″        ″    ″    H    OCH3      SCH3      CH13    ″        ″    ″    H    OCH3      OC2H5    N14    ″        ″    ″    H    OCH3      OC3H7    CH15    ″        ″    ″    H    CH3       Cl         CH16    ″        ″    ″    H    Cl         OC2H5    CH17    ″        ″    ″    H    OC2H5    OC2H5    CH18    ″        ″    ″    H    C2H5     OCH3      CH19    ″        ″    ″    H    CF3       OCH3      CH20    ″        ″    ″    H    OCH2CF3  CH3       CH21    ″        ″    ″    H    OCH2CF3  OCH3      CH22    ″        ″    ″    H    OCH2CF3  OCH2CF3  CH23    ″        ″    ″    H    OCH2CF3  OCH3      N24    ″        ″    ″    H    OCH3      CH(OCH3)2CH25    ″        ″    ″    CH3 OCH3      OCH3      CH Vb.   R1   R4   R5     R7   X         Y            Z    Fp.℃26    ″    ″    ″      CH3 OCH3      CH3         N27    ″    H     COCH3  H    OCH3      OCH3        CH   167-16928    ″    ″    ″      H    OCH3      CH3         CH29    ″    ″    ″      H    CH3       CH3         CH30    ″    ″    ″      H    CH3       OC2H5      CH31    ″    ″    ″      H    OCH3      OCH3        N32    ″    ″    ″      H    OCH3      CH3         N33    ″    ″    ″      H    OCH3      Cl           CH34    ″    ″    ″      H    OCF2H     CH3         CH35    ″    ″    ″      H    OCF2H     OCF2H       CH36    ″    ″    ″      H    OCH3      Br           CH37    ″    ″    ″      H    OCH3      OC2H5      CH38    ″    ″    ″      H    OCH3      SCH3        CH39    ″    ″    ″      H    OCH3      OC2H5      N40    ″    ″    ″      H    OCH3      OC3H7      CH41    ″    ″    ″      H    CH3       Cl           CH42    ″    ″    ″      H    Cl         OC2H5      CH43    ″    ″    ″      H    OC2H5    OC2H5      CH44    ″    ″    ″      H    C2H5     OCH3        CH45    ″    ″    ″      H    CF3       OCH3        CH46    ″    ″    ″      H    OCH2CF3  CH3         CH47    ″    ″    ″      H    OCH2CF3  OCH3        CH48    ″    ″    ″      H    OCH2CF3  OCH2CF3    CH49    ″    ″    ″      H    OCH2CF3  OCH3        N50    ″    ″    ″      H    OCH3       CH(OCH3)2  CH51    ″    ″    ″      CH3 OCH3      OCH3        CH52    ″    ″    ″      CH3 OCH3      CH3         N53    ″    CH3  CHO     H    OCH3      OCH3        CH   160-16254    ″    ″    ″      H    OCH3      CH3         CH55    ″    ″    ″      H    CH3        CH3         CH56    ″    ″    ″      H    CH3       OC2H5      CH57    ″    ″    ″      H    OCH3      OCH3        N58    ″    ″    ″      H    OCH3      CH3         N59    ″    ″    ″      H    OCH3      Cl           CH60    ″    ″    ″      H    OCF2H     CH3         CH Vb.   R1   R4   R5   R7   X         Y          Z    Fp.℃61    ″    ″    ″    H    OCF2H    OCF2H      CH62    ″    ″    ″    H    OCH3     Br          CH63    ″    ″    ″    H    OCH3     OC2H5     CH64    ″    ″    ″    H    OCH3     SCH3       CH65    ″    ″    ″    H    OCH3     OC2H5     N66    ″    ″    ″    H    OCH3     OC3H7     CH67    ″    ″    ″    H    CH3      Cl          CH68    ″    ″    ″    H    Cl        OC2H5     CH69    ″    ″    ″    H    OC2H5   OC2H5     CH70    ″    ″    ″    H    C2H5    OCH3       CH71    ″    ″    ″    H    CF3      OCH3       CH72    ″    ″    ″    H    OCH2CF3 CH3        CH73    ″    ″    ″    H    OCH2CF3 OCH3       CH74    ″    ″    ″    H    OCH2CF3 OCH2CF3   CH75    ″    ″    ″    H    OCH2CF3 OCH3       N76    ″    ″    ″    H    OCH3     CH(OCH3)3 CH77    ″    ″    ″    CH3 OCH3     OCH3       CH78    ″    ″    ″    CH3 OCH3     CH3        N79    ″    CH3  COCH3H    OCH3     OCH3       CH 166-16880    ″    ″    ″    H    OCH3     CH3        CH81    ″    ″    ″    H    CH3      CH3        CH82    ″    ″    ″    H    CH3      OC2H5     CH83    ″    ″    ″    H    OCH3     OCH3       N84    ″    ″    ″    H    OCH3     CH3        N85    ″    ″    ″    H    OCH3     Cl          CH86    ″    ″    ″    H    OCF2H    CH3        CH87    ″    ″    ″    H    OCF2H    OCF2H      CH88    ″    ″    ″    H    OCH3     Br          CH89    ″    ″    ″    H    OCH3     OC2H5     CH90    ″    ″    ″    H    OCH3     SCH3       CH91    ″    ″    ″    H    OCH3     OC2H5     N92    ″    ″    ″    H    OCH3     OC3H7     CH93    ″    ″    ″    H    CH3      Cl          CH94    ″    ″    ″    H    Cl        OC2H5     CH95    ″    ″    ″    H    OC2H5   OC2H5     CH Vb.    R1   R4   R5      R7   X         Y          Z    Fp.℃96     ″    ″    ″       H    C2H5    OCH3       CH97     ″    ″    ″       H    CF3      OCH3       CH98     ″    ″    ″       H    OCH2CF3 CH3        CH99     ″    ″    ″       H    OCH2CF3 OCH3       CH100    ″    ″    ″       H    OCH2CF3 OCH2CF3   CH101    ″    ″    ″       H    OCH2CF3 OCH3       N102    ″    ″    ″       H    OCH3     CH(OCH3)2 CH103    ″    ″    ″       CH3 OCH3     OCH3       CH104    ″    ″    ″       CH3 OCH3     CH3        N105    ″    H     SO2CH3 H    OCH3     OCH3       CH106    ″    ″    ″       H    OCH3     CH3        CH107    ″    ″    ″       H    CH3      CH3        CH108    ″    ″    ″       H    OCH3     OCH3       N109    ″    ″    ″       H    OCH3     CH3        N110    ″    ″    ″       H    OC2H5   NHCH3      N111    ″    ″    ″       CH3 OCH3     OCH3       CH112    ″    ″    ″       CH3 OCH3     CH3        N113    ″    CH3  SO2CH3 H   OCH3     OCH3       CH114    ″    ″    ″       H    OCH3     CH3        CH115    ″    ″    ″       H    CH3      CH3        CH116    ″    ″    ″       H    OCH3     OCH3       N117    ″    ″    ″       H    OCH3     CH3        N118    ″    ″    ″       H    OC2H5   NHCH3      N119    ″    ″    ″       CH3 OCH3     OCH3       CH120    ″    ″    ″       CH3 OCH3     CH3        N121    ″    OH    CHO      H    OCH3     OCH3       CH122    ″    ″    ″       H    OCH3     CH3        CH123    ″    ″    ″       H    CH3      CH3        CH124    ″    ″    ″       H    OCH3     OCH3       N125    ″    ″    ″       H    OCH3     CH3        N126    ″    ″    ″       H    OC2H5   NHCH3      N127    ″    ″    ″       CH3 OCH3     OCH3       CH128    ″    ″    ″       CH3 OCH3     CH3        N129    ″    OCH3 CHO      H    OCH3     OCH3       CH130    ″    ″    ″       H    OCH3     CH3        CH Vb.    R1   R4   R5          R7   X        Y     Z    Fp.℃131    ″    ″    ″           H    CH3    CH3   CH132    ″    ″    ″           H    OCH3   OCH3  N133    ″    ″    ″           H    OCH3   CH3   N134    ″    ″    ″           H    OC2H5 NHCH3 N135    ″    ″    ″           CH3 OCH3   OCH3  CH136    ″    ″    ″           CH3 OCH3   CH3   N137    ″    OH    COCH3       H    OCH3   OCH3  CH138    ″    ″    ″           H    OCH3   CH3   CH139    ″    ″    ″           H    CH3    CH3   CH140    ″    ″    ″           H    OCH3   OCH3  N141    ″    ″    ″           H    OCH3   CH3   N142    ″    ″    ″           H    OC2H5 NHCH3 N143    ″    ″    ″           CH3 OCH3   OCH3  CH144    ″    ″    ″           CH3 OCH3   CH3   N145    ″    OCH3 COCH3       H    OCH3   OCH3  CH146    ″    ″    ″           H    OCH3   CH3   CH147    ″    ″    ″           H    CH3    CH3   CH148    ″    ″    ″           H    OCH3   OCH3  N149    ″    ″    ″           H    OCH3   CH3   N150    ″    ″    ″           H    OC2H5 NHCH3 N151    ″    ″    ″           CH3 OCH3   OCH3  CH152    ″    ″    ″           CH3 OCH3   CH3   N153    ″    H     COC2H5     H    OCH3   OCH3  CH 196154    ″    ″    ″           H    OCH3   CH3   CH155    ″    ″    ″           H    OCH3   OCH3  N156    ″    ″    ″           H    OCH3   CH3   N157    ″    CH3  ″           H    OCH3   OCH3  CH158    ″    ″    ″           H    OCH3   CH3   CH159    ″    ″    ″           H    OCH3   OCH3  N160    ″    ″    ″           H    OCH3   CH3   N161    ″    H     COCH2OCH3  H    OCH3   OCH3  CH 192-195162    ″    ″    ″           H    OCH3   CH3   CH163    ″    ″    ″           H    OCH3   OCH3  N164    ″    ″    ″           H    OCH3   CH3   N165    ″    CH3  ″           H    OCH3   OCH3  CH Vb.    R1   R4   R5           R7   X      Y      Z   Fp.℃166    ″    ″    ″            H    OCH3   CH3   CH167    ″    ″    ″            H    OCH3   OCH3  N168    ″    ″    ″            H    OCH3   CH3   N169    ″    H     COCO2C2H5 H    OCH3   OCH3  CH 183-185170    ″    ″    ″            H    OCH3   CH3   CH171    ″    ″    ″            H    OCH3   OCH3  N172    ″    ″    ″            H    OCH3   CH3   N173    ″    CH3   ″           H    OCH3   OCH3  CH174    ″    ″    ″            H    OCH3   CH3   CH175    ″    ″    ″            H    OCH3   OCH3  N176    ″    ″    ″            H    OCH3   CH3   N177    ″    H     COCF3        H    OCH3   OCH3  CH 180-182178    ″    ″    ″            H    OCH3   CH3   CH179    ″    ″    ″            H    OCH3   OCH3  N180    ″    ″    ″            H    OCH3   CH3   N181    ″    CH3  ″            H    OCH3   OCH3  CH 144-147182    ″    ″    ″            H    OCH3   CH3   CH183    ″    ″    ″            H    OCH3   OCH3  N184    ″    ″    ″            H    OCH3   CH3   N185    ″    H     COOCH3       H    OCH3   OCH3  CH 178-180186    ″    ″    ″            H    OCH3   CH3   CH187    ″    ″    ″            H    OCH3   OCH3  N188    ″    ″    ″            H    OCH3   CH3   N189    ″    CH3  ″            H    OCH3   OCH3  CH190    ″    ″    ″            H    OCH3   CH3   CH191    ″    ″    ″            H    OCH3   OCH3  N192    ″    ″    ″            H    OCH3   CH3   N193    ″    H     CONHC2H5    H    OCH3   OCH3  CH194    ″    ″    ″            H    OCH3   CH3   CH195    ″    ″    ″            H    OCH3   OCH3  N196    ″    ″    ″            H    OCH3   CH3   N197    ″    CH3  ″           H    OCH3   OCH3  CH198    ″    ″    ″            H    OCH3   CH3   CH199    ″    ″    ″            H    OCH3   OCH3  N200    ″    ″    ″            H    OCH3   CH3   N Vb.    R1    R4       R5           R7   X       Y      Z    Fp.℃201    ″     H        CSNHC2H5     H    OCH3   OCH3  CH202    ″     ″       ″             H    OCH3   CH3   CH203    ″     ″       ″             H    OCH3   OCH3  N204    ″     ″       ″             H    OCH3   CH3   N205    ″     CH3     ″             H    OCH3   OCH3  CH206    ″     ″       ″             H    OCH3   CH3   CH207    ″     ″       ″             H    OCH3   OCH3  N208    ″     ″       ″             H    OCH3   CH3   N209    ″     H        SO2NHCH3    H    OCH3   OCH3  CH210    ″     ″       ″             H    OCH3   CH3   CH211    ″     ″       ″             H    OCH3   OCH3  N212    ″     ″       ″             H    OCH3    CH3   N213    ″     CH3     ″             H    OCH3   OCH3  CH214    ″     ″       ″             H    OCH3   CH3   CH215    ″     ″       ″             H    OCH3   OCH3  N216    ″     ″       ″             H    OCH3   CH3   N217    ″     H        SO2N(CH3)2 H    OCH3   OCH3  CH218    ″     ″       ″             H    OCH3   CH3   CH219    ″     ″       ″             H    OCH3   OCH3  N220    ″     ″       ″             H    OCH3   CH3   N221    ″     CH3     ″             H    OCH3   OCH3  CH222    ″     ″       ″             H    OCH3   CH3   CH223    ″     ″       ″             H    OCH3   OCH3  N224    ″     ″       ″             H    OCH3   CH3   N225    ″    -CH2CH2CH2CO-        H    OCH3   OCH3  CH226    ″          ″                 H    OCH3   CH3   CH227    ″          ″                 H    OCH3   OCH3  N228    ″          ″                 H    OCH3   CH3   N229    ″    -CH2CH2CH2SO2-      H    OCH3   OCH3  CH230    ″          ″                 H    OCH3   CH3   CH231    ″          ″                 H    OCH3   OCH3  N232    ″          ″                 H    OCH3   CH3   N233    ″    -CH2CH2CH2CH2CO-    H    OCH3   OCH3  CH234    ″          ″                 H    OCH3   CH3   CH235    ″          ″                 H    OCH3   OCH3  N Vb.    R1   R4       R5           R7   X      Y      Z    Fp.℃236    ″         ″                 H    OCH3   CH3   N237    ″    -CH2CH2CH2CH2SO2- H    OCH3   OCH3  CH238    ″         ″                 H    OCH3   CH3   CH239    ″         ″                 H    OCH3   OCH3  N240    ″         ″                 H    OCH3   CH3   N241    ″    -CH2CH2OCH2CH2-    H    OCH3   OCH3  CH242    ″         ″                 H    OCH3   CH3   CH243    ″         ″                 H    OCH3   OCH3  N244    ″         ″                 H    OCH3   CH3   N245    ″    H        COC3H7      H    OCH3   OCH3  CH246    ″    ″       ″             H    OCH3   CH3   CH247    ″    ″       ″             H    OCH3   OCH3  N248    ″    ″       ″             H    OCH3   CH3   N249    ″    CH3     ″             H    OCH3   OCH3  CH250    ″    ″       ″             H    OCH3   CH3   CH251    ″    ″       ″             H    OCH3   OCH3  N252    ″    ″       ″             H    OCH3   CH3   N253    ″    H        COCH2Cl       H    OCH3   OCH3  CH 170-172254    ″    ″       ″             H    OCH3   CH3   CH255    ″    ″       ″             H    OCH3   OCH3  N256    ″    ″       ″             H    OCH3   CH3   N257    ″    CH3     ″             H    OCH3   OCH3  CH258    ″    ″       ″             H    OCH3   CH3   CH259    ″    ″       ″             H    OCH3   OCH3  N260    ″    ″       ″             H    OCH3   CH3   N261    ″    H        COCHCl2       H    OCH3   OCH3  CH 158-160262    ″    ″       ″             H    OCH3   CH3   CH263    ″    ″       ″             H    OCH3   OCH3  N264    ″    ″       ″             H    OCH3   CH3   N265    ″    CH3     ″             H    OCH3   OCH3  CH266    ″    ″       ″             H    OCH3   CH3   CH267    ″    ″       ″             H    OCH3   OCH3  N268    ″    ″       ″             H    OCH3   CH3   N269    ″    H        COCCl3        H    OCH3   OCH3  CH 194-196270    ″    ″       ″             H    OCH3   CH3   CH Vb.    R1   R4       R5          R7   X        Y     Z    Fp.℃271    ″    ″        ″           H    OCH3   OCH3   N272    ″    ″        ″           H    OCH3   CH3    N273    ″    CH3      ″           H    OCH3   OCH3   CH274    ″    ″        ″           H    OCH3   CH3    CH275    ″    ″        ″           H    OCH3   OCH3   N276    ″    ″        ″           H    OCH3   CH3    N277    ″    H         COCH＝CH2   H    OCH3   OCH3   CH278    ″    ″        ″           H    OCH3   CH3    CH279    ″    ″        ″           H    OCH3   OCH3   N280    ″    ″        ″           H    OCH3   CH3    N281    ″    CH3      ″           H    OCH3   OCH3   CH282    ″    ″        ″           H    OCH3   CH3    CH283    ″    ″        ″           H    OCH3   OCH3   N284    ″    ″        ″           H    OCH3   CH3    N285    ″    H         COC＝CH      H    OCH3   OCH3   CH286    ″    ″        ″           H    OCH3   CH3    CH287    ″    ″        ″           H    OCH3   OCH3   N288    ″    ″        ″           H    OCH3   CH3    N289    ″    CH3      ″           H    OCH3   OCH3   CH290    ″    ″        ″           H    OCH3   CH3    CH291    ″    ″        ″           H    OCH3   OCH3   N292    ″    ″        ″           H    OCH3   CH3    N293    ″    H         COC6H5    H    OCH3   OCH3   CH294    ″    ″        ″           H    OCH3   CH3    CH295    ″    ″        ″           H    OCH3   OCH3   N296    ″    ″        ″           H    OCH3   CH3    N297    ″    CH3      ″           H    OCH3   OCH3   CH298    ″    ″        ″           H    OCH3   CH3    CH299    ″    ″        ″           H    OCH3   OCH3   N300    ″    ″        ″           H    OCH3   CH3    N301    ″    SO2C6H5SO2C6H5 H    OCH3   OCH3   CH302    ″    ″        ″           H    OCH3   CH3    CH303    ″    ″        ″           H    OCH3   OCH3   N304    ″    ″        ″           H    OCH3   CH3    N305    ″    SO2CH3  SO2CH3    H    OCH3   OCH3   CH Vb.    R1   R4   R5           R7   X       Y      Z    Fp.℃306    ″    ″    ″            H    OCH3   CH3    CH307    ″    ″    ″            H    OCH3   OCH3   N308    ″    ″    ″            H    OCH3   CH3    N309    ″    H     COCH2Br      H    OCH3   OCH3   CH310    ″    ″    ″            H    OCH3   CH3    N311    ″    CH3  ″            H    OCH3   OCH3   CH312    ″    ″    ″            H    OCH3   CH3    N313    ″    H     COCH2F       H    OCH3   OCH3   CH314    ″    ″    ″            H    OCH3   CH3    N315    ″    CH3  ″            H    OCH3   OCH3   CH316    ″    ″    ″            H    OCH3   CH3    N317    ″    H     COCH2C＝CH   H    OCH3   OCH3   CH318    ″    ″    ″            H    OCH3   CH3    N319    ″    CH3  ″            H    OCH3   OCH3   CH320    ″    ″    ″            H    OCH3   CH3    N321    ″    H     COCO2CH3   H    OCH3   OCH3   CH322    ″    ″    ″            H    OCH3   CH3    N323    ″    CH3  ″            H    OCH3   OCH3   CH324    ″    ″    ″            H    OCH3   CH3    N325    ″    H     CO2C2H5   H    OCH3   OCH3   CH326    ″    ″    ″            H    OCH3   CH3    N327    ″    CH3  ″            H    OCH3   OCH3   CH328    ″    ″    ″            H    OCH3   CH3    N329    ″    H     COSCH3       H    OCH3   OCH3   CH330    ″    ″    ″            H    OCH3   CH3    N331    ″    CH3  ″            H    OCH3   OCH3   CH332    ″    ″    ″            H    OCH3   CH3    N333    ″    H     CSOCH3       H    OCH3   OCH3   CH334    ″    ″    ″            H    OCH3   CH3    N335    ″    CH3  ″            H    OCH3   OCH3   CH336    ″    ″    ″            H    OCH3   CH3    N337    ″    H     CSSCH3       H    OCH3   OCH3   CH338    ″    ″    ″            H    OCH3   CH3    N339    ″    CH3  ″            H    OCH3   OCH3   CH340    ″    ″    ″            H    OCH3   CH3    N Vb.     R1   R4     R5           R7  X      Y      Z   Fp.℃341     ″    H     COCH(CH3)2    H   OCH3   OCH3  CH 195-196342     ″    ″    ″              H   OCH3   CH3   N343     ″    CH3  ″              H   OCH3   OCH3  CH344     ″    ″    ″              H   OCH3   CH3   N345     ″    H     COC(CH3)3    H   OCH3   OCH3  CH346     ″    ″    ″              H   OCH3   CH3   N347     ″    CH3  ″              H   OCH3   OCH3  CH348     ″    ″    ″              H   OCH3   CH3   N349     ″    H     CO-环丙基       H   OCH3   OCH3  CH 202-203350     ″    ″    ″              H   OCH3   CH3   N351     ″    CH3  ″              H   OCH3   OCH3  CH352     ″    ″    ″              H   OCH3   CH3   N353     ″    H     CO-环丁基       H   OCH3   OCH3  CH354     ″    ″    ″              H   OCH3   CH3   N355     ″    CH3  ″              H   OCH3   OCH3  CH356     ″    ″    ″              H   OCH3   CH3   N357     ″    H     CO-环戊基       H   OCH3   OCH3  CH358     ″    ″    ″              H   OCH3   CH3   N359     ″    CH3  ″              H   OCH3   OCH3  CH360     ″    ″    ″              H   OCH3   CH3   N361     ″    H     CO-环己基       H   OCH3   OCH3  CH362     ″    ″    ″              H   OCH3   CH3   N363     ″    CH3  ″              H   OCH3   OCH3  CH364     ″    ″    ″              H   OCH3   CH3   N365     ″    H     CONHCH2CH2Cl H   OCH3   OCH3  CH 178-182366     ″    ″    ″              H   OCH3   CH3   N367     ″    CH3  ″              H   OCH3   OCH3  CH368     ″    ″    ″              H   OCH3   CH3   N369     ″    H     CSNHCH2CH2Cl H   OCH3   OCH3  CH370     ″    ″    ″              H   OCH3   CH3   N371     ″    CH3  ″              H   OCH3   OCH3  CH372     ″    ″    ″              H   OCH3   CH3   N373     ″    H     CONH-n-C4H9  H   OCH3   OCH3  CH 183-184374     ″    ″    ″              H   OCH3   CH3   N375     ″    CH3  ″              H   OCH3   OCH3  CH Vb.    R1   R4       R5               R7   X       Y     Z    Fp.℃376    ″    ″        ″                H    OCH3   CH3   N377    ″    H         CSNHCH3          H    OCH3   OCH3  CH378    ″    ″        ″                H    OCH3   CH3   N379    ″    CH3      ″                H    OCH3   OCH3  CH380    ″    ″        ″                H    OCH3   CH3   N381    ″    H         CSNHCH2CH＝CH2 H    OCH3   OCH3  CH382    ″    ″        ″                H    OCH3   CH3   N383    ″    CH3      ″                H    OCH3   OCH3  CH384    ″    ″        ″                H    OCH3   CH3   N385    ″    CH3      CSNHCH2COCH3   H    OCH3   OCH3  CH386    ″    ″        ″                H    OCH3   CH3   N387    ″    CH3      CSNHCH2COC2H5 H    OCH3   OCH3  CH388    ″    ″        ″                H    OCH3   CH3   N389    ″    CH3      CONHCH2COCH3   H    OCH3   OCH3  CH390    ″    ″        ″                H    OCH3   CH3   N391    ″    CH3      CONHCH2COC2H5 H    OCH3   OCH3  CH392    ″    ″        ″                H    OCH3   CH3   N393    ″    -CONHCH2CO-                H    OCH3   OCH3  CH394    ″    ″        ″                H    OCH3   CH3   N395    ″    H         SO2CH2F        H    OCH3   OCH3  CH396    ″    ″        ″                H    OCH3   CH3   N397    ″    CH3      ″                H    OCH3   OCH3  CH398    ″    ″        ″                H    OCH3   CH3   N399    ″    H         SO2CF3         H    OCH3   OCH3  CH400    ″    ″        ″                H    OCH3   CH3   N401    ″    CH3      ″                H    OCH3   OCH3  CH402    ″    ″        ″                H    OCH3   CH3   N403    ″    H         SO2C2H5       H    OCH3   OCH3  CH404    ″    ″        ″                H    OCH3   CH3   N405    ″    CH3      ″                H    OCH3   OCH3  CH406    ″    ″        ″                H    OCH3   CH3   N407    ″    H         SO2-n-C3H7    H    OCH3   OCH3  CH408    ″    ″        ″                H    OCH3   CH3   N409    ″    CH3      ″                H    OCH3   OCH3  CH410    ″    ″        ″                H    OCH3   CH3   N Vb     R1   R4   R5          R7  X       Y     Z  Fp.℃411    ″    OH    COC2H5     H   OCH3   OCH3  CH412    ″    ″    ″           H   OCH3   CH3   N413    ″    OCH3 ″           H   OCH3   OCH3  CH414    ″    ″    ″           H   OCH3   CH3   N415    ″    OH    COCH2Cl     H   OCH3   OCH3  CH416    ″    ″    ″           H   OCH3   CH3   N417    ″    OCH3 ″           H   OCH3   OCH3  CH418    ″    ″    ″           H   OCH3   CH3   N419    ″    OH    COCF3       H   OCH3   OCH3  CH420    ″    ″    ″           H   OCH3   CH3   N421    ″    OCH3 ″           H   OCH3   OCH3  CH422    ″    ″    ″           H   OCH3   CH3   N423    ″    OH    COCH2OCH3 H   OCH3   OCH3  CH424    ″    ″    ″           H   OCH3   CH3   N425    ″    OCH3 ″           H   OCH3   OCH3  CH426    ″    ″    ″           H   OCH3   CH3   N427    ″    OH    COCO2C2H5H   OCH3   OCH3  CH428    ″    ″    ″           H   OCH3   CH3   N429    ″    OCH3 ″           H   OCH3   OCH3  CH430    ″    ″    ″           H   OCH3   CH3   N431    ″    OH    COOCH3      H   OCH3   OCH3  CH432    ″    ″    ″           H   OCH3   CH3   N433    ″    OCH3 ″           H   OCH3   OCH3  CH434    ″    ″    ″           H   OCH3   CH3   N435    ″    OH    环丙基       H   OCH3   OCH3  CH436    ″    ″    ″           H   OCH3   CH3   N437    ″    OCH3 ″           H   OCH3   OCH3  CH438    ″    ″    ″           H   OCH3   CH3   N439    ″    OH    COC6H5    H   OCH3   OCH3  CH440    ″    ″    ″           H   OCH3   CH3   N441    ″    OCH3 ″           H   OCH3   OCH3  CH442    ″    ″    ″           H   OCH3   CH3   N443    ″    OH    COCH(CH3)2H   OCH3   OCH3  CH444    ″    ″    ″           H   OCH3   CH3   N445    ″    OCH3 ″           H   OCH3   OCH3  CH Vb     R1   R4   R5          R7   X       Y     Z    Fp.℃446    ″    ″    ″           H    OCH3   CH3   N447    ″    OH    COCH＝CH2   H    OCH3   OCH3  CH448    ″    ″    ″           H    OCH3   CH3   N449    ″    OCH3 ″           H    OCH3   OCH3  CH450    ″    ″    ″           H    OCH3   CH3   N451    ″    OH    COC＝CH      H    OCH3   OCH3  CH452    ″    ″    ″           H    OCH3   CH3   N453    ″    OCH3 ″           H    OCH3   OCH3  CH454    ″    ″    ″           H    OCH3   CH3   N455    ″    OH    SO2CH3    H    OCH3   OCH3  CH456    ″    ″    ″           H    OCH3   CH3   N457    ″    OCH3 ″           H    OCH3   OCH3  CH458    ″    ″    ″           H    OCH3   CH3   N459    ″    OH    SO2NHCH3  H    OCH3   OCH3  CH460    ″    ″    ″           H    OCH3   CH3   N461    ″    OCH3 ″           H    OCH3   OCH3  CH462    ″    ″    ″           H    OCH3   CH3   N463    ″    OH    SO2N(CH3)2H   OCH3   OCH3  CH464    ″    ″    ″           H    OCH3   CH3   N465    ″    OCH3 ″           H    OCH3   OCH3  CH466    ″    ″    ″           H    OCH3   CH3   N467    ″    C2H5CHO         H    OCH3   OCH3  CH468    ″    ″    ″           H    OCH3   CH3   N469    ″    ″    COCH3       H    OCH3   OCH3  CH470    ″    ″    ″           H    OCH3   CH3   N471    ″    ″    环丙基       H    OCH3   OCH3  CH472    ″    ″    ″           H    OCH3   CH3   N473    ″    ″    COCH2Cl     H    OCH3   OCH3  CH474    ″    ″    ″           H    OCH3   CH3   N475    ″    ″    COCF3       H    OCH3   OCH3  CH476    ″    ″    ″           H    OCH3   CH3   N477    ″    ″    COOCH3      H    OCH3   OCH3  CH478    ″    ″    ″           H    OCH3   CH3   N479    ″    ″    COC6H5    H    OCH3   OCH3  CH480    ″    ″    ″           H    OCH3   CH3   N Vb.    R1        R4   R5            R7   X       Y     Z    Fp.℃481    ″         ″    CONHC2H5    H    OCH3   OCH3  CH482    ″         ″    ″             H    OCH3   CH3   N483    ″         ″    CSNHC2H5    H    OCH3   OCH3  CH484    ″         ″    ″             H    OCH3   CH3   N485    ″         ″    SO2CH3      H    OCH3   OCH3  CH486    ″         ″    ″             H    OCH3   CH3   N487    ″         ″    SO2NHCH3    H    OCH3   OCH3  CH488    ″         ″    ″             H    OCH3   CH3   N489    ″         ″    SO2N(CH3)2 H    OCH3   OCH3  CH490    ″         ″    ″             H    OCH3   CH3   N491    ″         ″    SO2C6H5    H    OCH3   OCH3  CH492    ″         ″    ″             H    OCH3   CH3   N493    CO2C2H5 H     CHO           H    OCH3   OCH3  CH494    ″         ″    ″             H    OCH3   CH3   N495    ″         ″    COCH3         H    OCH3   OCH3  CH496    ″         ″    ″             H    OCH3   CH3   N497    ″         ″    SO2CH3      H    OCH3   OCH3  CH498    ″         ″    ″             H    OCH3   CH3   N499    ″         CH3  CHO            H    OCH3   OCH3  CH500    ″         ″    ″             H    OCH3   CH3   N501    ″         ″    COCH3         H    OCH3   OCH3  CH502    ″         ″    ″             H    OCH3   CH3   N503    ″         ″    SO2CH3      H    OCH3   OCH3  CH504    ″         ″    ″             H    OCH3   CH3   N505    ″         C2H5CHO           H    OCH3   OCH3  CH506    ″         ″    ″             H    OCH3   CH3   N507    ″         ″    COCH3        H    OCH3   OCH3  CH508    ″         ″    ″             H    OCH3   CH3   N509    ″         ″    SO2CH3       H    OCH3   OCH3  CH510    ″         ″    ″             H    OCH3   CH3   N511    ″         OH    CHO            H    OCH3   OCH3  CH512    ″         ″    ″             H    OCH3   CH3   N513    ″         ″    COCH3         H    OCH3   OCH3  CH514    ″         ″    ″             H    OCH3   CH3   N515    ″         ″    SO2CH3       H    OCH3   OCH3  CH Vb.    R1         R4    R5      R7   X        Y      Z    Fp.℃516    ″        ″    ″         H    OCH3     CH3   N517    ″        OCH3 CHO        H    OCH3     OCH3  CH518    ″        ″    ″         H    OCH3     CH3   N519    ″        ″    COCH3     H    OCH3     OCH3  CH520    ″        ″    ″         H    OCH3     CH3   N521    CO2-n-Bu H     CHO        H    ″        OMe    CH522    CONMe2   Me    ″         H    ″        Me     N523    CONHMe    H     ″         H    ″        OMe    CH524    COSMe     Me    CO-Me      H    ″        Me     N525    CO2Me    n-Bu  CHO        H    ″        OMe    CH526    ″        n-Bu  ″         H    ″        Me     N527    ″        H     ″         H    OCH2CF3NMe2  ″528    ″        Me    ″         H    ″        ″     ″529    ″        H     CO-Me      H    ″        ″     ″530    ″        Me    ″         H    ″        ″     ″531    ″        ″    SO2CH3   H    OCH3     OCH3  CH532    ″        ″    ″         H    OCH3     CH3   N533    ″ H    OCH3     OCH3  CH534    ″              ″         H    OCH3     CH3   N
表3
Figure A9419413700751
Vb    R1     R4   R5   R7   X        Y          Z    Fp.℃1    CO2CH3 H    CHO    H    OCH3     OCH3     CH2    ″       ″    ″    H    OCH3     CH3      CH3    ″       ″    ″    H    CH3      CH3      CH4    ″       ″    ″    H    CH3      OC2H5   CH5    ″       ″    ″    H    OCH3     OCH3     N6    ″       ″    ″    H    OCH3     CH3      N7    ″       ″    ″    H    OCH3     Cl        CH8    ″       ″    ″    H    OCF2H    CH3      CH9    ″       ″    ″    H    OCF2H    OCF2H    CH10   ″       ″    ″    H    OCH3     Br        CH11   ″       ″    ″    H    OCH3     OC2H5   CH12   ″       ″    ″    H    OCH3     SCH3     CH13   ″       ″    ″    H    OCH3     OC2H5    N14   ″       ″    ″    H    OCH3     OC3H7    CH15   ″       ″    ″    H    CH3      Cl         CH16   ″       ″    ″    H    Cl        OC2H5    CH17   ″       ″    ″    H    OC2H5   OC2H5    CH18   ″       ″    ″    H    C2H5    OCH3      CH19   ″       ″    ″    H    CF3      OCH3      CH20   ″       ″    ″    H    OCH2CF3 CH3       CH21   ″       ″    ″    H    OCH2CF3 OCH3      CH22   ″       ″    ″    H    OCH2CF3 OCH2CF3  CH23   ″       ″    ″    H    OCH2CF3 OCH3      N24   ″       ″    ″    H    OCH3     CH(OCH3)2CH Vb.   R1   R4   R5   R7   X         Y          Z    Fp.℃25    ″    ″    ″    CH3 OCH3     OCH3       CH26    ″    ″    ″    CH3 OCH3     CH3        N27    ″    H     COCH3H    OCH3     OCH3       CH  198-20028    ″    ″    ″    H    OCH3     CH3        CH29    ″    ″    ″    H    CH3      CH3        CH30    ″    ″    ″    H    CH3      OC2H5     CH31    ″    ″    ″    H    OCH3     OCH3       N32    ″    ″    ″    H    OCH3     CH3        N33    ″    ″    ″    H    OCH3     Cl          CH34    ″    ″    ″    H    OCF2H    CH3        CH35    ″    ″    ″    H    OCF2H    OCF2H      CH36    ″    ″    ″    H    OCH3     Br          CH37    ″    ″    ″    H    OCH3     OC2H5     CH38    ″    ″    ″    H    OCH3     SCH3       CH39    ″    ″    ″    H    OCH3     OC2H5     N40    ″    ″    ″    H    OCH3     OC3H7     CH41    ″    ″    ″    H    CH3      Cl          CH42    ″    ″    ″    H    Cl        OC2H5     CH43    ″    ″    ″    H    OC2H5   OC2H5     CH44    ″    ″    ″    H    C2H5    OCH3       CH45    ″    ″    ″    H    CF3      OCH3       CH46    ″    ″    ″    H    OCH2CF3 CH3        CH47    ″    ″    ″    H    OCH2CF3 OCH3       CH48    ″    ″    ″    H    OCH2CF3 OCH2CF3   CH49    ″    ″    ″    H    OCH2CF3 OCH3       N50    ″    ″    ″    H    OCH3     CH(OCH3)2 CH51    ″    ″    ″    CH3 OCH3     OCH3       CH52    ″    ″    ″    CH3 OCH3     CH3        N53    ″    CH3  CHO   H    OCH3     OCH3       CH54    ″    ″    ″    H    OCH3     CH3        CH55    ″    ″    ″    H    CH3      CH3        CH56    ″    ″    ″    H    CH3      OC2H5     CH57    ″    ″    ″    H    OCH3     OCH3       N58    ″    ″    ″    H    OCH3     CH3        N59    ″    ″    ″    H    OCH3     Cl          CH Vb.   R1   R4   R5   R7   X         Y          Z    Fp.℃60    ″    ″    ″    H    OCF2H    CH3        CH61    ″    ″    ″    H    OCF2H    OCF2H      CH62    ″    ″    ″    H    OCH3     Br          CH63    ″    ″    ″    H    OCH3     OC2H5     CH64    ″    ″    ″    H    OCH3     SCH3       CH65    ″    ″    ″    H    OCH3     OC2H5     N66    ″    ″    ″    H    OCH3     OC3H7     CH67    ″    ″    ″    H    CH3      Cl          CH68    ″    ″    ″    H    Cl        OC2H5     CH69    ″    ″    ″    H    OC2H5   OC2H5     CH70    ″    ″    ″    H    C2H5    OCH3       CH71    ″    ″    ″    H    CF3      OCH3       CH72    ″    ″    ″    H    OCH2CF3 CH3        CH73    ″    ″    ″    H    OCH2CF3 OCH3       CH74    ″    ″    ″    H    OCH2CF3 OCH2CF3   CH75    ″    ″    ″    H    OCH2CF3 OCH3       N76    ″    ″    ″    H    OCH3     CH(OCH3)2 CH77    ″    ″    ″    CH3 OCH3     OCH3       CH78    ″    ″    ″    CH3 OCH3     CH3        N79    ″    CH3  COCH3H    OCH3     OCH3       CH80    ″    ″    ″    H    OCH3     CH3        CH81    ″    ″    ″    H    CH3      CH3        CH82    ″    ″    ″    H    CH3      OC2H5     CH83    ″    ″    ″    H    OCH3     OCH3       N84    ″    ″    ″    H    OCH3     CH3        N85    ″    ″    ″    H    OCH3     Cl          CH86    ″    ″    ″    H    OCF2H    CH3        CH87    ″    ″    ″    H    OCF2H    OCF2H      CH88    ″    ″    ″    H    OCH3     Br          CH89    ″    ″    ″    H    OCH3     OC2H5     CH90    ″    ″    ″    H    OCH3     SCH3       CH91    ″    ″    ″    H    OCH3     OC2H5     N92    ″    ″    ″    H    OCH3     OC3H7     CH93    ″    ″    ″    H    CH3      Cl          CH94    ″    ″    ″    H    Cl        OC2H5     CH Vb     R1   R4   R5     R7     X          Y       Z    Fp.℃95     ″    ″    ″      H    OC2H5   OC2H5     CH96     ″    ″    ″      H    C2H5    OCH3       CH97     ″    ″    ″      H    CF3      OCH3       CH98     ″    ″    ″      H    OCH2CF3 CH3        CH99     ″    ″    ″      H    OCH2CF3 OCH3       CH100    ″    ″    ″      H    OCH2CF3 OCH2CF3   CH101    ″    ″    ″      H    OCH2CF3 OCH3       N102    ″    ″    ″      H    OCH3     CH(OCH3)2 CH103    ″    ″    ″      CH3 OCH3     OCH3       CH104    ″    ″    ″      CH3 OCH3     CH3        N105    ″    H    SO2CH3 H    OCH3     OCH3       CH106    ″    ″    ″      H    OCH3     CH3        CH107    ″    ″    ″      H    CH3      CH3        CH108    ″    ″    ″      H    OCH3     OCH3       N109    ″    ″    ″      H    OCH3     CH3        N110    ″    ″    ″      H    OC2H5   NHCH3      N111    ″    ″    ″      CH3 OCH3     OCH3       CH112    ″    ″    ″      CH3 OCH3     CH3        N113    ″    CH3  SO2CH3H    OCH3     OCH3       CH114    ″    ″    ″      H    OCH3     CH3        CH115    ″    ″    ″      H    CH3      CH3        CH116    ″    ″    ″      H    OCH3     OCH3       N117    ″    ″    ″      H    OCH3     CH3        N118    ″    ″    ″      H    OC2H5   NHCH3      N119    ″    ″    ″      CH3 OCH3     OCH3       CH120    ″    ″    ″      CH3 OCH3     CH3        N121    ″    OH    CHO     H    OCH3     OCH3       CH122    ″    ″    ″      H    OCH3     CH3        CH123    ″    ″    ″      H    CH3      CH3        CH124    ″    ″    ″      H    OCH3     OCH3       N125    ″    ″    ″      H    OCH3     CH3        N126    ″    ″    ″      H    OC2H5   NHCH3      N127    ″    ″    ″      CH3 OCH3     OCH3       CH128    ″    ″    ″      CH3 OCH3     CH3        N129    ″    OCH3 CHO     H    OCH3     OCH3       CH Vb.    R1   R4   R5        R7   X       Y     Z    Fp.℃130    ″    ″    ″         H    OCH3   CH3   CH131    ″    ″    ″         H    CH3    CH3   CH132    ″    ″    ″         H    OCH3   OCH3  N133    ″    ″    ″         H    OCH3   CH3   N134    ″    ″    ″         H    OC2H5 NHCH3 N135    ″    ″    ″         CH3 OCH3   OCH3  CH136    ″    ″    ″         CH3 OCH3   CH3   N137    ″    OH    COCH3     H    OCH3   OCH3  CH138    ″    ″    ″         H    OCH3   CH3   CH139    ″    ″    ″         H    CH3    CH3   CH140    ″    ″    ″         H    OCH3   OCH3  N141    ″    ″    ″         H    OCH3   CH3   N142    ″    ″    ″         H    OC2H5 NHCH3 N143    ″    ″    ″         CH3 OCH3   OCH3  CH144    ″    ″    ″         CH3 OCH3   CH3   N145    ″    OCH3 COCH3     H    OCH3   OCH3  CH146    ″    ″    ″         H    OCH3   CH3   CH147    ″    ″    ″         H    CH3    CH3   CH148    ″    ″    ″         H    OCH3   OCH3  N149    ″    ″    ″         H    OCH3   CH3   N150    ″    ″    ″         H    OC2H5 NHCH3 N151    ″    ″    ″         CH3 OCH3   OCH3  CH152    ″    ″    ″         CH3 OCH3   CH3   N153    ″    H     COC2H5   H    OCH3   OCH3  CH154    ″    ″    ″         H    OCH3   CH3   CH155    ″    ″    ″         H    OCH3   OCH3  N156    ″    ″    ″         H    OCH3   CH3   N157    ″    CH3  ″         H    OCH3   OCH3  CH158    ″    ″    ″         H    OCH3   CH3   CH159    ″    ″    ″         H    OCH3   OCH3  N160    ″    ″    ″         H    OCH3   CH3   N161    ″    H     COCH2OCH3H    OCH3   OCH3  CH162    ″    ″    ″         H    OCH3   CH3   CH163    ″    ″    ″         H    OCH3   OCH3  N164    ″    ″    ″         H    OCH3   CH3   N Vb.    R1   R4   R5         R7   X       Y     Z    Fp.℃165    ″    CH3  ″          H    OCH3   OCH3  CH166    ″    ″    ″          H    OCH3   CH3   CH167    ″    ″    ″          H    OCH3   OCH3  N168    ″    ″    ″          H    OCH3   CH3   N169    ″    H     COCO2C2H5H   OCH3   OCH3  CH170    ″    ″    ″          H    OCH3   CH3   CH171    ″    ″    ″          H    OCH3   OCH3  N172    ″    ″    ″          H    OCH3   CH3   N173    ″    CH3  ″          H    OCH3   OCH3  CH174    ″    ″    ″          H    OCH3   CH3   CH175    ″    ″    ″          H    OCH3   OCH3  N176    ″    ″    ″          H    OCH3   CH3   N177    ″    H     COCF3      H    OCH3   OCH3  CH178    ″    ″    ″          H    OCH3   CH3   CH179    ″    ″    ″          H    OCH3   OCH3  N180    ″    ″    ″          H    OCH3   CH3   N181    ″    CH3  ″          H    OCH3   OCH3  CH182    ″    ″    ″          H    OCH3   CH3   CH183    ″    ″    ″          H    OCH3   OCH3  N184    ″    ″    ″          H    OCH3   CH3   N185    ″    H     COOCH3     H    OCH3   OCH3  CH186    ″    ″    ″          H    OCH3   CH3   CH187    ″    ″    ″          H    OCH3   OCH3  N188    ″    ″    ″          H    OCH3   CH3   N189    ″    CH3  ″          H    OCH3   OCH3  CH190    ″    ″    ″          H    OCH3   CH3   CH191    ″    ″    ″          H    OCH3   OCH3  N192    ″    ″    ″          H    OCH3   CH3   N193    ″    H    CONHC2H5   H    OCH3   OCH3  CH194    ″    ″    ″          H    OCH3   CH3   CH195    ″    ″    ″          H    OCH3   OCH3  N196    ″    ″    ″          H    OCH3   CH3   N197    ″    CH3  ″          H    OCH3   OCH3  CH198    ″    ″    ″          H    OCH3   CH3   CH199    ″    ″    ″          H    OCH3   OCH3  N Vb.    R1   R4       R5          R7   X       Y     Z    Fp.℃200    ″    ″        ″           H    OCH3   CH3   N201    ″    H         CSNHC2H5  H    OCH3   OCH3  CH202    ″    ″        ″           H    OCH3   CH3   CH203    ″    ″        ″           H    OCH3   OCH3  N204    ″    ″        ″           H    OCH3   CH3   N205    ″    CH3      ″           H    OCH3   OCH3  CH206    ″    ″        ″           H    OCH3   CH3   CH207    ″    ″        ″           H    OCH3   OCH3  N208    ″    ″        ″           H    OCH3   CH3   N209    ″    H         SO2NHCH3  H    OCH3   OCH3  CH210    ″    ″        ″           H    OCH3   CH3   CH211    ″    ″        ″           H    OCH3   OCH3  N212    ″    ″        ″           H    OCH3   CH3   N213    ″    CH3      ″           H    OCH3   OCH3  CH214    ″    ″        ″           H    OCH3   CH3   CH215    ″    ″        ″           H    OCH3   OCH3  N216    ″    ″        ″           H    OCH3   CH3   N217    ″    H         SO2N(CH3)2H   OCH3   OCH3  CH218    ″    ″        ″           H    OCH3   CH3   CH219    ″    ″        ″           H    OCH3   OCH3  N220    ″    ″        ″           H    OCH3   CH3   N221    ″    CH3       ″           H    OCH3   OCH3  CH222    ″    ″        ″           H    OCH3   CH3   CH223    ″    ″        ″           H    OCH3   OCH3  N224    ″    ″        ″           H    OCH3   CH3   N225    ″   -CH2CH2CH2CO-       H    OCH3   OCH3  CH226    ″         ″                H    OCH3   CH3   CH227    ″         ″                H    OCH3   OCH3  N228    ″         ″                H    OCH3   CH3   N229    ″   -CH2CH2CH2SO2-     H    OCH3   OCH3  CH230    ″         ″                H    OCH3   CH3   CH231    ″         ″                H    OCH3   OCH3  N232    ″         ″                H    OCH3   CH3   N233    ″   -CH2CH2CH2CH2CO-   H    OCH3   OCH3  CH234    ″         ″                H    OCH3   CH3   CH Vb.    R1   R4        R5        R7    X       Y     Z    Fp.℃235    ″         ″               H    OCH3   OCH3  N236    ″         ″               H    OCH3   CH3   N237    ″    -CH2CH2CH2CH2SO2-H   OCH3   OCH3  CH238    ″         ″               H    OCH3   CH3   CH239    ″         ″               H    OCH3   OCH3  N240    ″         ″               H    OCH3   CH3   N241    ″    -CH2CH2OCH2CH2-  H    OCH3   OCH3  CH242    ″         ″               H    OCH3   CH3   CH243    ″         ″               H    OCH3   OCH3  N244    ″         ″               H    OCH3   CH3   N245    ″    H         COC3H7   H    OCH3   OCH3  CH246    ″    ″        ″          H    OCH3   CH3   CH247    ″    ″        ″          H    OCH3   OCH3  N248    ″    ″        ″          H    OCH3   CH3   N249    ″    CH3      ″          H    OCH3   OCH3  CH250    ″    ″        ″          H    OCH3   CH3   CH251    ″    ″        ″          H    OCH3   OCH3  N252    ″    ″        ″          H    OCH3   CH3   N253    ″    H         COCH2Cl    H    OCH3   OCH3  CH254    ″    ″        ″          H    OCH3   CH3   CH255    ″    ″        ″          H    OCH3   OCH3  N256    ″    ″        ″          H    OCH3   CH3   N257    ″    CH3      ″          H    OCH3   OCH3  CH258    ″    ″        ″          H    OCH3   CH3   CH259    ″    ″        ″          H    OCH3   OCH3  N260    ″    ″        ″          H    OCH3   CH3   N261    ″    H         COCHCl2    H    OCH3   OCH3  CH262    ″    ″        ″          H    OCH3   CH3   CH263    ″    ″        ″          H    OCH3   OCH3  N264    ″    ″        ″          H    OCH3   CH3   N265    ″    CH3      ″          H    OCH3   OCH3  CH266    ″    ″        ″          H    OCH3   CH3   CH267    ″    ″        ″          H    OCH3   OCH3  N268    ″    ″        ″          H    OCH3   CH3   N269    ″    H         COCCl3     H    OCH3   OCH3  CH Vb.    R1  R4        R5         R7   X       Y     Z    Fp.℃270    ″    ″         ″          H    OCH3   CH3   CH271    ″    ″         ″          H    OCH3   OCH3  N272    ″    ″         ″          H    OCH3   CH3   N273    ″    CH3       ″          H    OCH3   OCH3  CH274    ″    ″         ″          H    OCH3   CH3   CH275    ″    ″         ″          H    OCH3   OCH3  N276    ″    ″         ″          H    OCH3   CH3   N277    ″    H          COCH＝CH2  H    OCH3   OCH3  CH278    ″    ″         ″          H    OCH3   CH3   CH279    ″    ″         ″          H    OCH3   OCH3  N280    ″    ″         ″          H    OCH3   CH3   N281    ″    CH3       ″          H    OCH3   OCH3  CH282    ″    ″         ″          H    OCH3   CH3   CH283    ″    ″         ″          H    OCH3   OCH3  N284    ″    ″         ″          H    OCH3   CH3   N285    ″    H          COC＝CH     H    OCH3   OCH3  CH286    ″    ″         ″          H    OCH3   CH3   CH287    ″    ″         ″          H    OCH3   OCH3  N288    ″    ″         ″          H    OCH3   CH3   N289    ″    CH3       ″          H    OCH3   OCH3  CH290    ″    ″         ″          H    OCH3   CH3   CH291    ″    ″         ″          H    OCH3   OCH3  N292    ″    ″         ″          H    OCH3   CH3   N293    ″    H          COC6H5    H    OCH3   OCH3  CH294    ″    ″         ″          H    OCH3   CH3   CH295    ″    ″         ″          H    OCH3   OCH3  N296    ″    ″         ″          H    OCH3   CH3   N297    ″    CH3       ″          H    OCH3   OCH3  CH298    ″    ″         ″          H    OCH3   CH3   CH299    ″    ″         ″          H    OCH3   OCH3  N300    ″    ″         ″          H    OCH3   CH3   N301    ″    SO2C6H5 SO2C6H5H    OCH3   OCH3  CH302    ″    ″         ″          H    OCH3   CH3   CH303    ″    ″         ″          H    OCH3    OCH3  N304    ″    ″         ″          H    OCH3   CH3   N Vb.    R1     R4     R5        R7   X       Y     Z    Fp.℃305    ″    SO2CH3 SO2CH3   H    OCH3   OCH3  CH306    ″    ″       ″          H    OCH3   CH3   CH307    ″    ″       ″          H    OCH3   OCH3  N308    ″    ″       ″          H    OCH3   CH3   N309    ″    H        COCH2Br    H    OCH3   OCH3  CH310    ″    ″       ″          H    OCH3   CH3   N311    ″    CH3     ″          H    OCH3   OCH3  CH312    ″    ″       ″          H    OCH3   CH3   N313    ″    H        COCH2F     H    OCH3   OCH3  CH314    ″    ″       ″          H    OCH3   CH3   N315    ″    CH3     ″          H    OCH3   OCH3  CH316    ″    ″       ″          H    OCH3   CH3   N317    ″    H        COCH2C＝CH H    OCH3   OCH3  CH318    ″    ″       ″          H    OCH3   CH3   N319    ″    CH3     ″          H    OCH3   OCH3  CH320    ″    ″       ″          H    OCH3   CH3   N321    ″    H        COCO2CH3  H    OCH3   OCH3  CH322    ″    ″       ″          H    OCH3   CH3    N323    ″    CH3     ″          H    OCH3   OCH3  CH324    ″    ″       ″          H    OCH3   CH3   N325    ″    H        CO2C2H5 H    OCH3   OCH3  CH326    ″    ″       ″          H    OCH3   CH3    N327    ″    CH3     ″          H    OCH3   OCH3  CH328    ″    ″       ″          H    OCH3   CH3    N329    ″    H        COSCH3     H    OCH3   OCH3   CH330    ″    ″       ″          H    OCH3   CH3   N331    ″    CH3     ″          H    OCH3   OCH3   CH332    ″    ″       ″          H    OCH3   CH3   N333    ″    H        CSOCH3     H    OCH3   OCH3  CH334    ″    ″       ″          H    OCH3   CH3   N335    ″    CH3     ″          H    OCH3   OCH3   CH336    ″    ″       ″          H    OCH3   CH3   N337    ″    H        CSSCH3     H    OCH3   OCH3  CH338    ″    ″       ″          H    OCH3   CH3   N339    ″    CH3     ″          H    OCH3   OCH3  CH Vb.   R1   R4   R5            R7   X       Y     Z    Fp.℃340   ″    ″    ″             H    OCH3   CH3   N341   ″    H     COCH(CH3)2  H    OCH3   OCH3  CH342   ″    ″    ″             H    OCH3   CH3   N343   ″    CH3  ″             H    OCH3   OCH3  CH344   ″    ″    ″             H    OCH3   CH3   N345   ″    H     COC(CH3)3   H    OCH3   OCH3  CH346   ″    ″    ″             H    OCH3   CH3   N347   ″    CH3  ″             H    OCH3   OCH3  CH348   ″    ″    ″             H    OCH3   CH3   N349   ″    H     CO-环丙基      H    OCH3   OCH3  CH350   ″    ″    ″             H    OCH3   CH3   N351   ″    CH3  ″             H    OCH3   OCH3  CH352   ″    ″    ″             H    OCH3   CH3   N353   ″    H     CO-环丁基      H    OCH3   OCH3  CH354   ″    ″    ″             H    OCH3   CH3   N355   ″    CH3  ″             H    OCH3   OCH3  CH356   ″    ″    ″             H    OCH3   CH3   N357   ″    H     CO-环戊基      H    OCH3   OCH3  CH358   ″    ″    ″             H    OCH3   CH3   N359   ″    CH3  ″             H    OCH3   OCH3  CH360   ″    ″    ″             H    OCH3   CH3   N361   ″    H     CO-环己基      H    OCH3   OCH3  CH362   ″    ″    ″             H    OCH3   CH3   N363   ″    CH3  ″             H    OCH3   OCH3  CH364   ″    ″    ″             H    OCH3   CH3   N365   ″    H     CONHCH2CH2ClH    OCH3   OCH3  CH366   ″    ″    ″             H    OCH3   CH3   N367   ″    CH3  ″             H    OCH3   OCH3  CH36B   ″    ″    ″             H    OCH3   CH3   N369   ″    H     CSNHCH2CH2ClH    OCH3   OCH3  CH370   ″    ″    ″             H    OCH3   CH3   N371   ″    CH3  ″             H    OCH3   OCH3  CH372   ″    ″    ″             H    OCH3   CH3   N373   ″    H     CONH-n-C4H9 H    OCH3   OCH3  CH374   ″    ″    ″             H    OCH3   CH3   N Vb.    R1   R4       R5              R7  X       Y       Z    Fp.℃375    ″    CH3      ″               H    OCH3   OCH3   CH376    ″    ″        ″               H    OCH3   CH3    N377    ″    H         CSNHCH3         H    OCH3   OCH3   CH378    ″    ″        ″               H    OCH3   CH3    N379    ″    CH3      ″               H    OCH3   OCH3   CH380    ″    ″        ″               H    OCH3   CH3    N381    ″    H         CSNHCH2CH＝CH2H    OCH3   OCH3   CH382    ″    ″        ″               H    OCH3   CH3    N383    ″    CH3      ″               H    OCH3   OCH3   CH384    ″    ″        ″               H    OCH3   CH3    N385    ″    CH3      CSNHCH2COCH3  H    OCH3   OCH3   CH386    ″    ″        ″               H    OCH3   CH3    N387    ″    CH3      CSNHCH2COC2H5H    OCH3   OCH3   CH388    ″    ″        ″               H    OCH3   CH3    N389    ″    CH3      CONHCH2COCH3  H    OCH3   OCH3   CH390    ″    ″        ″               H    OCH3   CH3    N391    ″    CH3      CONHCH2COC2H5H    OCH3   OCH3   CH392    ″    ″        ″               H    OCH3   CH3    N393    ″    -CONHCH2CO-               H    OCH3   OCH3   CH394    ″    ″                         H    OCH3   CH3    N395    ″    H         SO2CH2F       H    OCH3   OCH3   CH396    ″    ″        ″               H    OCH3   CH3    N397    ″    CH3      ″               H    OCH3   OCH3   CH398    ″    ″        ″               H    OCH3   CH3    N399    ″    H         SO2CF3        H    OCH3   OCH3   CH400    ″    ″        ″               H    OCH3   CH3    N401    ″    CH3      ″               H    OCH3   OCH3   CH402    ″    ″        ″               H    OCH3   CH3    N403    ″    H         SO2C2H5      H    OCH3   OCH3   CH404    ″    ″        ″               H    OCH3   CH3    N405    ″    CH3      ″               H    OCH3   OCH3   CH406    ″    ″        ″               H    OCH3   CH3    N407    ″    H         SO2-n-C3H7   H    OCH3   OCH3   CH408    ″    ″        ″               H    OCH3   CH3    N409    ″    CH3      ″               H    OCH3   OCH3   CH Vb.    R1   R4     R5           R7  X       Y       Z    Fp.℃410    ″    ″      ″            H    OCH3   CH3    N411    ″    OH      COC2H5     H    OCH3   OCH3   CH412    ″    ″      ″            H    OCH3   CH3    N413    ″    OCH3   ″            H    OCH3   OCH3   CH414    ″    ″      ″            H    OCH3   CH3    N415    ″    OH      COCH2Cl      H    OCH3   OCH3    CH416    ″    ″      ″            H    OCH3   CH3    N417    ″    OCH3   ″            H    OCH3   OCH3   CH418    ″    ″      ″            H    OCH3   CH3    N419    ″    OH      COCF3       H    OCH3   OCH3    CH420    ″    ″      ″            H    OCH3   CH3    N421    ″    OCH3   ″            H    OCH3   OCH3   CH422    ″    ″      ″            H    OCH3   CH3    N423    ″    OH      COCH2OCH3  H    OCH3   OCH3   CH424    ″    ″      ″            H    OCH3   CH3    N425    ″    OCH3   ″            H    OCH3   OCH3   CH426    ″    ″      ″            H    OCH3   CH3    N427    ″    OH      COCO2C2H5 H    OCH3   OCH3   CH428    ″    ″      ″            H    OCH3   CH3    N429    ″    OCH3   ″            H    OCH3   OCH3   CH430    ″    ″      ″            H    OCH3   CH3     N431    ″    OH      COOCH3       H    OCH3   OCH3   CH432    ″    ″      ″            H    OCH3   CH3    N433    ″    OCH3   ″            H    OCH3   OCH3   CH434    ″    ″      ″            H    OCH3   CH3    N435    ″    OH      环丙基        H    OCH3   OCH3   CH436    ″    ″      ″            H    OCH3   CH3    N437    ″    OCH3   ″            H    OCH3   OCH3   CH438    ″    ″      ″            H    OCH3   CH3    N439    ″    OH      COC6H5     H    OCH3   OCH3   CH440    ″    ″      ″            H    OCH3   CH3    N441    ″    OCH3   ″            H    OCH3   OCH3   CH442    ″    ″      ″            H    OCH3   CH3    N443    ″    OH      COCH(CH3)2 H    OCH3   OCH3   CH444    ″    ″      ″            H    OCH3   CH3    N Vb.    R1   R4   R5           R7   X       Y       Z     Fp.℃445    ″    OCH3 ″            H     OCH3   OCH3   CH446    ″    ″    ″            H     OCH3   CH3    N447    ″    OH    COCH＝CH2    H     OCH3   OCH3   CH448    ″    ″    ″            H     OCH3   CH3    N449    ″    OCH3 ″            H     OCH3   OCH3   CH450    ″    ″    ″            H     OCH3   CH3    N451    ″    OH    COC＝CH       H     OCH3   OCH3   CH452    ″    ″    ″            H     OCH3   CH3    N453    ″    OCH3 ″            H     OCH3   OCH3   CH454          ″    ″            H     OCH3   CH3    N455    ″    OH    SO2CH3     H     OCH3   OCH3   CH456    ″    ″    ″            H     OCH3   CH3    N457    ″    OCH3 ″            H     OCH3   OCH3   CH458    ″    ″    ″            H     OCH3   CH3    N459    ″    OH    SO2NHCH3   H     OCH3   OCH3   CH460    ″    ″    ″            H     OCH3   CH3    N461    ″    OCH3 ″            H     OCH3   OCH3   CH462    ″    ″    ″            H     OCH3   CH3    N463    ″    OH    SO3N(CH3)2H     OCH3   OCH3   CH464    ″    ″    ″            H     OCH3   CH3    N465    ″    OCH3 ″            H     OCH3   OCH3   CH466    ″    ″    ″            H     OCH3   CH3    N467    ″    C2H5CHO          H     OCH3   OCH3   CH468    ″    ″    ″            H     OCH3   CH3    N469    ″    ″    COCH3        H     OCH3   OCH3   CH470    ″    ″    ″            H     OCH3   CH3    N471    ″    ″    环丙基        H     OCH3   OCH3   CH472    ″    ″    ″            H     OCH3   CH3    N473    ″    ″    COCH2Cl      H     OCH3   OCH3   CH474    ″    ″    ″            H     OCH3   CH3    N475    ″    ″    COCF3        H     OCH3   OCH3   CH476    ″    ″    ″            H     OCH3   CH3    N477    ″    ″    COOCH3       H     OCH3   OCH3   CH478    ″    ″    ″            H     OCH3   CH3    N479    ″    ″    COC6H5      H     OCH3   OCH3   CH Vb.      R1     R4   R5           R7  X       Y       Z     Fp.℃480    ″        ″    ″            H    OCH3   CH3    N481    ″        ″    CONHC2H5   H    OCH3   OCH3   CH482    ″        ″    ″            H    OCH3   CH3    N483    ″        ″    CSNHC2H5   H    OCH3   OCH3   CH484    ″        ″    ″            H    OCH3   CH3    N485    ″        ″    SO2CH3     H    OCH3   OCH3   CH486    ″        ″    ″            H    OCH3   CH3    N487    ″        ″    SO2NHCH3   H    OCH3   OCH3   CH488    ″        ″    ″            H    OCH3   CH3    N489    ″        ″    SO2N(CH3)2H    OCH3   OCH3   CH490    ″        ″    ″            H    OCH3   CH3    N491    ″        ″    SO2C6H5   H    OCH3   OCH3   CH492    ″        ″    ″            H    OCH3   CH3    N493    CO2C2H5H    CHO           H    OCH3   OCH3   CH494    ″        ″    ″            H    OCH3   CH3    N495    ″        ″    COCH3        H    OCH3   OCH3   CH496    ″        ″    ″            H    OCH3   CH3     N497    ″        ″    SO2CH3      H    OCH3   OCH3   CH498    ″        ″    ″            H    OCH3   CH3    N499    ″        CH3   CHO          H    OCH3   OCH3   CH500    ″        ″    ″            H    OCH3   CH3    N501    ″        ″    COCH3       H    OCH3   OCH3   CH502    ″        ″    ″            H    OCH3   CH3    N503    ″        ″    SO2CH3     H    OCH3   OCH3   CH504    ″        ″    ″            H    OCH3   CH3    N505    ″        C2H5  CHO        H    OCH3   OCH3   CH506    ″        ″    ″            H    OCH3   CH3    N507    ″        ″    COCH3       H    OCH3   OCH3   CH508    ″        ″    ″            H    OCH3   CH3    N509    ″        ″    SO2CH3     H    OCH3   OCH3   CH510    ″        ″    ″            H    OCH3   CH3    N511    ″        OH    CHO           H    OCH3   OCH3   CH512    ″        ″    ″            H    OCH3   CH3    N513    ″        ″    COCH3        H    OCH3   OCH3   CH514    ″        ″    ″            H    OCH3   CH3    N Vb.    R1       R4    R5         R7  X          Y       Z     Fp.℃515    ″        ″     SO2CH3    H    OCH3      OCH3   CH516    ″        ″     ″          H    OCH3      CH3    N517    ″        OCH3  CHO         H    OCH3      OCH3   CH518    ″        ″     ″          H    OCH3      CH3    N519    ″        ″     COCH3      H    OCH3      OCH3   CH520    ″        ″     ″          H    OCH3      CH3    N521    COO-n-Bu  H      CHO         H    ″         OMe     CH522    CONMe2   Me     ″          H    ″         Me      N523    CONHMe    H      ″          H    ″         OMe     CH524    COSMe     Me     CO-Me       H    ″         Me      N525    COOMe     n-Bu   CHO         H    ″         OMe     CH526    ″        ″     ″          H    ″         Me      N527    ″        H      ″          H    OCH2CF3 NMe2   N528    ″        Me     ″          H    ″         ″      N529    ″        H      CO-Me       H    ″         ″      N530    ″        Me     ″          H    ″         ″      N531    ″        ″     SO2CH3   H    OCH3      OCH3   CH532    ″        ″     ″          H    OCH3      CH3    N533    ″
Figure A9419413700901
    H    OCH3      OCH3   CH534    ″               ″          H    OCH3      CH3    N535    CO2CH3  H      COCH3     H    OCH3      OCH3   CH Na-Salz270
表4Vb.  R1     R4   R5   R7   X         Y         Z    Fp.℃1    CO2CH3H     CHO   H    OCH3     OCH3      CH2    ″      ″    ″    H    OCH3     CH3       CH3    ″      ″    ″    H    CH3      CH3       CH4    ″      ″    ″    H    CH3      OC2H5    CH5    ″      ″    ″    H    OCH3     OCH3      N6    ″      ″    ″    H    OCH3     CH3       N7    ″      ″    ″    H    OCH3     Cl         CH8    ″      ″    ″    H    OCF2H    CH3       CH9    ″      ″    ″    H    OCF2H    OCF2H     CH10   ″      ″    ″    H    OCH3     Br         CH11   ″      ″    ″    H    OCH3     OC2H5    CH12   ″      ″    ″    H    OCH3     SCH3      CH13   ″      ″    ″    H    OCH3     OC2H5    N14   ″      ″    ″    H    OCH3     OC3H7    CH15   ″      ″    ″    H    CH3      Cl         CH16   ″      ″    ″    H    Cl        OC2H5    CH17   ″      ″    ″    H    OC2H5   OC2H5    CH18   ″      ″    ″    H    C2H5    OCH3      CH19   ″      ″    ″    H    CF3      OCH3      CH20   ″      ″    ″    H    OCH2CF3 CH3       CH21   ″      ″    ″    H    OCH2CF3 OCH3      CH22   ″      ″    ″    H    OCH2CF3 OCH2CF3  CH23   ″      ″    ″    H    OCH2CF3 OCH3      N24   ″      ″    ″    H    OCH3     CH(OCH3)2CH Vb.   R1   R4   R5     R7    X          Y        Z    Fp.℃25    ″    ″    ″      CH3 OCH3     OCH3      CH26    ″    ″    ″      CH3 OCH3     CH3       N27    ″    H     COCH3  H    OCH3     OCH3      CH28    ″    ″    ″      H    OCH3     CH3       CH29    ″    ″    ″      H    CH3      CH3       CH30    ″    ″    ″      H    CH3      OC2H5    CH31    ″    ″    ″      H    OCH3     OCH3      N32    ″    ″    ″      H    OCH3     CH3       N33    ″    ″    ″      H    OCH3     Cl         CH34    ″    ″    ″      H    OCF2H    CH3       CH35    ″    ″    ″      H    OCF2H    OCF2H     CH36    ″    ″    ″      H    OCH3     Br         CH37    ″    ″    ″      H    OCH3     OC2H5    CH38    ″    ″    ″      H    OCH3     SCH3      CH39    ″    ″    ″      H    OCH3     OC2H5    N40    ″    ″    ″      H    OCH3     OC3H7    CH41    ″    ″    ″      H    CH3      Cl         CH42    ″    ″    ″      H    Cl        OC2H5    CH43    ″    ″    ″      H    OC2H5   OC2H5    CH44    ″    ″    ″      H    C2H5    OCH3      CH45    ″    ″    ″      H    CF3      OCH3      CH46    ″    ″    ″      H    OCH2CF3 CH3       CH47    ″    ″    ″      H    OCH2CF3 OCH3      CH48    ″    ″    ″      H    OCH2CF3 OCH2CF3  CH49    ″    ″    ″      H    OCH2CF3 OCH3      N50    ″    ″    ″      H    OCH3     CH(OCH3)2CH51    ″    ″    ″      CH3 OCH3     OCH3      CH52    ″    ″    ″      CH3 OCH3     CH3       N53    ″    CH3  CHO     H    OCH3     OCH3      CH 150-15154    ″    ″    ″      H    OCH3     CH3       CH55    ″    ″    ″      H    CH3      CH3       CH56    ″    ″    ″      H    CH3      OC2H5    CH57    ″    ″    ″      H    OCH3     OCH3      N58    ″    ″    ″      H    OCH3     CH3       N59    ″    ″    ″      H    OCH3     Cl         CH Vb.   R1   R4   R5   R7   X         Y          Z    Fp.℃60    ″    ″    ″    H    OCF2H    CH3        CH61    ″    ″    ″    H    OCF2H    OCF2H      CH62    ″    ″    ″    H    OCH3     Br          CH63    ″    ″    ″    H    OCH3     OC2H5     CH64    ″    ″    ″    H    OCH3     SCH3       CH65    ″    ″    ″    H    OCH3     OC2H5     N66    ″    ″    ″    H    OCH3     OC3H7     CH67    ″    ″    ″    H    CH3      Cl          CH68    ″    ″    ″    H    Cl        OC2H5     CH69    ″    ″    ″    H    OC2H5   OC2H5     CH70    ″    ″    ″    H    C2H5    OCH3       CH71    ″    ″    ″    H    CF3      OCH3       CH72    ″    ″    ″    H    OCH2CF3 CH3        CH73    ″    ″    ″    H    OCH2CF3 OCH3       CH74    ″    ″    ″    H    OCH2CF3 OCH2CF3   CH75    ″    ″    ″    H    OCH2CF3 OCH3       N76    ″    ″    ″    H    OCH3     CH(OCH3)2 CH77    ″    ″    ″    CH3 OCH3     OCH3       CH78    ″    ″    ″    CH3 OCH3     CH3        N79    ″    CH3  COCH3H    OCH3     OCH3       CH80    ″    ″    ″    H    OCH3     CH3        CH81    ″    ″    ″    H    CH3      CH3        CH82    ″    ″    ″    H    CH3      OC2H5     CH83    ″    ″    ″    H    OCH3     OCH3       N84    ″    ″    ″    H    OCH3     CH3        N85    ″    ″    ″    H    OCH3     Cl          CH86    ″    ″    ″    H    OCF2H    CH3        CH87    ″    ″    ″    H    OCF2H    OCF2H      CH88    ″    ″    ″    H    OCH3     Br          CH89    ″    ″    ″    H    OCH3     OC2H5     CH90    ″    ″    ″    H    OCH3     SCH3       CH91    ″    ″    ″    H    OCH3     OC2H5     N92    ″    ″    ″    H    OCH3     OC3H7     CH93    ″    ″    ″    H    CH3      Cl          CH94    ″    ″    ″    H    Cl        OC2H5     CH Vb.    R1   R4   R5      R7   X          Y          Z     Fp.℃95     ″    ″    ″       H    OC2H5    OC2H5     CH96     ″    ″    ″       H    C2H5     OCH3       CH97     ″    ″    ″       H    CF3       OCH3       CH98     ″    ″    ″       H    OCH2CF3  CH3        CH99     ″    ″    ″       H    OCH2CF3  OCH3       CH100    ″    ″    ″       H    OCH2CF3  OCH2CF3   CH101    ″    ″    ″       H    OCH2CF3  OCH3       N102    ″    ″    ″       H    OCH3      CH(OCH3)2 CH103    ″    ″    ″       CH3 OCH3      OCH3       CH104    ″    ″    ″       CH3 OCH3      CH3        N105    ″    H     SO2CH3H    OCH3      OCH3       CH106    ″    ″    ″       H    OCH3      CH3        CH107    ″    ″    ″       H    CH3       CH3        CH108    ″    ″    ″       H    OCH3      OCH3       N109    ″    ″    ″       H    OCH3      CH3        N110    ″    ″    ″       H    OC2H5    NHCH3      N111    ″    ″    ″       CH3 OCH3      OCH3       CH112    ″    ″    ″       CH3 OCH3      CH3        N113    ″    CH3  SO2CH3H    OCH3      OCH3       CH114    ″    ″    ″       H    OCH3      CH3        CH115    ″    ″    ″       H    CH3       CH3        CH116    ″    ″    ″       H    OCH3      OCH3       N117    ″    ″    ″       H    OCH3      CH3        N118    ″    ″    ″       H    OC2H5    NHCH3      N119    ″    ″    ″       CH3 OCH3      OCH3       CH120    ″    ″    ″       CH3 OCH3      CH3        N121    ″    OH    CHO      H    OCH3      OCH3       CH122    ″    ″    ″       H    OCH3      CH3        CH123    ″    ″    ″       H    CH3       CH3        CH124    ″    ″    ″       H    OCH3      OCH3       N125    ″    ″    ″       H    OCH3      CH3        N126    ″    ″    ″       H    OC2H5    NHCH3      N127    ″    ″    ″       CH3 OCH3      OCH3       CH128    ″    ″    ″       CH3 OCH3      CH3        N129    ″    OCH3 CHO      H    OCH3      OCH3       CH Vb.    R1   R4  R5       R7   X       Y      Z   Fp.℃130    ″    ″    ″         H    OCH3   CH3   CH131    ″    ″    ″         H    CH3    CH3   CH132    ″    ″    ″         H    OCH3   OCH3  N133    ″    ″    ″         H    OCH3   CH3   N134    ″    ″    ″         H    OC2H5 NHCH3 N135    ″    ″    ″         CH3 OCH3   OCH3  CH136    ″    ″    ″         CH3 OCH3   CH3   N137    ″    OH    COCH3     H    OCH3   OCH3  CH138    ″    ″    ″         H    OCH3   CH3   CH139    ″    ″    ″         H    CH3    CH3   CH140    ″    ″    ″         H    OCH3   OCH3  N141    ″    ″    ″         H    OCH3   CH3   N142    ″    ″    ″         H    OC2H5 NHCH3 N143    ″    ″    ″         CH3 OCH3   OCH3  CH144    ″    ″    ″         CH3 OCH3   CH3   N145    ″    OCH3 COCH3     H    OCH3   OCH3  CH146    ″    ″    ″         H    OCH3   CH3   CH147    ″    ″    ″         H    CH3    CH3   CH148    ″    ″    ″         H    OCH3   OCH3  N149    ″    ″    ″         H    OCH3   CH3   N150    ″    ″    ″         H    OC2H5 NHCH3 N151    ″    ″    ″         CH3 OCH3   OCH3  CH152    ″    ″    ″         CH3 OCH3   CH3   N153    ″    H     COC2H5   H    OCH3   OCH3  CH154    ″    ″    ″         H    OCH3   CH3   CH155    ″    ″    ″         H    OCH3   OCH3  N156    ″    ″    ″         H    OCH3   CH3   N157    ″    CH3  ″         H    OCH3   OCH3  CH158    ″    ″    ″         H    OCH3   CH3   CH159    ″    ″    ″         H    OCH3   OCH3  N160    ″    ″    ″         H    OCH3   CH3   N161    ″    H     COCH2OCH3H   OCH3   OCH3  CH162    ″    ″    ″         H    OCH3   CH3   CH163    ″    ″    ″         H    OCH3   OCH3  N164    ″    ″    ″         H    OCH3   CH3   N Vb.    R1   R4   R5          R7  X       Y       Z  Fp.℃165    ″    CH3  ″           H    OCH3   OCH3   CH166    ″    ″    ″           H    OCH3   CH3    CH167    ″    ″    ″           H    OCH3    OCH3   N168    ″    ″    ″           H    OCH3   CH3    N169    ″    H     COCO2C2H5H    OCH3   OCH3   CH170    ″    ″    ″           H    OCH3   CH3    CH171    ″    ″    ″           H    OCH3   OCH3   N172    ″    ″    ″           H    OCH3  CH3    N173    ″    CH3  ″           H    OCH3    OCH3   CH174    ″    ″    ″           H    OCH3   CH3    CH175    ″    ″    ″           H    OCH3   OCH3   N176    ″    ″    ″           H    OCH3   CH3    N177    ″    H     COCF3       H    OCH3    OCH3   CH178    ″    ″    ″           H    OCH3   CH3    CH179    ″    ″    ″           H    OCH3   OCH3   N180    ″    ″    ″           H    OCH3   CH3    N181    ″    CH3  ″           H    OCH3   OCH3   CH182    ″    ″    ″           H    OCH3    CH3    CH183    ″    ″    ″           H    OCH3   OCH3   N184    ″    ″    ″           H    OCH3   CH3    N185    ″    H     COOCH3      H    OCH3   OCH3   CH186    ″    ″    ″           H    OCH3   CH3    CH187    ″    ″    ″           H    OCH3   OCH3   N188    ″    ″    ″           H    OCH3   CH3    N189    ″    CH3  ″           H    OCH3   OCH3   CH190    ″    ″    ″           H    OCH3   CH3    CH191    ″    ″    ″           H    OCH3   OCH3   N192    ″    ″    ″           H    OCH3    CH3    N193    ″    H     CONHC2H5  H    OCH3   OCH3   CH194    ″    ″    ″           H    OCH3   CH3    CH195    ″    ″    ″           H    OCH3   OCH3   N196    ″    ″    ″           H    OCH3   CH3    N197    ″    CH3  ″           H    OCH3   OCH3   CH198    ″    ″    ″           H    OCH3   CH3    CH199    ″    ″    ″           H    OCH3   OCH3   N Vb.    R1   R4        R5           R7  X       Y      Z Fp.℃200    ″    ″        ″            H    OCH3   CH3   N201    ″    H         CSNHC2H5   H    OCH3   OCH3  CH202    ″    ″        ″            H    OCH3   CH3   CH203    ″    ″        ″            H    OCH3   OCH3  N204    ″    ″        ″            H    OCH3   CH3   N205    ″    CH3      ″            H    OCH3   OCH3  CH206    ″    ″        ″            H    OCH3   CH3   CH207    ″    ″        ″            H    OCH3   OCH3  N208    ″    ″        ″            H    OCH3   CH3   N209    ″    H         SO2NHCH3   H    OCH3   OCH3  CH210    ″    ″        ″            H    OCH3   CH3   CH211    ″    ″        ″            H    OCH3   OCH3  N212    ″    ″        ″            H    OCH3   CH3   N213    ″    CH3      ″            H    OCH3   OCH3  CH214    ″    ″        ″            H    OCH3   CH3   CH215    ″    ″        ″            H    OCH3   OCH3  N216    ″    ″        ″            H    OCH3   CH3   N217    ″    H         SO2N(CH3)2H    OCH3   OCH3  CH218    ″    ″        ″            H    OCH3   CH3   CH219    ″    ″        ″            H    OCH3   OCH3 N220    ″    ″        ″            H    OCH3   CH3   N221    ″    CH3      ″            H    OCH3   OCH3  CH222    ″    ″        ″            H    OCH3   CH3   CH223    ″    ″        ″            H    OCH3   OCH3  N224    ″    ″        ″            H    OCH3   CH3   N225    ″    -CH2CH2CH2CO-       H    OCH3   OCH3  CH226    ″          ″                H    OCH3   CH3   CH227    ″          ″                H    OCH3   OCH3  N228    ″          ″                H    OCH3   CH3   N229    ″    -CH2CH2CH2SO2-     H    OCH3   OCH3  CH230    ″          ″                H    OCH3   CH3   CH231    ″          ″                H    OCH3   OCH3  N232    ″          ″                H    OCH3   CH3   N233    ″    -CH2CH2CH2CH2CO-   H    OCH3   OCH3  CH234    ″          ″                H     CH3   CH3   CH Vb.    R1   R4   R5              R7  X       Y       Z Fp.℃235    ″          ″               H    OCH3   OCH3   N236    ″          ″               H    OCH3   CH3    N237    ″    -CH2CH2CH2CH2SO2-H   OCH3   OCH3   CH238    ″          ″               H    OCH3   CH3    CH239    ″          ″               H    OCH3   OCH3   N240    ″          ″               H    OCH3   CH3    N241    ″    -CH2CH2OCH2CH2-   H    OCH3   OCH3   CH242    ″          ″               H    OCH3   CH3    CH243    ″          ″               H    OCH3   OCH3   N244    ″          ″               H    OCH3   CH3    N245    ″    H         COC3H7    H    OCH3   OCH3   CH246    ″    ″        ″           H    OCH3   CH3    CH247    ″    ″        ″           H    OCH3   OCH3   N248    ″    ″        ″           H    OCH3   CH3    N249    ″    CH3      ″           H    OCH3   OCH3   CH250    ″    ″        ″           H    OCH3   CH3    CH251    ″    ″        ″           H    OCH3   OCH3   N252    ″    ″        ″           H    OCH3   CH3    N253    ″    H         COCH2Cl     H    OCH3   OCH3   CH254    ″    ″        ″           H    OCH3   CH3    CH255    ″    ″        ″           H    OCH3   OCH3   N256    ″    ″        ″           H    OCH3   CH3    N257    ″    CH3      ″           H    OCH3   OCH3   CH258    ″    ″        ″           H    OCH3   CH3    CH259    ″    ″        ″           H    OCH3   OCH3   N260    ″    ″        ″           H    OCH3   CH3    N261    ″    H         COCHCl2     H    OCH3   OCH3   CH262    ″    ″        ″           H    OCH3   CH3    CH263    ″    ″        ″           H    OCH3   OCH3   N264    ″    ″        ″           H    OCH3   CH3    N265    ″    CH3      ″           H    OCH3   OCH3   CH266    ″    ″        ″           H    OCH3   CH3    CH267    ″    ″        ″           H    OCH3   OCH3   N268    ″    ″        ″           H    OCH3   CH3    N269    ″    H         COCCl3      H    OCH3   OCH3   CH Vb     R1   R4         R5       R7  X       Y       Z    Fp℃270    ″    ″          ″         H    OCH3   CH3    CH271    ″    ″          ″         H    OCH3   OCH3   N272    ″    ″          ″         H    OCH3   CH3    N273    ″    CH3        ″         H    OCH3   OCH3   CH274    ″    ″          ″         H    OCH3   CH3    CH275    ″    ″          ″         H    OCH3   OCH3   N276    ″    ″          ″         H    OCH3   CH3    N277    ″    H           COCH＝CH2 H    OCH3  OCH3   CH278    ″    ″          ″         H    OCH3   CH3    CH279    ″    ″          ″         H    OCH3   OCH3   N280    ″    ″          ″         H    OCH3   CH3    N281    ″    CH3        ″         H    OCH3   OCH3   CH282    ″    ″          ″         H    OCH3   CH3    CH283    ″    ″          ″         H    OCH3   OCH3   N284    ″    ″          ″         H    OCH3   CH3    N285    ″    H           COC＝CH    H    OCH3   OCH3   CH286    ″    ″          ″         H    OCH3   CH3    CH287    ″    ″          ″         H    OCH3   OCH3   N288    ″    ″          ″         H    OCH3   CH3    N289    ″    CH3        ″         H    OCH3   OCH3   CH290    ″    ″          ″         H    OCH3   CH3    CH291    ″    ″          ″         H    OCH3   OCH3   N292    ″    ″          ″         H    OCH3   CH3    N293    ″    H           COC6H5   H    OCH3   OCH3   CH294    ″    ″          ″         H    OCH3   CH3    CH295    ″    ″          ″         H    OCH3   OCH3   N296    ″    ″          ″         H    OCH3   CH3    N297    ″    CH3        ″         H    OCH3   OCH3  CH298    ″    ″          ″         H    OCH3   CH3    CH299    ″    ″          ″         H    OCH3   OCH3   N300    ″    ″          ″         H    OCH3   CH3    N301    ″    SO2C6H5  SO2C6H5H   OCH3   OCH3   CH302    ″    ″          ″         H    OCH3   CH3    CH303    ″    ″          ″         H    OCH3   OCH3   N304    ″    ″          ″         H    OCH3   CH3    N Vb    R1    R4       R5           R7  X       Y       Z     Fp.℃305    ″    SO2CH3  SO2CH3     H    OCH3   OCH3   CH306    ″    ″        ″            H    OCH3   CH3    CH307    ″    ″        ″            H    OCH3   OCH3   N308    ″    ″        ″            H    OCH3   CH3    N309    ″    H         COCH2Br      H    OCH3   OCH3   CH310    ″    ″        ″            H    OCH3   CH3    N311    ″    CH3      ″            H    OCH3   OCH3   CH312    ″    ″        ″            H    OCH3   CH3    N313    ″    H         COCH2F       H    OCH3   OCH3    CH314    ″    ″        ″            H    OCH3   CH3    N315    ″    CH3      ″            H    OCH3   OCH3   CH316    ″    ″        ″            H    OCH3   CH3    N317    ″    H         COCH2C＝CH   H    OCH3   OCH3   CH318    ″    ″        ″            H    OCH3   CH3    N319    ″    CH3      ″            H    OCH3   OCH3   CH320    ″    ″        ″            H    OCH3   CH3    N321    ″    H         COCO2CH3   H    OCH3   OCH3   CH322    ″    ″        ″            H    OCH3   CH3    N323    ″    CH3      ″            H    OCH3   OCH3   CH324    ″    ″        ″            H    OCH3   CH3    N325    ″    H         CO2C2H5   H    OCH3   OCH3   CH326    ″    ″        ″            H    OCH3   CH3    N327    ″    CH3      ″            H    OCH3   OCH3   CH328    ″    ″        ″            H    OCH3   CH3    N329    ″    H         COSCH3       H    OCH3   OCH3   CH330    ″    ″        ″            H    OCH3   CH3    N331    ″    CH3      ″            H    OCH3   OCH3    CH332    ″    ″        ″            H    OCH3   CH3    N333    ″    H         CSOCH3       H    OCH3   OCH3   CH334    ″    ″        ″            H    OCH3   CH3    N335    ″    CH3      ″            H    OCH3   OCH3   CH336    ″    ″        ″            H    OCH3   CH3    N337    ″    H         CSSCH3       H    OCH3   OCH3   CH338    ″    ″        ″            H    OCH3   CH3    N339    ″    CH3      ″            H    OCH3   OCH3   CH Vb.    R1    R4   R5                R7  X       Y     Z      Fp.℃340    ″    ″    ″                  H    OCH3   CH3   N341    ″    H     COCH(CH3)2       H    OCH3   OCH3  CH342    ″    ″    ″                 H    OCH3   CH3   N343    ″    CH3  ″                 H    OCH3   OCH3  CH344    ″    ″    ″                 H    OCH3   CH3   N345    ″    H     COC(CH3)3       H    OCH3   OCH3  CH346    ″    ″    ″                 H    OCH3   CH3   N347    ″    CH3  ″                 H    OCH3   OCH3  CH348    ″    ″    ″                 H    OCH3   CH3   N349    ″    H     CO-环丙基          H    OCH3   OCH3  CH350    ″    ″    ″                 H    OCH3   CH3   N351    ″    CH3  ″                 H    OCH3   OCH3  CH352    ″    ″    ″                 H    OCH3   CH3   N353    ″    H     CO-环丁基          H    OCH3   OCH3  CH354    ″    ″    ″                 H    OCH3   CH3   N355    ″    CH3  ″                 H    OCH3   OCH3  CH356    ″    ″    ″                 H    OCH3   CH3   N357    ″    H     CO-环戊基          H    OCH3   OCH3  CH358    ″    ″    ″                 H    OCH3   CH3   N359    ″    CH3  ″                 H    OCH3   OCH3  CH360    ″    ″    ″                 H    OCH3   CH3   N361    ″    H     CO-环己基          H    OCH3   OCH3  CH362    ″    ″    ″                 H    OCH3   CH3   N363    ″    CH3  ″                 H    OCH3   OCH3  CH364    ″    ″    ″                 H    OCH3   CH3   N365    ″    H     CONHCH2CH2Cl    H    OCH3   OCH3  CH366    ″    ″    ″                 H    OCH3   CH3   N367    ″    CH3  ″                 H    OCH3   OCH3  CH368    ″    ″    ″                 H    OCH3   CH3   N369    ″    H     CSNHCH2CH2Cl    H    OCH3   OCH3  CH370    ″    ″    ″                 H    OCH3   CH3   N371    ″    CH3  ″                 H    OCH3   OCH3  CH372    ″    ″    ″                 H    OCH3   CH3   N373    ″    H     CONH-n-C4H9     H    OCH3   OCH3  CH374    ″    ″    ″                 H    OCH3   CH3   N Vb.    R1   R4      R5             R7   X        Y     Z    Fp.℃375    ″    CH3     ″               H    OCH3   OCH3   CH376    ″    ″       ″               H    OCH3   CH3    N377    ″    H        CSNHCH3         H    OCH3   OCH3   CH378    ″    ″       ″               H    OCH3   CH3    N379    ″    CH3     ″               H    OCH3   OCH3   CH380    ″    ″       ″               H    OCH3   CH3    N381    ″    H        CSNHCH2CH＝CH2H    OCH3   OCH3   CH382    ″    ″       ″               H    OCH3   CH3    N383    ″    CH3     ″               H    OCH3   OCH3   CH384    ″    ″       ″               H    OCH3   CH3    N385    ″    CH3     CSNHCH2COCH3  H    OCH3   OCH3   CH386    ″    ″       ″               H    OCH3   CH3    N387    ″    CH3     CSNHCH2COC2H5H    OCH3   OCH3   CH388    ″    ″       ″               H    OCH3   CH3    N389    ″    CH3     CONHCH2COCH3  H    OCH3   OCH3   CH390    ″    ″       ″               H    OCH3   CH3    N391    ″    CH3     CONHCH2COC2H5H    OCH3   OCH3   CH392    ″    ″       ″               H    OCH3   CH3    N393    ″    -CONHCH2CO-              H    OCH3   OCH3   CH394    ″    ″                        H    OCH3   CH3    N395    ″    H        SO2CH2F       H    OCH3   OCH3   CH396    ″    ″       ″               H    OCH3   CH3    N397    ″    CH3     ″               H    OCH3   OCH3   CH398    ″    ″       ″               H    OCH3   CH3    N399    ″    H        SO2CF3        H    OCH3   OCH3   CH400    ″    ″       ″               H    OCH3   CH3    N401    ″    CH3     ″               H    OCH3   OCH3   CH402    ″    ″       ″               H    OCH3   CH3    N403    ″    H        SO2C2H5      H    OCH3    OCH3   CH404    ″    ″       ″               H    OCH3   CH3    N405    ″    CH3     ″               H    OCH3   OCH3   CH406    ″    ″       ″               H    OCH3   CH3    N407    ″    H        SO2-n-C3H7   H    OCH3   OCH3   CH408    ″    ″       ″               H    OCH3   CH3   N409    ″    CH3     ″               H    OCH3   OCH3   CH Vb.    R1   R4   R5           R7  X       Y     Z    Fp℃410          ″    ″            H   OCH3   CH3   N411    ″    OH    COC2H5      H   OCH3   OCH3  CH412    ″    ″    ″            H   OCH3   CH3   N413    ″    OCH3 ″            H   OCH3   OCH3  CH414    ″    ″    ″            H   OCH3   CH3   N415    ″    OH    COCH2Cl      H   OCH3   OCH3  CH416    ″    ″    ″            H   OCH3   CH3   N417    ″    OCH3 ″            H   OCH3   OCH3  CH418    ″    ″    ″            H   OCH3   CH3   N419    ″    OH    COCF3        H   OCH3   OCH3  CH420    ″    ″    ″            H   OCH3   CH3   N421    ″    OCH3 ″            H   OCH3   OCH3   CH422    ″    ″    ″            H   OCH3   CH3   N423    ″    OH    COCH2OCH3  H   OCH3   OCH3  CH424    ″    ″    ″            H   OCH3   CH3   N425    ″    OCH3 ″            H   OCH3   OCH3  CH426    ″    ″    ″            H   OCH3   CH3   N427    ″    OH    COCO2C2H5 H   OCH3  OCH3  CH428    ″    ″    ″            H   OCH3   CH3   N429    ″    OCH3 ″            H   OCH3   OCH3  CH430    ″    ″    ″            H   OCH3   CH3   N431    ″    OH    COOCH3       H   OCH3   OCH3  CH432    ″    ″    ″            H   OCH3   CH3   N433    ″    OCH3 ″            H   OCH3   OCH3  CH434    ″    ″    ″            H   OCH3  CH3   N435    ″    OH    环丙基        H   OCH3   OCH3  CH436    ″    ″    ″            H   OCH3   CH3   N437    ″    OCH3 ″            H   OCH3   OCH3  CH438    ″    ″    ″            H   OCH3   CH3   N439    ″    OH    COC6H5     H   OCH3   OCH3   CH440    ″    ″    ″            H   OCH3   CH3   N441    ″    OCH3 ″            H   OCH3   OCH3  CH442    ″    ″    ″            H   OCH3   CH3   N443    ″    OH    COCH(CH3)2 H   OCH3   OCH3  CH444    ″    ″    ″            H   OCH3   CH3   N Vb.   R1   R4   R5          R7  X       Y     Z   Fp.℃445   ″    OCH3 ″           H   OCH3   OCH3  CH446   ″    ″    ″           H   OCH3   CH3   N447   ″    OH    COCH＝CH2   H   OCH3   OCH3  CH448   ″    ″    ″           H   OCH3    CH3   N449   ″    OCH3 ″           H   OCH3   OCH3  CH450   ″    ″    ″           H   OCH3   CH3   N451   ″    OH    COCH＝CH     H   OCH3   OCH3  CH452   ″    ″    ″           H   OCH3   CH3   N453   ″    OCH3 ″           H   OCH3   OCH3  CH454   ″    ″    ″           H   OCH3   CH3   N455   ″    OH    SO2CH3    H   OCH3   OCH3  CH456   ″    ″    ″           H   OCH3   CH3   N457   ″    OCH3 ″           H   OCH3   OCH3  CH458   ″    ″    ″           H   OCH3   CH3   N459   ″    OH    SO2NHCH3  H   OCH3   OCH3  CH460   ″    ″    ″           H   OCH3    CH3   N461   ″    OCH3 ″           H   OCH3    OCH3  CH462   ″    ″    ″           H   OCH3   CH3   N463   ″    OH    SO2N(CH3)2H  OCH3   OCH3  CH464   ″    ″    ″           H   OCH3   CH3   N465   ″    OCH3 ″           H   OCH3   OCH3  CH466   ″    ″    ″           H   OCH3   CH3   N467   ″    C2H5CHO         H   OCH3    OCH3  CH468   ″    ″    ″           H   OCH3   CH3   N469   ″    ″    COCH3       H   OCH3  OCH3  CH470   ″    ″    ″           H   OCH3   CH3   N471   ″    ″    环丙基       H   OCH3   OCH3  CH472   ″    ″    ″           H   OCH3   CH3   N473   ″    ″    COCH2Cl     H   OCH3    OCH3  CH474   ″    ″    ″           H   OCH3    CH3   N475   ″    ″    COCF3       H   OCH3   OCH3  CH476   ″    ″    ″           H   OCH3   CH3   N477   ″    ″    COOCH3      H   OCH3   OCH3  CH478   ″    ″    ″           H   OCH3   CH3   N479   ″    ″    COC6H5    H   OCH3   OCH3  CH Vb     R1        R4    R5          R7   X       Y     Z    Fp℃480    ″         ″    ″            H    OCH3   CH3   N481    ″         ″    CONHC2H5   H    OCH3   OCH3  CH482    ″         ″    ″            H    OCH3   CH3   N483    ″         ″    CSNHC2H5   H    OCH3   OCH3  CH484    ″         ″    ″            H    OCH3   CH3   N485    ″         ″    SO2CH3     H    OCH3   OCH3  CH486    ″         ″    ″            H    OCH3   CH3   N487    ″         ″    SO2NHCH3   H    OCH3   OCH3  CH488    ″         ″    ″            H    OCH3   CH3   N489    ″         ″    SO2N(CH3)2H    OCH3   OCH3  CH490    ″         ″    ″            H    OCH3   CH3   N491    ″         ″    SO2C6H5   H    OCH3   OCH3  CH492    ″         ″    ″            H    OCH3   CH3   N493    CO2C2H5 H     CHO          H    OCH3   OCH3  CH494    ″         ″    ″            H    OCH3   CH3   N495    ″         ″    COCH3       H    OCH3   OCH3  CH496    ″         ″    ″            H    OCH3   CH3   N497    ″         ″    SO2CH3     H    OCH3   OCH3  CH498    ″         ″    ″            H    OCH3   CH3   N499    ″         CH3  CHO          H    OCH3   OCH3 CH500    ″         ″    ″            H    OCH3   CH3   N501    ″         ″    COCH3        H    OCH3   OCH3  CH502    ″         ″    ″            H    OCH3   CH3   N503    ″         ″    SO2CH3     H    OCH3   OCH3  CH504    ″         ″    ″            H    OCH3   CH3   N505    ″         C2H5CHO          H    OCH3   OCH3  CH506    ″         ″    ″            H    OCH3   CH3   N507    ″         ″    COCH3       H    OCH3   OCH3  CH508    ″         ″    ″            H    OCH3   CH3   N509    ″         ″    SO2CH3     H    OCH3   OCH3  CH510    ″         ″    ″            H    OCH3   CH3   N511    ″         OH    CHO           H    OCH3   OCH3  CH512    ″         ″    ″            H    OCH3   CH3   N513    ″         ″    COCH3        H    OCH3   OCH3  CH514    ″         ″    ″            H    OCH3   CH3   N Vb     R1       R4     R5           R7   X       Y     Z    Fp℃515    ″        ″    SO2CH3         H    OCH3    OCH3  CH516    ″        ″    ″               H    OCH3    CH3   N517    ″        OCH3 CHO              H    OCH3    OCH3  CH518    ″        ″    ″               H    OCH3    CH3   N519    ″        ″    COCH3           H    OCH3    OCH3  CH520    ″        ″    ″               H    OCH3    CH3   N521    COO-n-Bu  H     CHO              H    ″       OMe    CH522    CONMe2   Me    ″               H    ″       Me     N523    CONHMe    H     ″               H    ″       OMe    CH524    CO-SMe    Me    CO-Me            H    ″       Me     N525    CO-OMe    n-Bu  CHO              H    ″       OMe    CH526    ″        n-Bu  ″               H    ″       Me     N527    ″        H     ″               H    OCH2CF3NMe2  N528    ″        Me    ″               H    ″       ″     N529    ″        H     CO-Me            H    ″       ″     N530    ″        Me    ″               H    ″       ″     N531    ″        ″    SO2CH3        H    OCH3    OCH3  CH532    ″        ″    ″               H    OCH3    CH3   N533    CO2CH3
Figure A9419413701061
  H    OCH3    OCH3  CH534    ″              ″                H    OCH3    CH3   N
B.制剂实施例a)粉剂的制备是通过混合10重量份的式(I)化合物和90重量份惰性物质滑石并在锤磨中磨碎混合物。b)容易分散在水中的可湿性粉剂的制备是通过混合25重量份的式(I)化合物，64重量份惰性物质含高岭土石英，10重量份木质素磺酸钾和1重量份油酰基甲基牛磺酸钠作为湿润剂和分散剂，并在钉盘磨研磨混合物。c)容易分散在水中的浓悬浮液的制备是通过混合20重量份的式(I)化合物和6重量份的烷基酚聚乙二醇醚(riton X 207)，3重量份的异十三烷醇聚乙二醇醚(8EO)和71重量份石蜡矿物油(沸点范围例如大约255至277℃)，并在球磨中研磨混合物至细度小于5微米。d)可乳化浓缩液的制备是通过混合15重量份的式(I)化合物，75重量份的环己烷溶剂和10重量份乙氧基化的壬基酚乳化剂。e)水分散颗粒剂的制备是通过混合
75重量份   式(I)化合物
10重量份   木质素磺酸钙
5重量份    十二烷基硫酸钠
3重量份    聚乙烯醇和
7重量份    高岭土，在针盘磨(stiftmhle)中研磨混合物并通过喷入作为成粒流体的水于流动床上形成颗粒粉末。f)水分散性颗粒剂的制备还可通过在胶体磨中的匀化和预粉碎25重量份的式(I)化合物，5重量份    2，2’-二萘基甲烷-6，6’-二磺酸钠2重量份    牛酰基甲基牛磺酸钠
       (oleoylmethyltaurinsaures Natrium)1重量份    聚乙烯醇17重量份    碳酸钙和50重量份    水，然后在珠磨中研磨混合物用单物质-喷嘴在喷雾塔中将所得悬浮液雾化，并干燥产品。C.生物实施例1.对杂草的苗前作用
将单子叶和双子叶杂草品种的种子或根茎放置于塑料盆中的沙质沃土中并用土盖上。然后将根据本发明式(I)化合物或其盐作为可湿性粉剂或乳化浓缩液的水悬浮液或乳液，以600至800l水/ha的施用剂量，按不同剂量施用到覆盖土的表面。
处理后，将盆放置在温室中并保持杂草生长的良好条件。试验期3至4周后，在供试植物萌发后，与未处理对照物比较，目测评价对植物的损害和对萌发的损害。如试验结果所示，根据本发明化合物对广谱的禾本科杂草和双子叶杂草具有好的苗前除草活性。例如表1中实施例1，27，53至55，58，59，79，105，113，129，145，153，177，181，185，189，213，217，221，253，257，421，425，429，433，437，445，457，461，465，467，485，487，535，至543，547，551至559，562，563，和565至578和表2中实施例1，27，53，79，153，161，169，177，181，185，253，261，269，341，349，365和373和表3中的实施例27和535和表4中的实施例53的化合物，以每公顷0.3Kg至0.005Kg活性物质的剂量施用，对有害植物如田白芥、繁缕、珍珠菊和多花黑麦草具有好的苗前作用。2.对杂草的苗后作用
将单子叶和双子叶杂草品种的种子或根茎放置于塑料盆中的沙质沃土中并用土盖上并使之在良好条件的温室中生长。播种3周后，处理三叶期的的植物。将根据本发明式(I)化合物或其盐作为可湿性粉剂或乳化浓缩液剂以不同的剂量，以600至800l水/ha施用剂量，施用到植物的绿色部分，其后在理想的生长条件下，将供试植物放置在温室中大约3至4周，与未处理对照物比较，目测评价制剂的活性。根据本发明制剂还对经济上重要的广谱的禾本科杂草和双子叶杂草具有好的苗后除草活性。例如表1中实施例1，27，53至55，58，59，79，105，113，129，145，153，177，181，185，189，213，217，221，253，257，421，425，429，433，437，445，457，461，465，467，485，487，535，至543，547，551至559，562，563，和565至578和表2中实施例1，27，53，79，153，161，169，177，181，185，253，261，269，341，349，365和373和表3中的实施例27和535和表4中的实施例53的化合物，以每公顷0.3Kg至0.005Kg活性物质的剂量施用，对有害植物如田白芥、繁缕、珍珠菊和多花黑麦草具有好的苗后作用。3.作物的耐药性
在进一步的温室试验中，将许多种作物和杂草的种子放置于砂质沃土中并用土覆盖。
按照1.中所述方法立即处理一些盆，并把其余盆放在温室中直到植物发育出二至三个真叶，然后如2.所述用不同剂量的根据本发明的式(I)化合物或其盐进行喷雾。
施药并放置在温室中四至五周后进行目测评价，结果显示甚至在高活性物质使用剂量下，根据本发明化合物在苗前-和苗后-使用对双子叶作物不会造成任何伤害，双子叶作物如大豆、棉花、油菜、糖甜菜和土豆。而且，一些物质甚至对禾本科作物无害，禾本科作物如大麦、小麦、黑麦、高粱、小米、玉米或水稻。因此，式(I)化合物或其盐在防治农作物中有害植物生长时具有高度的选择性。

Claims (9)

1.式(I)的化合物或其盐，
其中
R1为CO-Q-R8，
R2和R3各自独立为H或(C1-C4)烷基，
R4为H，未取代或被一或多个下组包括的基团取代的(C1-C8)
烷基，上述取代基团由卤素、(C1-C4)烷氧基、(C1-C4)
烷硫基、(C1-C4)烷基亚磺酰基、(C1-C4)烷基磺酰基、[(C1
-C4)烷氧基]羰基和CN组成，或为未被取代或被一至多个卤原
子取代的(C3-C6)链烯基，或为未被取代或被一至多个卤原子
取代的(C3-C6)链炔基，或为羟基，(C1-C4)烷氧基，[(C1-C4)
烷基]羰基或(C1-C4)烷基磺酰基，后三个基团各自未被取代或
在烷基部分被-或多个卤原子或被(C1-C4)烷氧基或(C1-
C4)烷硫基取代，或为苯基磺酰基，其中苯基是未被取代或取代的，
R5为(C1-C4)烷基磺酰基或(C3-C6)链烯基磺酰基，后两
个基团各自未被取代或被一至多个卤原子或被(C1-C4)烷氧基
或(C1-C4)烷硫基取代的，或为苯基磺酰基或苯基羰基，后两
个基团的苯基各自未被取代或被取代，或为单-或二-[(C1-
C4)烷基]氨基磺酰基或[(C1-C6)烷基]羰基，后三个基团各自未被取
代或被一或多个下述基团取代，上述取代基由卤素、(C1-C4)
烷氧基、(C1-C4)烷硫基、(C1-C4)烷基亚磺酰基、(C1
-C4)烷基磺酰基、[(C1-C4)烷基]羰基、[(C1-C4)烷氧
基]羰基和CN组成，或为甲酰基，式-CO-CO-R’的基团
其中R’＝H，OH，(C1-C4)烷氧基或(C1-C4)烷基，
或为[(C3-C6)环烷基]羰基，[(C2-C6)链烯基]羰基或[(C2-C6)链炔基]
羰基，后三个基团各自未被取代或被一或多个卤原子取代，或为下
式的基团
Figure A9419413700031
或
R4和R5一起为是(-CH2)mB-或-B1-(CH2)ml-B-，
上述链是未被取代或被一个或多个(C1-C3)烷基取代和m为3
或4或m1为2或3，和
W为氧或硫原子，
B和B1各自独立为SO2或CO，
Q为O，S或-NR13-，
T为O或S，
R6为H，(C1-C4)烷基，(C1-C4)烷氧基，[(C1-C4)
烷基]羰基或[(C1-C4)烷氧基]羰基，后四个基团各自未被取代
或在烷基部分被一至多个卤原子取代，或为卤素，NO2或CN，
R7为H或CH3，
R8为H，(C1-C4)烷基，(C3-C4)链烯基或(C3-C4)
链炔基，后三个基团各自未被取代或被一或多个选自由卤素、(C1
-C4)烷氧基、(C1-C4)烷硫基、[(C1-C4)烷基]羰基和
[(C1-C4)烷氧基]羰基组成的一组基团取代，
R9为(C1-C4)烷基，(C3-C4)链烯基或(C3-C4)链炔
基，后三个基团各自未被取代或被一或多个选自由卤素、(C1-
C4)烷氧基、(C1-C4)烷硫基、[(C1-C4)烷基]羰基和[(C1
-C4)烷氧基]羰基组成的一组基团取代，
R10和R11各自独立地为H，(C1-C4)烷基，(C3-C4)链烯
基或(C3-C4)链炔基，后三个基团各自未被取代或被一或多个
由卤素、(C1-C4)烷氧基、(C1-C4)烷硫基、[(C1-C4)
烷基]羰基和[(C1-C4)烷氧基]羰基组成的一组基团取代，
R12基团与氮原子一起为5或6元杂环，上述杂环在可能的氧化态
中可含有一个其它N，O和S杂原子，且是未被取代或被(C1-
C4)烷基或氧基取代，或被苯环稠和，
R13为H，(C1-C4)烷基，(C3-C4)链烯基或(C3-C4)
链炔基，后三个基团各自未被取代或被一或多个由卤素、(C1-
C4)烷氧基、(C1-C4)烷硫基组成的一组基团取代，
A为下式的基团
X和Y基团之一是氢，卤素，(C1-C3)烷基或(C1-C3)烷
氧基，后两个基团是未被取代或被卤素单取代或多取代或被(C1
-C3)烷氧基单取代，和
X和Y基团的另一个是氢，(C1-C3)烷基，(C1-C3)烷氧
基或(C1-C3)烷硫基，后三个含有烷基的基团是未被取代或被
卤原子单或多取代或被(C1-C3)烷氧基或(C1-C3)烷硫基
单取代或二取代，或为式NR14R15的基团，(C3-C6)环烷基，
(C2-C4)链烯基，(C2-C4)链炔基，(C3-C4)链烯氧
基，(C3-C4)链炔氧基，
Z为CH或N，
R14和R15各自彼此独立地为H，(C1-C3)烷基，(C3-C4)
链烯基，
X1为CH3、OCH3、OC2H5或OCHF2，
Y1为-O-或-CH2-
X2为CH3、C2H5或CH2CF3
Y2为OCH3、OC2H5、SCH3、SCH2CH3、CH3或C2H5
X3为CH3或OCH3，
Y3为H或CH3，
X4为CH3、OCH3、OC2H5、CH2OCH3或Cl，
Y4为CH3、OCH3、OC2H5或Cl和
Y5为CH3、C2H5、OCH3或Cl。
2.根据权利要求1的化合物及其盐，其中
R4为H，未取代或被一或多个下组包括的基团取代的(C1-C4)
烷基，上述取代基团由卤素、(C1-C4)烷氧基、(C1-C4)
烷硫基、(C1-C4)烷基磺酰基、[(C1-C4)烷氧基]羰基和
CN组成，或为(C3-C4)链烯基、(C3-C4)链炔基、羟基，
(C1-C4)烷氧基，[(C1-C4)烷基]羰基或(C1-C4)烷基磺酰
基，后五个基团各自未被取代或在烷基部分被一至多个卤原子取
代，或为苯基磺酰基，其中苯基是未被取代或被一或多个下述基团
取代的，取代基由卤素、(C1-C4)烷基和(C1-C4)烷氧基
组成，和
R5为(C1-C4)烷基磺酰基、(C1-C4)卤代烷基磺酰基、苯
基磺酰基或苯基羰基，后两个基团中的苯基各自未被取代或被一至
多个选自卤原子、(C1-C4)烷基和(C1-C4)烷氧基的基团
取代，或为单-或二-[(C1-C4)烷基]氨基磺酰基，未被取代
或被一或多个卤原子或(C1-C4)烷氧基或(C1-C4)烷硫基
取代的[(C1-C6)烷基]羰基，或为甲酰基、OHC-CO-、2-氧
-(C3-C5)链烷酰基、[(C1-C4)烷氧基]草酰基、[(C3-C6)
环烷基]羰基，[(C2-C4)链烯基]羰基或[(C2-C4)链炔基]羰基、或为下
式的基团
W为O或S
R6为H、(C1-C4)烷基、(C1-C4)卤代烷基、(C1-C4)
烷氧基、(C1-C4)卤代烷氧基或卤素，
R8各自为未被取代或被一或多个卤原子取代的(C1-C4)烷基，
或为(C3-C4)链烯基或(C3-C4)链炔基，
R9为H、未被取代或被一或多个卤原子或被(C1-C4)烷氧基、
(C1-C4)烷硫基、[(C1-C4)烷氧基]羰基和[(C1-C4)
烷基]羰基取代的(C1-C4)烷基，
R10和R11各自独立地为H、未被取代或被一或多个卤原子取代的
(C1-C4)烷基、或为(C3-C4)链烯基或(C3-C4)链炔
基、其中R10和R11至少一个不是氢，
R12基团与氮原子一起为5或6元杂环，上述杂环在不同的氧化态
中可含有一个其它N，O和S杂原子，且是未被取代或被(C1-
C4)烷基或氧基取代，
R13为H，未被取代或被一或多个由卤素原子取代的(C1-C4)
烷基、或为(C3-C4)链烯基或(C3-C4)链炔基。
3.根据权利要求1或2的化合物及其盐，其中
R4为H、(C1-C4)烷基、羟基或(C1-C4)烷氧基，
R5为(C1-C4)烷基磺酰基、CHO、未被取代或被一或多个卤
原子取代的[(C1-C4)烷基]羰基、或为[(C1-C4)烷氧基]
草酰基、[(C3-C6)环烷基]羰基或下式的基团
Figure A9419413700081
其中
W，T和R9至R12如上面式(I)中的定义，
R6为H、(C1-C3)烷基、(C1-C3)烷氧基或卤素，
A为下式的基团
Z为CH或N，和
X和Y基团之一为卤素、(C1-C2)烷基、(C1-C2)烷氧基、
OCF2H、CF3或OCH2CF3和X和Y的另一个为(C1-C2)烷
基、(C1-C2)烷氧基或(C1-C2)卤代烷氧基。
4.根据权利要求1的式(I)化合物或其盐的制备方法，其中包括
a)式(II)的化合物与式(III)杂环氨基甲酸酯反应
Figure A9419413700091
R*-O-CO-NR7-A    (III)
其中R*是必要时被取代的苯基或(C1-C4)烷基，或
b)式(IV)的苯基磺酰基氨基甲酸酯与式(V)的氨基杂环反应
Figure A9419413700092
    H-NR7-A    (V)
或
c)式(VI)的磺酰基异氰酸酯与式(V)H-NR7-A的氨基杂
环反应
Figure A9419413700101
或
d)在一个单釜反应中，首先在碱存在下使式(V)H-NR7-A
的氨基杂环化物与光气反应，然后反应的中间体与式(II)的苯
基磺酰胺反应，或
e)在碱存在下式(VII)的磺酰氯与其中M＝NH4、Na或K的
氰酸酯M-OCN以及式(V)H-NR7-A的氨基杂环化物反
应，
f)在碱存在下上述式(II)的磺酰胺与式(V’)的(硫代)异
氰酸酯反应
           W＝C＝N-A    (V’)，
在式(II)-(VII)和(V’)中的基团R1-R7、A或W如
在式(I)中的定义，在方法a)-e)中，最初获得的是W＝O的式
(I)化合物。
5.一种除草和植物生长调节剂组合物，其中包含至少一种根据权利
要求1至3的式(I)化合物或其盐和植物保护中常用的制剂助剂。
6.一种防治有害植物或调节植物生长的方法，其中包含施用有效量
的至少一种根据权利要求1至3的式(I)化合物或其盐于有害植
物或植物、其植物种子或其生长地。
7.根据权利要求1至3的式(I)化合物或其盐作为除草剂或植物
生长调节剂的用途。
8.式(II)化合物
Figure A9419413700111
其中R1至R6如权利要求1中式(I)的定义。
9.根据权利要求8的式(II)化合物的制备方法，其中包含采用类
似于已知的方法使式(XV)化合物反应以除去叔丁基保护基
Figure A9419413700112
式(XV)中R1至R6如式(II)中的定义。
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CN102119701B (zh) * 1996-12-07 2013-11-20 赫彻斯特-舍林农业发展有限公司 包含苯磺酰胺的除草组合物
CN100344612C (zh) * 2000-07-24 2007-10-24 拜尔作物科学有限公司 经取代的磺酰氨基甲基苯甲酸（衍生物）及其制备方法
CN102792958A (zh) * 2011-05-23 2012-11-28 山东滨农科技有限公司 含有甲基二磺隆和唑嘧磺草胺的除草剂组合物
CN102792960A (zh) * 2011-05-23 2012-11-28 山东滨农科技有限公司 含有甲基二磺隆和氟啶嘧磺隆的除草剂组合物
CN103404528A (zh) * 2012-01-16 2013-11-27 河北博嘉农业有限公司 甲基二磺隆复配除草剂
CN102550585A (zh) * 2012-01-16 2012-07-11 河北博嘉农业有限公司 甲基二磺隆复配除草剂
CN103404528B (zh) * 2012-01-16 2015-07-08 河北博嘉农业有限公司 甲基二磺隆复配除草剂
CN103355336A (zh) * 2013-07-30 2013-10-23 河北博嘉农业有限公司 氟磺隆复配的玉米田除草剂
CN103524386A (zh) * 2013-10-24 2014-01-22 滨海白云化工有限公司 2-氨基-4-甲磺酰胺甲基苯甲酸甲酯的制备方法
CN103755603A (zh) * 2014-01-28 2014-04-30 江苏省农用激素工程技术研究中心有限公司 2-氨基磺酰基-4-甲磺酰胺基甲基苯甲酸甲酯的制备方法
CN106305749A (zh) * 2016-08-15 2017-01-11 河南省莱恩坪安园林植保有限公司 一种结缕草中防治杂草的除草剂
CN106305749B (zh) * 2016-08-15 2019-01-25 河南省莱恩坪安园林植保有限公司 一种结缕草中防治杂草的除草剂
CN114456120A (zh) * 2021-12-24 2022-05-10 郑州手性药物研究院有限公司 双磺酰氨基取代的磺酰脲类化合物及其制备方法和应用
CN114456120B (zh) * 2021-12-24 2024-06-18 郑州手性药物研究院有限公司 双磺酰氨基取代的磺酰脲类化合物及其制备方法和应用

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EP0723534B1 (de) 1998-07-29
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UA44714C2 (uk) 2002-03-15
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