公开(公告)号：US4052413A

公开(公告)日：1977-10-04

申请号：US705376

申请日：1976-07-14

申请人： Zoltan George Hajos

发明人： Zoltan George Hajos

IPC分类号： C07C62/26 ,  C07C62/38 ,  C07D317/72

CPC分类号： C07C62/38 ,  C07C62/26 ,  C07C2103/16

摘要： Total synthesis of known progestationally active steroidal materials. The steroids can be synthesized depending on the particular starting reactants selected by employing as intermediates bicyclic compounds of the formula ##STR1## WHEREIN M IS AN INTEGER HAVING A VALUE OF 1 OR 2; R.sub.4 is hydrogen or lower alkyl; Z is lower alkylenedioxy, CH(OR.sub.2) and carbonyl; R.sub.8 when taken alone is hydrogen; R.sub.9 when taken alone is lower alkoxycarbonyl, aryloxy-carbonyl, lower cycloalkyloxycarbonyl, carbonyl-halide, hydrogen, carboxy, formyl and methylene-X, where X is a leaving group and when taken together are methylene; with the proviso that when Z is carbonyl R.sub.8 when taken alone is hydrogen; R.sub.9 when taken alone is carbonyl halide, hydrogen, carboxy, formyl and methylene-X where X is a leaving group and when taken together are methylene and R.sub.2 is hydrogen, lower alkyl, lower alkoxy-lower alkyl, phenyl-lower alkyl, tetrahydropyranyl, lower alkanoyl, benzoyl, nitrobenzoyl, carboxy-lower alkanoyl, carboxy-benzoyl, trifluoroacetyl and camphorsulfonylAnd reacting them in the case where R.sub.8 and R.sub.9 taken together are methylene or R.sub.8 is hydrogen and R.sub.9 is methylene-X with .beta.-keto esters and other analogs of the formula ##STR2## wherein R.sub.6 is selected from the group consisting of ##STR3## and lower alkyl; R.sub.7 is lower alkyl; R.sub.15 is selected from the group consisting of oxo, lower alkylenedioxy or (hydrogen and lower alkoxy); B is selected from the group consisting of lower alkoxy-carbonyl-methylene, lower-aryloxy-carbonyl-methylene, cyanomethylene, lower alkyl sulfinyl-methylene, lower alkyl sulfonyl-methylene, and R.sub.25 and R.sub.26 are independently selected from the group consisting of hydrogen, hydroxyl and lower alkyl.

公开(公告)号：US3965117A

公开(公告)日：1976-06-22

申请号：US482541

申请日：1974-06-24

申请人： Zoltan George Hajos

发明人： Zoltan George Hajos

IPC分类号： C07C62/26 ,  C07C62/38 ,  C07C103/19

CPC分类号： C07C62/26 ,  C07C62/38 ,  C07C2103/16

摘要： Total synthesis of known progestationally active steroidal materials. The steroids can be synthesized depending on the particular starting reactants selected by employing as intermediates bicyclic compounds of the formula ##SPC1##Wherein m is an integer having a value of 1 or 2; R.sub.4 is hydrogen or lower alkyl; Z is lower alkylenedioxy, CH(OR.sub.2) and carbonyl; R.sub.8 when taken alone is hydrogen; R.sub.9 when taken alone is lower alkoxycarbonyl, aryloxy-carbonyl, lower cycloalkyloxycarbonyl, carbonyl-halide, hydrogen, carboxy, formyl and methylene-X, where X is a leaving group and when taken together are methylene; with the proviso that when Z is carbonyl R.sub.8 when taken alone is hydrogen; R.sub.8 when taken alone is carbonyl halide, hydrogen, carboxy, formyl and methylene-X where X is a leaving group and when taken together are methylene and R.sub.2 is hydrogen, lower alkyl, lower alkoxy-lower alkyl, phenyl-lower alkyl, tetrahydropyranyl, lower alkanoyl, benzoyl, nitrobenzoyl, carboxy-lower alkanoyl, carboxybenzoyl, trifluoroacetyl and camphorsulfonyl.

摘要翻译： 已知的促孕活性甾体材料的全合成。 可以根据通过使用作为中间体选择的特定起始反应物来合成类固醇，其具有下式的双环化合物，其中M是具有1或2的值的整数; R4是氢或低级烷基; Z是低亚烷基二氧基，CH（OR 2）和羰基; 单独使用时为R8; 当单独使用时，R 9为低级烷氧基羰基，芳氧基羰基，低级环烷氧基羰基，羰基卤化物，氢，羧基，甲酰基和亚甲基-X，其中X为离去基团，并且一起为亚甲基时; 条件是当Z为羰基时，当单独使用时为氢; 当单独使用时，R 8为羰基卤，氢，羧基，甲酰基和亚甲基-X，其中X为离去基团，当一起为亚甲基且R 2为氢时，低级烷基，低级烷氧基 - 低级烷基，苯基 - 低级烷基，四氢吡喃基， 低级烷酰基，苯甲酰基，硝基苯甲酰基，羧基 - 低级烷酰基，羧基苯甲酰基，三氟乙酰基和樟脑磺酰基。

公开(公告)号：US3950389A

公开(公告)日：1976-04-13

申请号：US482540

申请日：1974-06-24

申请人： Zoltan George Hajos

发明人： Zoltan George Hajos

IPC分类号： C07C62/26 ,  C07C62/38 ,  C07C61/36 ,  C07C69/74

CPC分类号： C07C62/26 ,  C07C62/38 ,  C07C2103/16

摘要： Total synthesis of known progestationally active steroidal materials. The steroids can be synthesized depending on the particular starting reactants selected by employing as intermediates bicyclic compounds of the formula ##SPC1##Wherein m is an integer having a value of 1 or 2; R.sub.4 is hydrogen or lower alkyl; Z is lower alkylenedioxymethylene CH(OR.sub.2) and carbonyl; R.sub.8 when taken alone is hydrogen; R.sub.9 when taken alone is lower alkoxycarbonyl, aryloxy-carbonyl, lower cycloalkyloxycarbonyl, carbonyl-halide, hydrogen, carboxy, formyl and methylene-X, where X is a leaving group and when taken together are methylene; with the proviso that when Z is carbonyl R.sub.8 when taken alone is hydrogen; R.sub.9 when taken alone is carbonyl halide, hydrogen, carboxy, formyl and methylene-X where X is a leaving group and when taken together are methylene and R.sub.2 is hydrogen, lower alkyl, lower alkoxy-lower alkyl, phenyl-lower alkyl, tetrahydropyranyl, lower alkanoyl, benzoyl, nitrobenzoyl, carboxy-lower alkanoyl, carboxybenzoyl, trifluoroacetyl and camphorsulfonylAnd reacting them in the case where R.sub.8 and R.sub.9 taken together are methylene or R.sub.8 is hydrogen and R.sub.9 is methylene-X with .beta.-keto esters and other analogs of the formula ##EQU1## wherein R.sub. 6 is selected from the group CONSISTING OF ##EQU2## and LOWER ALKYL; R.sub.7 is lower alkyl; R.sub.15 is selected from the group consisting of oxo, lower alkylene-dioxy or (hydrogen and lower alkoxy); B is selected from the group consisting of lower alkoxy-carbonyl-methylene, lower-aryloxy-carbonyl-methylene, cyanomethylene, lower alkyl sulfinyl-methylene, lower alkyl sulfonyl-methylene, and R.sub.25 and R.sub.26 are independently selected from the group consisting of hydrogen, hydroxyl and lower alkyl.

摘要翻译： 已知的促孕活性甾体材料的全合成。 可以根据通过使用作为中间体选择的特定起始反应物来合成类固醇，其具有下式的双环化合物，其中M是具有1或2的值的整数; R4是氢或低级烷基; Z是低级亚烷基二氧基亚甲基CH（OR 2）和羰基; 单独使用时为R8; 当单独使用时，R 9为低级烷氧基羰基，芳氧基羰基，低级环烷氧基羰基，羰基卤化物，氢，羧基，甲酰基和亚甲基-X，其中X为离去基团，并且一起为亚甲基时; 条件是当Z为羰基时，当单独使用时为氢; 当单独使用时，R 9是卤素，氢，羧基，甲酰基和亚甲基-X，其中X是离去基团，当它们一起是亚甲基且R 2是氢时，低级烷基，低级烷氧基 - 低级烷基，苯基 - 低级烷基，四氢吡喃基， 低级烷酰基，苯甲酰基，硝基苯甲酰基，羧基 - 低级烷酰基，羧基苯甲酰基，三氟乙酰基和樟脑磺酰，并在其中反应。其中R8和R9一起为亚甲基或R8为氢，R9为亚甲基-X，带有β-酮酯和其他类似物 式O PARALLEL R6-CBV其中R 6选自下列基团：R 26 R 25 | R 7 -C-CH-CH-CH 2 - 并行R 15和低级烷基; R7是低级烷基; R 15选自氧代，低级亚烷基 - 二氧基或（氢和低级烷氧基）; B选自低级烷氧基 - 羰基 - 亚甲基，低级 - 芳氧基 - 羰基 - 亚甲基，氰基亚甲基，低级烷基亚磺酰基 - 亚甲基，低级烷基磺酰基 - 亚甲基，R 25和R 26独立地选自氢 ，羟基和低级烷基。

公开(公告)号：US3929876A

公开(公告)日：1975-12-30

申请号：US48271374

申请日：1974-06-24

申请人： HOFFMANN LA ROCHE

发明人： HAJOS ZOLTAN GEORGE

IPC分类号： C07C62/26 ,  C07C62/38 ,  C07C61/36

CPC分类号： C07C62/26 ,  C07C62/38 ,  C07C2603/16

摘要： Total synthesis of known progestationally active steroidal materials. The steroids can be synthesized depending on the particular starting reactants selected by employing as intermediates bicyclic compounds of the formula

WHEREIN M IS AN INTEGER HAVING A VALUE OF 1 OR 2; R4 is hydrogen or lower alkyl; Z is lower alkylenedioxy methylene, CH(OR2) and carbonyl; R8 when taken alone is hydrogen; R9 when taken alone is lower alkoxycarbonyl, aryloxy-carbonyl, lower cycloalkyloxycarbonyl, carbonyl-halide, hydrogen, carboxy, formyl and methylene-X, where X is a leaving group and when taken together are methylene; with the proviso that when Z is carbonyl R8 when taken alone is hydrogen; R9 when taken alone is carbonyl halide, hydrogen, carboxy, formyl and methylene-X where X is a leaving group and when taken together are methylene and R2 is hydrogen, lower alkyl, lower alkoxy-lower alkyl, phenyl-lower alkyl, tetrahydropyranyl, lower alkanoyl, benzoyl, nitrobenzyl, carboxy-lower alkanoyl, carboxybenzoyl, trifluoroacetyl and camphorsulfonyl.

摘要翻译： 已知的促孕活性甾体材料的全合成。 可以根据通过使用作为中间体选择的特定起始反应物来合成类固醇，其具有下式的双环化合物，其中M是具有1或2的值的整数; R4是氢或低级烷基; Z是低级亚烷基二氧基亚甲基，CH（OR 2）和羰基; 单独使用时为R8; 当单独使用时，R 9为低级烷氧基羰基，芳氧基羰基，低级环烷氧基羰基，羰基卤化物，氢，羧基，甲酰基和亚甲基-X，其中X为离去基团，并且一起为亚甲基时; 条件是当Z为羰基时，当单独使用时为氢; 当单独使用时，R 9是卤素，氢，羧基，甲酰基和亚甲基-X，其中X是离去基团，当它们一起是亚甲基且R 2是氢时，低级烷基，低级烷氧基 - 低级烷基，苯基 - 低级烷基，四氢吡喃基， 低级烷酰基，苯甲酰基，硝基苄基，羧基 - 低级烷酰基，羧基苯甲酰基，三氟乙酰基和樟脑磺酰基。

公开(公告)号：US3927031A

公开(公告)日：1975-12-16

申请号：US48271474

申请日：1974-06-24

申请人： HOFFMANN LA ROCHE

发明人： HAJOS ZOLTAN GEORGE

IPC分类号： C07C62/26 ,  C07C62/38 ,  C07C49/27 ,  C07D317/26

CPC分类号： C07C49/523 ,  C07C62/26 ,  C07C62/38 ,  C07C205/43 ,  C07C2603/16

摘要： Total synthesis of known progestationally active steroidal materials. The steroids can be synthesized depending on the particular starting reactants selected by employing as intermediates bicyclic compounds of the formula
and lower alkyl; R7 is lower alkyl; R15 is selected from the group consisting of oxo, lower alkylenedioxy or (hydrogen and lower alkoxy); B is selected from the group consisting of lower alkoxy-carbonyl-methylene, lower-aryloxy-carbonyl-methylene, cyanomethylene, lower alkyl sulfinyl-methylene, lower alkyl sulfonyl-methylene, and R25 and R26 are independently selected from the group consisting of hydrogen, hydroxyl and lower alkyl.

wherein R6 is selected from the group

WHEREIN M IS AN INTEGER HAVING A VALUE OF 1 OR 2; R4 is hydrogen or lower alkyl;; Z is lower alkylenedioxymethylene, CH(OR2) and carbonyl; R8 when taken alone is hydrogen; R9 when taken alone is lower alkoxycarbonyl, aryloxy-carbonyl, lower cycloalkyloxycarbonyl, carbonyl-halide, hydrogen, carboxy, formyl and methylene-X, where X is a leaving group and when taken together are methylene; with the proviso that when Z is carbonyl R8 when taken alone is hydrogen; R9 when taken alone is carbonyl halide, hydrogen, carboxy, formyl and methylene-X where X is a leaving group and when taken together are methylene and R2 is hydrogen, lower alkyl, lower alkoxy-lower alkyl, phenyllower alkyl, tetrahydropyranyl, lower alkanoyl, benzoyl, nitrobenzoyl, carboxy-lower alkanoyl, carboxybenzoyl, trifluoroacetyl and camphorsulfonyl AND REACTING THEM IN THE CASE WHERE R8 and R9 taken together are methylene or R8 is hydrogen and R9 is methylene-X with Beta keto esters and other analogs of the formula


D R A W I N G

摘要翻译： 已知的促孕活性甾体材料的全合成。 可以根据通过使用作为中间体选择的特定起始反应物来合成类固醇，其具有下式的双环化合物，其中M是具有1或2的值的整数; R4是氢或低级烷基; Z是低级亚烷基二氧基亚甲基，CH（OR 2）和羰基; 单独使用时为R8; 当单独使用时，R 9为低级烷氧基羰基，芳氧基羰基，低级环烷氧基羰基，羰基卤化物，氢，羧基，甲酰基和亚甲基-X，其中X为离去基团，并且一起为亚甲基时; 条件是当Z为羰基时，当单独使用时为氢; 当单独使用时，R 9是卤素，氢，羧基，甲酰基和亚甲基-X，其中X是离去基团，当它们一起是亚甲基且R 2是氢时，低级烷基，低级烷氧基 - 低级烷基，苯基 - 低级烷基，四氢吡喃基， 低级烷酰基，苯甲酰基，硝基苯甲酰基，羧基 - 低级烷酰基，羧基苯甲酰基，三氟乙酰基和樟脑磺酰，并在其中反应。其中R8和R9一起为亚甲基或R8为氢，R9为亚甲基-X，带有β-酮酯和其他类似物 式O-PARALLEL R6-CBV其中R6选自基团R26R25 || R7-C-CH-CH2-PAR-PARALLELR15和低级烷基; R7是低级烷基; R 15选自氧代，低级亚烷基二氧基或（氢和低级烷氧基）; B选自低级烷氧基 - 羰基 - 亚甲基，低级 - 芳氧基 - 羰基 - 亚甲基，氰基亚甲基，低级烷基亚磺酰基 - 亚甲基，低级烷基磺酰基 - 亚甲基，R 25和R 26独立地选自氢 ，羟基和低级烷基。

公开(公告)号：US3852331A

公开(公告)日：1974-12-03

申请号：US29807072

申请日：1972-10-16

申请人： HOFFMANN LA ROCHE

发明人： HAJOS Z

IPC分类号： C07C62/26 ,  C07C62/38 ,  C07C69/00

CPC分类号： C07C62/38 ,  C07C62/26 ,  C07C2603/16

摘要： Total synthesis of known progestationally active steroidal materials. The steroids can be synthesized depending on the particular starting reactants selected by employing as intermediates bicyclic compounds of the formula

WHEREIN M IS AN INTEGER HAVING A VALUE OF 1 OR 2; R4 is hydrogen or lower alkyl; Z is lower alkylenedioxy, CH(OR2) and carbonyl; R8 when taken along is hydrogen; R9 when taken alone is lower alkoxycarbonyl, aryloxy-carbonyl, lower cycloalkyloxycarbonyl, carbonyl-halide, hydrogen, carboxy, formyl and methylene-X, where X is a leaving group and when taken together are methylene; with the proviso that when Z is carbonyl R8 when taken alone is hydrogen; R9 when taken alone is carbonyl halide, hydrogen, carboxy, formyl and methylene-X where X is a leaving group and when taken together are methylene and R2 is hydrogen, lower alkyl, lower alkoxy-lower alkyl, PHENYL-LOWER ALKYL, TETRAHYDROPYRANYL, LOWER ALKANOYL, BENZOYL, NITROBENZOYL, CARBOXY-LOWER ALKANOYL, CARBOXY-BENZOYL, TRIFLUOROACETYL AND CAMPHORSULFONYL AND REACTING THEM IN THE CASE WHERE R8 and R9 taken together are methylene or R8 is hydrogen and R9 is methylene-X with Beta keto esters and other analogs of the formula

WHEREIN R6 is selected from the group

LOWER ALKYL; R7 is lower alkyl; R15 is selected from the group consisting of oxo, lower alkylene-dioxy or (hydrogen and lower alkoxy); B is selected from the group consisting of lower alkoxycarbonyl-methylene, lower-aryloxy-carbonyl-methylene, cyanomethylene, lower alkyl sulfinyl-methylene, lower alkyl sulfonyl-methylene, and R25 and R26 are independently selected from the group consisting of hydrogen, hydroxyl and lower alkyl.

摘要翻译： 已知的促孕活性甾体材料的全合成。 可以根据通过使用作为中间体选择的特定起始反应物来合成类固醇，其具有下式的双环化合物，其中M是具有1或2的值的整数; R4是氢或低级烷基; Z是低亚烷基二氧基，CH（OR 2）和羰基; 取R8时为氢; 当单独使用时，R 9为低级烷氧基羰基，芳氧基羰基，低级环烷氧基羰基，羰基卤化物，氢，羧基，甲酰基和亚甲基-X，其中X为离去基团，并且一起为亚甲基时; 条件是当Z为羰基时，当单独使用时为氢; 当单独使用时，R 9是羰基卤，氢，羧基，甲酰基和亚甲基-X，其中X是离去基团，当它们一起是亚甲基且R 2是氢时，低级烷基，低级烷氧基 - 低级烷基，苯基 - 低级烷基，四氢呋喃基， 低级烷基，苯甲酰基，硝基苯甲酰，羧基 - 低级烷基，羧基 - 苯甲酰基，三氟乙酸和环戊二烯并在其中反应。其中R8和R9一起为亚甲基或R8为氢，R9为亚甲基-X，带有β-酮酯等 式WHERE R6的类似物选自LOWER ALKYL; R7是低级烷基; R 15选自氧代，低级亚烷基 - 二氧基或（氢和低级烷氧基）; B选自低级烷氧基 - 羰基 - 亚甲基，低级 - 芳氧基 - 羰基 - 亚甲基，氰基亚甲基，低级烷基亚磺酰基 - 亚甲基，低级烷基磺酰基 - 亚甲基，R 25和R 26独立地选自氢 ，羟基和低级烷基。

公开(公告)号：US3197485A

公开(公告)日：1965-07-27

申请号：US21084262

申请日：1962-07-18

申请人： SHIONOGI & CO

发明人： WATARU NAGATA

IPC分类号： C07C29/147 ,  C07C35/44 ,  C07C62/26 ,  C07J1/00 ,  C07J5/00 ,  C07J7/00 ,  C07J9/00 ,  C07J21/00 ,  C07J63/00 ,  C07J71/00 ,  C07J75/00

CPC分类号： C07J71/00 ,  C07C29/147 ,  C07C35/44 ,  C07C62/26 ,  C07C2603/26 ,  C07C2603/42 ,  C07C2603/48 ,  C07J1/00 ,  C07J5/00 ,  C07J7/00 ,  C07J9/00 ,  C07J21/00 ,  C07J63/00 ,  C07J63/008 ,  C07J71/0042 ,  C07J75/00

摘要： The invention comprises compounds having the following formulae wherein R is a hydrogen atom or an alkanoyl group having not more than 8 carbon atoms. These compounds are obtained by subjecting a 17-oxo compound having the formula to a Grignard reaction to obtain the 17a -methyl - 17b - hydroxy compound which on dehydration yields the D 16-17-methyl compound. Dehydration may be effected with phosphorus oxychloride. Specification 873,019 also is referred to.

公开(公告)号：US20110313032A1

公开(公告)日：2011-12-22

申请号：US13141614

申请日：2009-12-23

申请人： Cóncepcion González Bello ,  Verónica Filipa Vieira Prazeres ,  Sonia Paz Gómez ,  Cristina Sánchez Sixto ,  Lorena Tizón Valverde

发明人： Cóncepcion González Bello ,  Verónica Filipa Vieira Prazeres ,  Sonia Paz Gómez ,  Cristina Sánchez Sixto ,  Lorena Tizón Valverde

IPC分类号： A61K31/381 ,  C07C62/26 ,  C07D333/60 ,  C07D409/12 ,  C07D333/54 ,  C07D333/24 ,  C07C51/09 ,  C07D307/00 ,  C07D495/08 ,  C07F7/08 ,  C07D409/10 ,  A61K31/19 ,  A61K31/192 ,  A61P31/00 ,  A61P31/06 ,  A61P35/00 ,  A61P1/00 ,  A61P1/04 ,  C07C62/38

CPC分类号： C07D333/16 ,  C07C62/26 ,  C07C62/38 ,  C07D333/54 ,  C07D333/56

摘要： The present invention is directed to a compound of formula (I), its diastereoisomers, its enantiomers or its pharmaceutically acceptable salts or solvates, formula (I), to procedures of obtaining the same, to intermediates thereof, and use as competitive inhibitors of the third enzyme of the shikimic acid pathway, the type II dehydroquinase.

摘要翻译： 本发明涉及式（I）化合物，其非对映异构体，其对映异构体或其药学上可接受的盐或溶剂化物，式（I），其获得方法的中间体，并用作 莽草酸途径的第三种酶II型脱氢喹喔啉。

公开(公告)号：US06569810B1

公开(公告)日：2003-05-27

申请号：US10245431

申请日：2002-09-17

申请人： Reiner Fischer ,  Michael Ruther ,  Alan Graff ,  Arno Widdig ,  Jacques Dumas ,  Christoph Erdelen ,  Peter Dahmen ,  Markus Dollinger ,  Ulrike Wachendorff-Neumann

发明人： Reiner Fischer ,  Michael Ruther ,  Alan Graff ,  Arno Widdig ,  Jacques Dumas ,  Christoph Erdelen ,  Peter Dahmen ,  Markus Dollinger ,  Ulrike Wachendorff-Neumann

IPC分类号： A01N4328

CPC分类号： C07D317/72 ,  A01N35/06 ,  C07C45/455 ,  C07C49/697 ,  C07C49/747 ,  C07C49/753 ,  C07C62/26 ,  C07C69/013 ,  C07C69/757 ,  C07C69/96 ,  C07C309/66 ,  C07C2601/14 ,  C07C2602/24 ,  C07D317/08

摘要： The present invention relates to novel bicyclic cyclopentane-1,3-dione derivatives of the formula (I) to a process for their preparation and to their use as pesticides and herbicides.

摘要翻译： 本发明涉及式（I）的新型双环环戊烷-1,3-二酮衍生物，其用于制备和用作农药和除草剂的方法。

公开(公告)号：US06500958B2

公开(公告)日：2002-12-31

申请号：US10176528

申请日：2002-06-24

申请人： Atsuro Nakazato ,  Toshihito Kumagai ,  Kazunari Sakagami ,  Kazuyuki Tomisawa

发明人： Atsuro Nakazato ,  Toshihito Kumagai ,  Kazunari Sakagami ,  Kazuyuki Tomisawa

IPC分类号： C07D23500

CPC分类号： C07D235/02 ,  C07C62/26 ,  C07C65/40 ,  C07C69/757 ,  C07C2602/18 ,  C07D339/06 ,  C07D495/10

摘要： The present invention relates to compounds which are useful for efficient synthesis of 2-amino-4-oxobicyclo[3.1.0]hexane-2,6-dicarboxylic acids. The compounds according to the present invention comprise 2-oxobicyclo[3.1.0]hexane-6-carboxylic acid derivatives represented by the formula as follows: [wherein, R1 represents a hydrogen atom, a C1-C6 alkyl group, a C3-C6 cycloalkyl group, a C3-C6 cycloalkyl C1-C6 alkyl group, an aryl group, an aryl C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group, a C1-C6 hydroxyalkyl group, a C1-C6 alkylthio C1-C6 alkyl group, a C1-C6 mercaptoalkyl group, a tetrahydrofuranyl group, or a tetrahydropyranyl group; R2 and R3 are identical or different, and each represents a C1-C6 alkyl group, a C3-C6 cycloalkyl group, a C3-C6 cycloalkyl C1-C6 alkyl group, an aryl group, or an aryl C1-C6 alkyl group, or alternatively, R2 and R3 together represent —(CH2)n— (wherein n represents 2 or 3); and Y1 and Y2 are identical or different, and each represents a sulfur atom, an oxygen atom, or a nitrogen atom].

摘要翻译： 本发明涉及可用于高效合成2-氨基-4-氧代双环[3.1.0]己烷-2,6-二羧酸的化合物。根据本发明的化合物包含2-氧代双环[3.1.0] 由下式表示的己烷-6-羧酸衍生物：[其中，R1表示氢原子，C1-C6烷基，C3-C6环烷基，C3-C6环烷基C1-C6烷基，芳基 基团，芳基C1-C6烷基，C1-C6烷氧基C1-C6烷基，C1-C6羟基烷基，C1-C6烷硫基C1-C6烷基，C1-C6巯基烷基，四氢呋喃基， 或四氢吡喃基; R2和R3相同或不同，各自表示C1-C6烷基，C3-C6环烷基，C3-C6环烷基C1-C6烷基，芳基或芳基C1-C6烷基，或 或者，R2和R3一起表示 - （CH 2）n - （其中n表示2或3）; Y 1和Y 2相同或不同，各自表示硫原子，氧原子或氮原子]。