公开(公告)号：US5079382A

公开(公告)日：1992-01-07

申请号：US617345

申请日：1990-11-23

申请人： Naoaki Taoka ,  Kenji Inoue ,  Shigeo Hayashi ,  Noboru Ueyama ,  Satomi Takahashi

发明人： Naoaki Taoka ,  Kenji Inoue ,  Shigeo Hayashi ,  Noboru Ueyama ,  Satomi Takahashi

IPC分类号： C07C303/30 ,  C07C309/65 ,  C07C309/66 ,  C07C309/73 ,  C07D303/40

CPC分类号： C07D303/40 ,  C07C309/65 ,  C07C309/73

摘要： A 3,4-epoxybutyrate of the formula: ##STR1## wherein R.sup.1 is an alkyl or aralkyl group is efficiently prepared by a process comprising steps of:(a) reacting 3,4-dihydroxybutyronitrile of the formula: ##STR2## with a sulfonyl chloride of the formula: R.sup.2 --SO.sub.2 --Cl wherein R.sup.2 is an alkyl group or a phenyl group which may be substituted in the presence of a base to obtain a compound of the formula: ##STR3## (b) reacting the compound prepared in the step (a) with an alcohol of the formula: R.sup.1 --OH in the presence of an acid to obtain a compound of the formula: ##STR4## and (c) reacting the compound prepared in the step (b) with a base to obtain the 3,4-epoxybutyrate.

公开(公告)号：US5179212A

公开(公告)日：1993-01-12

申请号：US619974

申请日：1990-11-30

申请人： Satomi Takahashi ,  Shigeo Hayashi ,  Naoaki Taoka ,  Noboru Ueyama

发明人： Satomi Takahashi ,  Shigeo Hayashi ,  Naoaki Taoka ,  Noboru Ueyama

IPC分类号： B01J23/40 ,  B01J25/00 ,  C07B61/00 ,  C07C303/30 ,  C07C309/06 ,  C07C309/65 ,  C07C309/66 ,  C07C309/73 ,  C07D207/12

CPC分类号： C07D207/12 ,  C07C309/06 ,  C07C309/66 ,  C07C309/73

摘要： 3-Pyrrolidinol or its salt is economically produced by cyclizing an aminobutanol derivative of the formula: ##STR1## wherein R is an alkyl or a substituted or unsubstituted phenyl group, or its salt.

公开(公告)号：US5214197A

公开(公告)日：1993-05-25

申请号：US724728

申请日：1991-07-02

申请人： Shigeo Hayashi ,  Noboru Ueyama ,  Kenji Inoue ,  Teruyoshi Koga ,  Satomi Takahashi

发明人： Shigeo Hayashi ,  Noboru Ueyama ,  Kenji Inoue ,  Teruyoshi Koga ,  Satomi Takahashi

IPC分类号： C07C69/675 ,  C07C69/738

CPC分类号： C07C69/738 ,  C07C69/675 ,  Y02P20/55

摘要： A novel 2,4-dihydroxyadipic acid derivative of the formula: ##STR1## wherein R.sup.1 and R.sup.4 are the same or different and each a hydrogen atom, an alkyl group, an aralkyl group, an aryl group or a silyl group, and R.sup.2 and R.sup.3 are the same or different and each a hydrogen atom or a protective group of a hydroxy group or together form a ring, which is useful as a common intermediate in the synthesis of HMG-CoA reductase inhibitor.

公开(公告)号：US5214199A

公开(公告)日：1993-05-25

申请号：US755496

申请日：1991-08-30

申请人： Teruyoshi Koga ,  Noboru Ueyama ,  Kenji Inoue ,  Satomi Takahashi

发明人： Teruyoshi Koga ,  Noboru Ueyama ,  Kenji Inoue ,  Satomi Takahashi

IPC分类号： B01J31/02 ,  C07B61/00 ,  C07C67/08 ,  C07C67/287 ,  C07C69/38 ,  C07C69/635

CPC分类号： C07C67/08

摘要： A malonic monoester is prepared in a good yield by a single step reaction by reacting malonic acid with an alcohol in the presence of a base and an activator of malonic acid selected from the group consisting of an acyl halide or halocarbonate and an acid anhydride or dicarbonate.

公开(公告)号：US4983759A

公开(公告)日：1991-01-08

申请号：US452470

申请日：1989-12-20

申请人： Kenji Inoue ,  Satomi Takahashi ,  Keiichi Yonetsu ,  Noboru Ueyama

发明人： Kenji Inoue ,  Satomi Takahashi ,  Keiichi Yonetsu ,  Noboru Ueyama

IPC分类号： B01J23/06 ,  B01J23/80 ,  C07B61/00 ,  C07C67/317 ,  C07C67/343 ,  C07C69/675 ,  C07C69/708 ,  C07C69/716 ,  C07C69/78 ,  C07C255/13 ,  C07C255/14 ,  C07D317/30 ,  C07D319/06 ,  C07D319/08 ,  C07F7/18

CPC分类号： C07D319/08 ,  C07C255/13 ,  C07C255/14 ,  C07D317/30 ,  C07D319/06 ,  Y02P20/55

摘要： A compound of a 3,5,6-trihydroxyhexanoic acid derivative of the formula: ##STR1## wherein P.sup.1 and P.sup.2 are independently hydrogen atoms or hydroxy-protecting groups, or together form a ring, and R is an alkyl group is effectively prepared by a process comprising steps of:reacting a butyronitrile derivative of the formula: ##STR2## wherein P.sup.1 and P.sup.2 are the same as defined above with an .alpha.-haloacetate of the formula:X--CH.sub.2 --COOR (III) wherein X is a halogen atom, and R is the same as defined above in the presence of a metallic catalyst selected from the group consisting zinc and zinc-copper to form a keto acid derivative of the formula: ##STR3## wherein P.sup.1, P.sup.2 and R are the same as defined above, and then reducing the obtained keto-acid derivative of the formula (IV).

公开(公告)号：US5565345A

公开(公告)日：1996-10-15

申请号：US380334

申请日：1995-01-30

申请人： Yoshihiko Yasohara ,  Yoshiko Tari ,  Noboru Ueyama ,  Junzo Hasegawa ,  Satomi Takahashi

发明人： Yoshihiko Yasohara ,  Yoshiko Tari ,  Noboru Ueyama ,  Junzo Hasegawa ,  Satomi Takahashi

IPC分类号： A61K31/35 ,  A61P27/02 ,  A61P27/06 ,  C07D495/04 ,  C12P17/18 ,  C12P41/00 ,  C12R1/645 ,  C12R1/72 ,  C12R1/74 ,  C12R1/78 ,  C12R1/84 ,  C12R1/85 ,  C12R1/865 ,  C12P11/00 ,  C07D409/04 ,  C12P17/00

CPC分类号： C07D495/04 ,  C12P17/185 ,  C12P41/002

摘要： A process for preparing 5,6-dihydro-4-hydroxy-(S)-6-methyl-thieno[2,3-b]thiopyran-7,7-dioxide having the formula (II): ##STR1## which comprises subjecting 5,6-dihydro-4-oxo-(S)-6-methyl-thieno[2,3-b]thiopyran-7,7-dioxide having the formula (I): ##STR2## to the action of a microorganism to reduce the thienothiopyran derivative having the formula (I), and collecting 5,6-dihydro-4-hydroxy-(S)-6-methyl-thieno-[2,3-b]thiopyran-7,7-dioxide having the formula (II) from the reaction mixture, wherein said microorganism belongs to the genus selected from the group consisting of Ambrosiozyma, Arthroascus, Ashbya, Candida, Cryptococcus, Hansenula, Kluyveromyces, Lipomyces, Lodderomyces, Metschnikowia, Pachysolen, Pichia, Rhodosporidium, Rhodotorula, Saccharomyces, Saccharomycopsis, Schwanniomyces, Sporidiobolus, Spolobolomyces, Stephanoascus, Trigonopsis, Trichosporon and Wingea, according to which, a simple and effective. process for preparing 5,6-dihydro-4-hydroxy-(S)-6-methyl-thieno-[2,3-b]thiopyran-7,7-dioxide.

摘要翻译： 具有式（II）的5,6-二氢-4-羟基 - （S）-6-甲基 - 噻吩并[2,3-b]噻喃-7,7-二氧化物的制备方法： 其包括将具有式（I）的5,6-二氢-4-氧代 - （S）-6-甲基 - 噻吩并[2,3-b]噻喃-7,7-二氧化物：（I） 微生物降低具有式（I）的噻吩并吡喃衍生物的作用，并收集5,6-二氢-4-羟基 - （S）-6-甲基 - 噻吩并[2,3-b]噻喃-7， 其中所述微生物属于选自Ambrosiozyma，Arthroascus，Ashbya，Candida，Cryptococcus，Hansenula，Kluyveromyces，Lipomyces，Lodderomyces，Metschnikowia，Pachysolen，Pichia ，Rhodosporidium，Rhodotorula，Saccharomyces，Saccharomycopsis，Schwanniomyces，Sporidiobolus，Spolobolomyces，Stephanoascus，Trigonopsis，Trichosporon和Wingea，据此，一个简单有效的。 制备5,6-二氢-4-羟基 - （S）-6-甲基 - 噻吩并[2,3-b]噻喃-7,7-二氧化物的方法。

公开(公告)号：US4716235A

公开(公告)日：1987-12-29

申请号：US900051

申请日：1986-08-25

申请人： Satomi Takahashi ,  Kenji Inoue ,  Yoshifumi Yanagida ,  Takehisa Ohashi ,  Kiyoshi Watanabe

发明人： Satomi Takahashi ,  Kenji Inoue ,  Yoshifumi Yanagida ,  Takehisa Ohashi ,  Kiyoshi Watanabe

IPC分类号： C07K14/81 ,  C07D207/16 ,  C07K1/02 ,  C07K5/02 ,  C07K5/06 ,  C07K14/435 ,  C07D207/09

CPC分类号： C07K5/0222

摘要： A process for preparing N-[1(S)-ethoxycarbonyl-3-phenylpropyl]-L-alanyl-L-proline, which comprises reacting N-carboxyanhydride of N-[1(S)-ethoxycarbonyl-3-phenylpropyl]-L-alanine with L-proline in the presence of a base. According to the process, enalapril can be prepared economically, easily and effectively.

摘要翻译： 制备N- [1（S） - 乙氧基羰基-3-苯丙基] -L-丙氨酰-L-脯氨酸的方法，其包括使N- [1（S） - 乙氧基羰基-3-苯基丙基] -L-脯氨酸的N-羧酸酐 - 丙氨酸与L-脯氨酸在碱的存在下。 根据该过程，依那普利可以经济，容易和有效地制备。

公开(公告)号：US5227497A

公开(公告)日：1993-07-13

申请号：US810082

申请日：1991-12-19

申请人： Kenji Inoue ,  Satomi Takahashi

发明人： Kenji Inoue ,  Satomi Takahashi

IPC分类号： C07C237/20 ,  C07C255/42 ,  C07K5/062

CPC分类号： C07K5/06086 ,  C07C237/20 ,  C07C255/42

摘要： A process for producing N.sup.2 -(1-(S)-carboxy-3-phenylpropyl)-L-lysil-L-proline of formula (VIII); ##STR1## N.sup.2 -(1-substituted-3-phenylpropyl)-L-lysil-L-proline derivative of formula (VII); ##STR2## and N.sup.2 -(1-carbonyl-3-phenylpropyl)-L-lysil-L-proline derivative of formula (XXVI); ##STR3## is disclosed.

摘要翻译： 制备式（VIII）的N 2 - （1-（S） - 羧基-3-苯基丙基）-L-赖氨酰-L-脯氨酸的方法; （VIII）式（VII）的N 2 - （1-取代-3-苯基丙基）-L-裂解物-L-脯氨酸衍生物; （VII）和式（XXVI）的N 2 - （1-羰基-3-苯基丙基）-L-赖氨酰-L-脯氨酸衍生物; （XXVI）被披露。

公开(公告)号：US4925969A

公开(公告)日：1990-05-15

申请号：US324497

申请日：1989-03-16

申请人： Satomi Takahashi ,  Yasuyoshi Ueda ,  Kazuhiko Yamada ,  Yukio Yamada ,  Takehiko Yamane ,  Yoshifumi Yanagita ,  Yoshio Shimada ,  Kiyoshi Watanabe ,  Michio Nomura ,  Takehisa Ohashi ,  Kenji Inoue

发明人： Satomi Takahashi ,  Yasuyoshi Ueda ,  Kazuhiko Yamada ,  Yukio Yamada ,  Takehiko Yamane ,  Yoshifumi Yanagita ,  Yoshio Shimada ,  Kiyoshi Watanabe ,  Michio Nomura ,  Takehisa Ohashi ,  Kenji Inoue

IPC分类号： C07C227/08 ,  C07C233/46 ,  C07C271/06

CPC分类号： C07C233/46 ,  C07C227/08 ,  C07C271/06

摘要： Ethyl-.beta.-benzoyacrylate is reacted with an alkali metal salt of (S)-alanine or an alkali metal salt of N.sup.6 -trifluoroacetyl-L-lysine to form the corresponding Michael addition product, and not less than an equivalent amount of acid is added after completion of the Michael addition to prevent conversion of the (S,S) form of the product to the (R,S) form.

摘要翻译： 乙基-β-苯甲酸酯与（S） - 丙氨酸的碱金属盐或N6-三氟乙酰基-L-赖氨酸的碱金属盐反应形成相应的迈克尔加成产物，加入不少于等量的酸 完成迈克尔加成以防止（S，S）形式的产物转化为（R，S）形式。

公开(公告)号：US4910320A

公开(公告)日：1990-03-20

申请号：US369164

申请日：1989-06-21

申请人： Kenji Inoue ,  Hidetoshi Kutsuki ,  Junzo Hasegawa ,  Satomi Takahashi

发明人： Kenji Inoue ,  Hidetoshi Kutsuki ,  Junzo Hasegawa ,  Satomi Takahashi

IPC分类号： B01J23/40 ,  B01J25/02 ,  C07B61/00 ,  C07D207/12

CPC分类号： C07D207/12

摘要： A process for preparing 3-pyrrolidinol having the formula (II): ##STR1## or a salt thereof, which comprises reducing 4-chloro-3-hydroxybutyronitrile having the formula (I): ##STR2## to convert said 4-chloro-3-hydroxybutyronitrile (I) into said 3-pyrrolidinol (II). According to the present invention, 3-pyrrolidinol, particularly optically active 3-pyrrolidinol can be prepared economically and efficiently.