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1. 发明申请

US20100010225A1 ISOQUINUCLIDINE DERIVATIVE AND METHOD FOR MANUFACTURING 1-CYCLOHEXENE-1-CARBOXYLIC ACID DERIVATIVE USING THE SAME 审中-公开
标题翻译：使用该化合物的异喹啉衍生物及其制备1-环己基-1-羧酸衍生物的方法
公开(公告)号：US20100010225A1
公开(公告)日：2010-01-14
申请号：US12309674
申请日：2007-07-27
申请人： Tohru Fukuyama , Satoshi Yokoshima , Nobuhiro Satoh
发明人： Tohru Fukuyama , Satoshi Yokoshima , Nobuhiro Satoh
IPC分类号： C07D221/22 , C07D453/02
CPC分类号： C07C271/24 , C07C269/00 , C07C2601/16 , C07D453/06 , C07D491/18 , Y02P20/55
摘要： The present invention provides an isoquinuclidine derivative which can be used to easily synthesize oseltamivir or an analog thereof. In particular, the present invention provides an isoquinuclidine derivative represented by the following formula (1) or an enantiomer thereof: wherein in the formula (1), A represents a protective group for the nitrogen atom; R1 to R1 each independently represent an alkyl group which may have a substituent, an aryl group which may have a substituent, or a hydrogen atom; and X represents a halogen atom.
摘要翻译：本发明提供了可用于容易地合成奥司他韦或其类似物的异奎宁环衍生物。特别是本发明提供下述式（1）所示的异奎宁环衍生物或其对映异构体：其中，在式（1）中，A表示氮原子的保护基; R 1〜R 1各自独立地表示可以具有取代基的烷基，可以具有取代基的芳基或氢原子; X表示卤素原子。

2. 发明授权

US07420052B2 Intermediates for synthesis of vinblastine, process for preparation of the intermediates and process for synthesis of vinblastines 失效
标题翻译：用于合成长春花碱的中间体，中间体的制备方法和长春花碱的合成方法
公开(公告)号：US07420052B2
公开(公告)日：2008-09-02
申请号：US11464560
申请日：2006-08-15
申请人： Tohru Fukuyama , Hidetoshi Tokuyama , Satoshi Yokoshima
发明人： Tohru Fukuyama , Hidetoshi Tokuyama , Satoshi Yokoshima
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , C07D519/04 , C07F7/1804
摘要： An intermediate for vinblastine synthesis represented by general formula A. general formula A. (in the formula, R1, R2, R3 and R4 are the group selected independently from the group consisting of H, lower alkyl group, lower alkoxy group, halogen, lower perfluoroalkyl group, lower alkylthio group, hydroxy group, amino group, mono- or di-alkyl or acylamino group, lower alkyl or arylsulfonyloxy group. R5 is H, or a lower alkyl group or a substituted or non-substituted aryl group, R6 is an alkyl group of carbon number 4 or less, R7 is a substituted or non-substituted aryl group, R8 is a substituted or non-substituted aryl group or lower alkyl group and R9 is an acyl group or trialkylsilyl group.) A method for synthesis of the compound of general formula A utilizing radical ring forming reaction of thioanilides and using the compound of general formula B as the starting material, synthesizing thioanilide of general formula C by the reaction with compound 1 and the formation of a 11-membered ring by intramolecular alkylation of 2-nitrobenzenesulfonamide by which the reactions can proceed under mild conditions and high yield can be accomplished.
摘要翻译：通式A表示的长春花碱合成中间体（通式A）（式中，R 1，R 2，R 3，和 R 4是独立地选自H，低级烷基，低级烷氧基，卤素，低级全氟烷基，低级烷硫基，羟基，氨基，单 - 或二 - 烷基或酰氨基，低级烷基或芳基磺酰氧基，R 5是H或低级烷基或取代或未取代的芳基，R 6是烷基碳原子数4以下的基团，R 7是取代或未取代的芳基，R 8是取代或未取代的芳基或低级烷基， R 9是酰基或三烷基甲硅烷基。）通过使用硫代苯酰苯胺的自由基形成反应合成通式A的化合物的方法，使用通式B的化合物作为起始原料，合成通过与化合物1的反应和通过2-硝基苯磺酰胺的分子内烷基化形成11元环的通式C的硫代苯胺，可以在温和条件下进行反应并获得高产率。

3. 发明授权

US07238802B2 Intermediates for synthesis of vinblastines, process for preparation of the intermediates and process for synthesis on vinblastines 失效
标题翻译：用于合成长春花碱的中间体，中间体的制备方法和长春花碱合成方法
公开(公告)号：US07238802B2
公开(公告)日：2007-07-03
申请号：US10486384
申请日：2002-08-09
申请人： Tohru Fukuyama , Hidetoshi Tokuyama , Satoshi Yokoshima
发明人： Tohru Fukuyama , Hidetoshi Tokuyama , Satoshi Yokoshima
IPC分类号： C07D487/04 , C07D519/04 , C07F7/18
CPC分类号： C07D487/04 , C07D519/04 , C07F7/1804
摘要： An intermediate for vinblastine synthesis represented by general formula A. general formula A. (in the formula, R1, R2, R3 and R4 are the group selected independently from the group consisting of H, lower alkyl group, lower alkoxy group, halogen, lower perfluoroalkyl group, lower alkylthio group, hydroxy group, amino group, mono- or di-alkyl or acylamino group, lower alkyl or arylsulfonyloxy group. R5 is H, or a lower alkyl group or a substituted or non-substituted aryl group, R6 is an alkyl group of carbon number 4 or less, R7 is a substituted or non-substituted aryl group, R8 is a substituted or non-substituted aryl group or lower alkyl group and R9 is an acyl group or trialkylsilyl group.) A method for synthesis of the compound of general formula A utilizing radical ring forming reaction of thioanilides and using the compound of general formula B as the starting material, synthesizing thioanilide of general formula C by the reaction with compound 1 and the formation of a 11-membered ring by intramolecular alkylation of 2-nitrobenzenesulfonamide by which the reactions can proceed under mild conditions and high yield can be accomplished.
摘要翻译：通式A表示的长春花碱合成中间体（通式A）（式中，R 1，R 2，R 3，和 R 4是独立地选自H，低级烷基，低级烷氧基，卤素，低级全氟烷基，低级烷硫基，羟基，氨基，单 - 或二 - 烷基或酰氨基，低级烷基或芳基磺酰氧基，R 5是H或低级烷基或取代或未取代的芳基，R 6是烷基碳原子数4以下的基团，R 7是取代或未取代的芳基，R 8是取代或未取代的芳基或低级烷基， R 9是酰基或三烷基甲硅烷基。）通过使用硫代苯酰苯胺的自由基形成反应合成通式A的化合物的方法，使用通式B的化合物作为起始原料，合成通过与化合物1的反应和通过2-硝基苯磺酰胺的分子内烷基化形成11元环的通式C的硫代苯胺，可以在温和条件下进行反应并获得高产率。

4. 发明申请

US20060293357A1 Intermediates for synthesis of vinblastine, process for preparation of the intermediates and process for synthesis of vinblastines 失效
标题翻译：用于合成长春花碱的中间体，中间体的制备方法和长春花碱的合成方法
公开(公告)号：US20060293357A1
公开(公告)日：2006-12-28
申请号：US11464560
申请日：2006-08-15
申请人： Tohru Fukuyama , Hidetoshi Tokuyama , Satoshi Yokoshima
发明人： Tohru Fukuyama , Hidetoshi Tokuyama , Satoshi Yokoshima
IPC分类号： C07D487/22 , A61K31/4745
CPC分类号： C07D487/04 , C07D519/04 , C07F7/1804
摘要： An intermediate for vinblastine synthesis represented by general formula A. general formula A. (in the formula, R1, R2, R3 and R4 are the group selected independently from the group consisting of H, lower alkyl group, lower alkoxy group, halogen, lower perfluoroalkyl group, lower alkylthio group, hydroxy group, amino group, mono- or di-alkyl or acylamino group, lower alkyl or arylsulfonyloxy group. R5 is H, or a lower alkyl group or a substituted or non-substituted aryl group, R6 is an alkyl group of carbon number 4 or less, R7 is a substituted or non-substituted aryl group, R8 is a substituted or non-substituted aryl group or lower alkyl group and R9 is an acyl group or trialkylsilyl group.) A method for synthesis of the compound of general formula A utilizing radical ring forming reaction of thioanilides and using the compound of general formula B as the starting material, synthesizing thioanilide of general formula C by the reaction with compound 1 and the formation of a 11-membered ring by intramolecular alkylation of 2-nitrobenzenesulfonamide by which the reactions can proceed under mild conditions and high yield can be accomplished.
摘要翻译：通式A表示的长春花碱合成中间体（通式A）（式中，R 1，R 2，R 3，和 R 4是独立地选自H，低级烷基，低级烷氧基，卤素，低级全氟烷基，低级烷硫基，羟基，氨基，单 - 或二 - 烷基或酰氨基，低级烷基或芳基磺酰氧基，R 5是H或低级烷基或取代或未取代的芳基，R 6是烷基碳原子数4以下的基团，R 7是取代或未取代的芳基，R 8是取代或未取代的芳基或低级烷基， R 9是酰基或三烷基甲硅烷基。）通过使用硫代苯酰苯胺的自由基形成反应合成通式A的化合物的方法，使用通式B的化合物作为起始原料，合成通过与化合物1的反应和通过2-硝基苯磺酰胺的分子内烷基化形成11元环的通式C的硫代苯胺，可以在温和条件下进行反应并获得高产率。

5. 发明授权

US07820838B2 Method for total synthesis of ecteinascidins and intermediate compounds thereof 失效
标题翻译： ecteinascidins及其中间体化合物的全合成方法
公开(公告)号：US07820838B2
公开(公告)日：2010-10-26
申请号：US12178939
申请日：2008-07-24
申请人： Tohru Fukuyama , Toshiyuki Kan
发明人： Tohru Fukuyama , Toshiyuki Kan
IPC分类号： C07D317/54 , C07D405/06 , C07D317/50 , C07D413/04 , C07D241/38
CPC分类号： C07D471/08 , C07C271/22 , C07D317/64 , C07D405/06 , C07D413/04 , Y02P20/55
摘要： An intermediate compound for total synthesis of ecteinascidins comprising, a compound represented by general formula 2 having thioether group at C4 site, and the substituent R2 of N12 site is trichloroethoxycarbonyl (Troc) to which various substituents can be introduced by mild condition, further having 10 members ring structure which can be converted to a ring of other numbered members.
摘要翻译：一种用于全合成海鞘糖苷的中间体化合物，其包含在C4位具有硫醚基的通式2表示的化合物和N12位点的取代基R2是可以通过温和条件引入各种取代基的三氯乙氧基羰基（Troc），进一步具有10 构件环结构可以转换成其他编号的构件的环。

6. 发明申请

US20050043308A1 Process for total synthesis of ecteinascidins and intermediates therefor 失效
标题翻译： ecteinascidins及其中间体的全合成方法
公开(公告)号：US20050043308A1
公开(公告)日：2005-02-24
申请号：US10498367
申请日：2002-09-20
申请人： Tohru Fukuyama , Toshiyuki Kan
发明人： Tohru Fukuyama , Toshiyuki Kan
IPC分类号： C07B61/00 , C07C269/06 , C07C271/22 , C07D317/64 , C07D405/06 , C07D413/04 , C07D451/14 , C07D471/08 , C07D491/22 , C07D493/22 , C07D498/18 , C07D513/22 , C07D515/22 , C07F7/18 , C07D491/14 , A61K31/498
CPC分类号： C07D471/08 , C07C271/22 , C07D317/64 , C07D405/06 , C07D413/04 , Y02P20/55
摘要： An intermediate compound for total synthesis of ecteinascidins comprising, a compound represented by general formula 2 having thioether group at C4 site, and the substituent R2 of N12 site is trichloroethoxicarbonyl (Troc) to which various substituents can be introduced by mild condition, further having 10 members ring structure which can be converted to a ring of other numbered members.
摘要翻译：一种用于全合成电子束丝氨酸的中间体化合物，其包含在C4位具有硫醚基的通式2表示的化合物和N12位点的取代基R2是三氯乙氧羰基（Troc），其中可以通过温和条件引入各种取代基，进一步具有10 构件环结构可以转换成其他编号的构件的环。

7. 发明授权

US4973693A Novel pentacyclic compound and stereoselective synthesis thereof 失效
标题翻译：新型五环化合物及其立体选择性合成
公开(公告)号：US4973693A
公开(公告)日：1990-11-27
申请号：US401746
申请日：1989-09-01
申请人： Shunsuke Goto , Tohru Fukuyama
发明人： Shunsuke Goto , Tohru Fukuyama
IPC分类号： A61K31/535 , A61P31/04 , A61P35/00 , C07D498/22
CPC分类号： C07D498/22
摘要： Novel pentacyclic compounds having antimicrobial and antitumor activity and a process for preparing the same. The pentacyclic compounds are also usefual as intermediates in the production of known tetracyclic antitumor compounds.
摘要翻译：具有抗微生物和抗肿瘤活性的新型五环化合物及其制备方法。五环化合物在生产已知的四环抗肿瘤化合物中也是有用的中间体。

8. 发明授权

US07807833B2 Method for total synthesis of ecteinascidins and intermediate compounds thereof 失效
标题翻译： ecteinascidins及其中间体化合物的全合成方法
公开(公告)号：US07807833B2
公开(公告)日：2010-10-05
申请号：US11740115
申请日：2007-04-25
申请人： Tohru Fukuyama , Toshiyuki Kan
发明人： Tohru Fukuyama , Toshiyuki Kan
IPC分类号： C07D241/38 , C07D405/06 , C07D317/50 , C07D413/04
CPC分类号： C07D471/08 , C07C271/22 , C07D317/64 , C07D405/06 , C07D413/04 , Y02P20/55
摘要： An intermediate compound for total synthesis of ecteinascidins comprising, a compound represented by general formula 2 having thioether group at C4 site, and the substituent R2 of N12 site is trichloroethoxicarbonyl (Troc) to which various substituents can be introduced by mild condition, further having 10 members ring structure which can be converted to a ring of other numbered members.
摘要翻译：一种用于全合成电子束丝氨酸的中间体化合物，其包含在C4位具有硫醚基的通式2表示的化合物和N12位点的取代基R2是三氯乙氧羰基（Troc），其中可以通过温和条件引入各种取代基，进一步具有10 构件环结构可以转换成其他编号的构件的环。

9. 发明申请

US20090270623A1 PROCESS FOR PRODUCTION OF CINNAMIDE DERIVATIVE 审中-公开
标题翻译：生产氰化氢衍生物的方法
公开(公告)号：US20090270623A1
公开(公告)日：2009-10-29
申请号：US12093287
申请日：2006-11-17
申请人： Naoyuki Shimomura , Nobuaki Sato , Toshihiko Kaneko , Mamoru Takaishi , Kazunori Wakasugi , Seiji Yoshikawa , Yoshihiro Nishikawa , Taiju Nakamura , Tohru Fukuyama
发明人： Naoyuki Shimomura , Nobuaki Sato , Toshihiko Kaneko , Mamoru Takaishi , Kazunori Wakasugi , Seiji Yoshikawa , Yoshihiro Nishikawa , Taiju Nakamura , Tohru Fukuyama
IPC分类号： C07F9/59 , C07D401/10 , C07D211/76
CPC分类号： C07D401/10
摘要： A compound (8) represented by the formula: (8) wherein R1 represents a 6- to 14-membered aromatic hydrocarbon ring group which may have a substituent; and n represents 0 to 2, can be produced with good efficiency by reacting a compound (3) represented by the formula: (3) wherein R1 and n are as defined above; and Q represents a single bond or —CH(Y)— where Y represents a hydrogen atom or a C1-6 alkyl group] with 3-methoxy-4-(4-methyl-1H-imidazol-1-yl)benzaldehyde in the presence of a base.
摘要翻译：由式（8）表示的化合物（8）：其中R1表示可具有取代基的6至14元芳族烃环基团; n表示0〜2，可以通过使式（3）表示的化合物（3）（其中R 1和n如上所定义）反应而得到良好的效率。和Q表示单键或-CH（Y） - ，其中Y表示氢原子或C 1-6烷基]与3-甲氧基-4-（4-甲基-1H-咪唑-1-基）苯甲醛在存在基地

10. 发明授权

US07417145B2 Process for total synthesis of ecteinascidins and intermediates therefor 失效
标题翻译： ecteinascidins及其中间体的全合成方法
公开(公告)号：US07417145B2
公开(公告)日：2008-08-26
申请号：US10498367
申请日：2002-09-20
申请人： Tohru Fukuyama , Toshiyuki Kan
发明人： Tohru Fukuyama , Toshiyuki Kan
IPC分类号： C07D241/36 , C07D405/06 , C07D317/50 , C07D413/04
CPC分类号： C07D471/08 , C07C271/22 , C07D317/64 , C07D405/06 , C07D413/04 , Y02P20/55
摘要： An intermediate compound for total synthesis of ecteinascidins comprising, a compound represented by general formula 2 having thioether group at C4 site, and the substituent R2 of N12 site is trichloroethoxicarbonyl (Troc) to which various substituents can be introduced by mild condition, further having a 10-membered ring structure which can be converted to a ring of other numbered members.
摘要翻译：一种用于全合成海鞘糖苷的中间体化合物，其包含在C4位具有硫醚基的通式2表示的化合物和N 12 12位的取代基R 2 2是三氯乙氧羰基（ Troc），其中可以通过温和条件引入各种取代基，进一步具有可被转化成其它编号的成员的环的10元环结构。

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