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131. 发明授权

US5322939A Process for preparing azetidin-2-one derivatives 失效
标题翻译：制备氮杂环丁-2-酮衍生物的方法
公开(公告)号：US5322939A
公开(公告)日：1994-06-21
申请号：US909678
申请日：1992-07-07
申请人： Tadakatsu Mandai , Jiro Tsuji
发明人： Tadakatsu Mandai , Jiro Tsuji
IPC分类号： B01J31/18 , C07B61/00 , C07D205/08 , C07D205/10 , C07B43/06
CPC分类号： C07D205/08 , C07D205/10 , Y02P20/55
摘要： A process for preparing an azetidin-2-one derivative represented by formula (2): ##STR1## wherein R.sup.4 and R.sup.5, which may be the same or different, each represents a hydrogen atom, an alkyl group having from 1 to 8 carbon atoms, or an alkyl group having from 1 to 8 carbon atoms substituted with an alkoxy group, an acyl group, or an alkoxycarbonyl group; R.sup.6 represents a protective group for an amino group; and R.sup.7 represents a vinylidene group of formula ##STR2## or an acetylene group of formula ##STR3## wherein R.sup.2 and R.sup.3, which may be the same or different, each represents a hydrogen atom or an alkyl group having from 1 to 8 carbon atoms; and R.sup.8 represents an alkyl group having from 1 to 8 carbon atoms corresponding to R.sup.2 or R.sup.3, which comprises reacting a propargyl alcohol derivative represented by formula (1): ##STR4## wherein R.sup.1 represents an alkyl group having from 1 to 6 carbon atoms, a phenyl group, or a halogen-substituted phenyl group; R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are as defined above, with carbon monoxide in the presence of a palladium complex. The compound (2), an intermediate of penem antibiotics, can be obtained through one reaction step in good yield.
摘要翻译：制备由式（2）表示的氮杂环丁-2-酮衍生物的方法：其中R 4和R 5可以相同或不同，各自表示氢原子，具有1〜 8个碳原子或具有1至8个碳原子被烷氧基，酰基或烷氧基羰基取代的烷基; R6表示氨基的保护基; 并且R 7表示式“IMAGE”的亚乙烯基或式“IMAGE”的乙炔基，其中R 2和R 3可以相同或不同，各自表示氢原子或具有1至8个碳原子的烷基; R8代表对应于R2或R3的具有1至8个碳原子的烷基，其包括使由式（1）表示的炔丙醇衍生物：其中R 1表示具有1至6个碳原子的烷基碳原子，苯基或卤素取代的苯基; R2，R3，R4，R5，R6和R7如上定义，与钯络合物存在下的一氧化碳。化合物（2）是penin抗生素的中间体，可以通过一个反应步骤以良好的产率获得。

132. 发明授权

US5286883A (3R,5S)-3,5,6-trihydroxyhexanoic acid derivative and production method thereof 失效
标题翻译：（3R，5S）-3,5,6-三羟基己酸衍生物及其制备方法
公开(公告)号：US5286883A
公开(公告)日：1994-02-15
申请号：US976498
申请日：1992-11-13
申请人： Kazutoshi Sakurai , Shigeru Mitsuhashi , Hidenori Kumobayashi
发明人： Kazutoshi Sakurai , Shigeru Mitsuhashi , Hidenori Kumobayashi
IPC分类号： B01J31/24 , C07B53/00 , C07B61/00 , C07D309/12 , C07D319/06
CPC分类号： C07D319/06 , C07D309/12
摘要： A (3R,5S)-3,5,6-trihydroxyhexanoic acid derivative and a process of producing the (3R,5S)-3,5,6-trihydroxyhexanoic acid derivative which comprises the step of enantioselectively hydrogenating an (S)-5,6-dihydroxy-3-oxohexanoic acid derivative with a specific ruthenium-optically active phosphine complex represented as a catalyst are disclosed. The (3R,5S)-3,5,6-trihydroxyhexanoic acid derivative which is a useful compound capable of being easily converted into a lactone moiety, which is the active part of an inhibitor on HMG-CoA reductase, can be easily and efficiently obtained under a mild reaction condition with a high selectivity for the syn-diol form.
摘要翻译： A（3R，5S）-3,5,6-三羟基己酸衍生物和（3R，5S）-3,5,6-三羟基己酸衍生物的制备方法，其包括以下步骤：对（S）-5 公开了以表示为催化剂的特定钌光学活性膦配合物的6-二羟基-3-氧代己酸衍生物。作为HMG-CoA还原酶抑制剂的活性成分的能够容易地转化为内酯部分的有用化合物的（3R，5S）-3,5,6-三羟基己酸衍生物可以容易且有效地在温和的反应条件下以对顺式二醇形式的高选择性获得。

133. 发明授权

US5210315A Process for producing .alpha.-hydroxyketones 失效
标题翻译：生产（ALPHA） - 羟基酮的方法
公开(公告)号：US5210315A
公开(公告)日：1993-05-11
申请号：US779529
申请日：1991-10-18
申请人： Takao Saito , Hidenori Kumobayashi , Shunichi Murahashi
发明人： Takao Saito , Hidenori Kumobayashi , Shunichi Murahashi
IPC分类号： C07C45/28 , C07C45/30 , C07C49/245 , C07C49/337 , C07C49/493 , C07C49/497 , C07C49/503 , C07C49/713 , C07C49/747 , C07C49/82 , C07C67/29 , C07C67/313 , C07D303/16 , C07J9/00 , C07J71/00
CPC分类号： C07J71/001 , C07C45/28 , C07C45/30 , C07C49/245 , C07C49/337 , C07C49/493 , C07C49/497 , C07C49/503 , C07C49/713 , C07C49/747 , C07C49/82 , C07C67/29 , C07C67/313 , C07D303/16 , C07J9/00
摘要： A process for producing an .alpha.-hydroxyketone represented by formula (I): ##STR1## wherein R.sup.1 represents a substituted or unsubstituted alkyl group, a substituted or unsubstituted aralkyl group, or an alkoxycarbonyl group; and R.sup.2 and R.sup.3 each represent a hydrogen atom, a substituted or unsubstituted alkyl group, or a substituted or unsubstituted aralkyl group, provided that they do not simultaneously represent a hydrogen atom; or a pair of R.sup.1 and R.sup.2, a pair of R.sup.1 and R.sup.3, or a pair of R.sup.2 and R.sup.3 is taken together to form a ring; and the pair of R.sup.1 and R.sup.2 and the pair of R.sup.2 and R.sup.3 may form a ring simultaneously, is disclosed, comprising reacting a compound represented by formula (II): ##STR2## wherein R.sup.1, R.sup.2, and R.sup.3 are as defined above, with an oxidizing agent in the presence of a ruthenium compound and water. .alpha.-Hydroxyketones useful as physiologically active substances are produced with good selectivity and in high yield.

134. 发明授权

US5200429A Acne vulgaris treating 失效
标题翻译：寻常痤疮治疗
公开(公告)号：US5200429A
公开(公告)日：1993-04-06
申请号：US765739
申请日：1991-09-26
申请人： Toshiya Sato , Satoko Tsukada , Hamako Hata , Kenya Ishida
发明人： Toshiya Sato , Satoko Tsukada , Hamako Hata , Kenya Ishida
IPC分类号： A61K8/30 , A61K8/00 , A61K31/015 , A61K36/00 , A61P17/00 , A61Q19/00 , C07C13/32 , C07C13/605
CPC分类号： A61K31/015 , Y10S514/859
摘要： An acne vulgaris treating and preventing topica, which comprises, as an active ingredient, at least one compound selected from the group consisting of caryophyllene, cedrene, longifolene and thujopsene. The topica exhibits sufficient inhibitory activity on proliferation of Propionibacterium acnes, a pathogenic bacterium causing acne vulgaris, at a small therapeutic dose without causing skin irritation.
摘要翻译：一种寻常痤疮治疗和预防痤疮，其包含作为活性成分的至少一种选自以下的化合物：石竹烯，雪松烯，长叶烯和thujopsene。对于痤疮丙酸杆菌（Acionibacterium acnes）的致病菌，对痤疮丙酸杆菌的增殖具有足够的抑制作用，这种痤疮是导致寻常痤疮的致病菌，治疗剂量小，不引起皮肤刺激。

135. 发明授权

US5198562A Ruthenium-phosphine complex and intermediate for producing the same 失效
标题翻译：二氢卟吩复合物及其生产中间体
公开(公告)号：US5198562A
公开(公告)日：1993-03-30
申请号：US739022
申请日：1991-08-01
申请人： Ryoji Noyori , Masato Kitamura , Noboru Sayo , Hidenori Kumobayashi , Martin F. Giles
发明人： Ryoji Noyori , Masato Kitamura , Noboru Sayo , Hidenori Kumobayashi , Martin F. Giles
IPC分类号： B01J31/24 , C07B53/00 , C07B61/00 , C07C67/31 , C07C69/675 , C07F15/00
CPC分类号： B01J31/2404 , B01J31/2452 , C07C67/31 , C07F15/0053 , B01J2231/643 , B01J2531/821 , B01J31/1805
摘要： A ruthenium-phosphine complex represented by formula (I): ##STR1## wherein R.sup.2 -BINAP represents a teritary phosphine compound represented by formula (II): ##STR2## wherein R.sup.2 represents a hydrogen atom, a methyl group, a methoxy group, or a t-butyl group; X represents a halogen atom; and R and R.sup.1, which may be the same or different, each represent a phenyl group or a substituted phenyl group, and a ruthenium-phosphine complex represented by formula (III): ##STR3## wherein R and R.sup.1 are as defined above; and dma represents N,N-dimethylacetamide, which is an intermediate for synthesizing the ruthenium-phosphine complex of formula (I), are disclosed. The complex of formula (I) is useful as a catalyst for general syntheses with its ligand being an optically inactive compound or for asymmetric syntheses with its ligand being an optically active compound and, also, can be prepared at a low cost.

136. 发明授权

US5144042A Process for preparing optically active 3-hydroxypyrrolidine derivatives 失效
标题翻译：制备光学活性3-羟基吡咯烷衍生物的方法
公开(公告)号：US5144042A
公开(公告)日：1992-09-01
申请号：US682273
申请日：1991-04-09
申请人： Nobuo Seido , Yoshiki Okeda , Hidenori Kumobayashi
发明人： Nobuo Seido , Yoshiki Okeda , Hidenori Kumobayashi
IPC分类号： C07B53/00 , C07C31/34 , C07C211/27 , C07C309/65 , C07C309/73 , C07D207/12
CPC分类号： C07D207/12
摘要： A process for preparing optically active 3-hydroxypyrrolidine derivatives useful as intermediates represented by formula (III): ##STR1## wherein Q represents a substituted or unsubstituted phenyl group; and * indicates an asymmetric carbon atom, comprising reacting an optically active 4-halo-3-hydroxybutane derivative represented by formula (I): ##STR2## wherein * is as defined above; R.sup.1 represents a lower alkyl group or a substituted or unsubstituted phenyl group; and X represents a halogen atom, with a benzylamine derivative represented by formula (II):H.sub.2 NCH.sub.2 Q (II)wherein Q is as defined above, is disclosed. The starting compound (I) is easily available through chemical synthesis. Any complicated procedure or use of an expensive reagent is not required.

137. 发明授权

US5141921A Perfume composition 失效
标题翻译：香水组成
公开(公告)号：US5141921A
公开(公告)日：1992-08-25
申请号：US683911
申请日：1991-04-11
申请人： Kiyohito Sawano , Kenya Ishida , Akemi Shimada
发明人： Kiyohito Sawano , Kenya Ishida , Akemi Shimada
IPC分类号： A61K8/36 , A61Q13/00 , C07C57/03 , C11B9/00
CPC分类号： A61Q13/00 , A61K8/361 , C07C57/03 , C11B9/0019 , A61K2800/70
摘要： A perfume composition containing 3-methyl-2-hexenoic acid and/or 7-octenoic acid is disclosed. The perfume composition has a fresh and natural animal note and excellent diffusibility and tastiness. The perfume composition produces psychological effects on humans, such as an awakening effect and/or a sedative effect.
摘要翻译：公开了含有3-甲基-2-己烯酸和/或7-辛烯酸的香料组合物。香水组合物具有清新自然的动物笔记，具有优异的扩散性和口感性。香水组合物对人类产生心理影响，例如觉醒作用和/或镇静作用。

138. 发明授权

US5081310A Process for preparing optically active ketones 失效
标题翻译：制备光学活性酮的方法
公开(公告)号：US5081310A
公开(公告)日：1992-01-14
申请号：US553285
申请日：1990-07-17
申请人： Nobuo Seido , Hidenori Kumobayashi
发明人： Nobuo Seido , Hidenori Kumobayashi
IPC分类号： B01J31/24 , C07B61/00 , C07C45/62 , C07C49/395 , C07C49/403
CPC分类号： C07C49/395 , C07C45/62 , C07C49/403
摘要： A process for preparing an optically active ketone represented by formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom or an alkyl group having from 1 to 5 carbon atoms; and n represents 1 or 2,which comprises asymmetrically hydrogenating an .alpha., .beta.-unsaturated ketone represented by formula (II): ##STR2## wherein R.sup.1 and n are as defined above, in the presence of a ruthenium-optically active phosphine complex as a catalyst. An optically active ketone having a high optical purity can be prepared.

139. 发明授权

US4994602A Process for preparing optically active 6-t-butyoxy-3,5-dihydroxyhexanoic esters 失效
标题翻译：光学活性6-叔丁氧基-3,5-二羟基己酸酯的制备方法
公开(公告)号：US4994602A
公开(公告)日：1991-02-19
申请号：US485692
申请日：1990-02-27
申请人： Nobuo Seido , Noboru Sayo , Hidenori Kumobayashi
发明人： Nobuo Seido , Noboru Sayo , Hidenori Kumobayashi
IPC分类号： C07C67/31 , C07C69/708
CPC分类号： C07C67/31 , C07C69/708
摘要： A process for preparing an optically active 6-t-butoxy-3,5-dihydroxyhexanoic ester represented by formula: ##STR1## wherein t-Bu represents a t-butyl group; and R.sup.4 represents a lower alkyl group, which is useful as a precursor of a lactone moiety of campactin, mevinolin or analogues thereof is disclosed, comprising asymmetrically hydrogenating a 4-t-butoxyacetoacetic ester in the presence of a ruthenium-optically active phosphine complex to obtain an optically active 4-t-butyoxy-3-hydroxybutanoic ester, reacting the ester with a lithium enolate of an acetic ester to obtain an optically active 6-t-butyoxy-5-hydroxy-3-oxohexanoic ester, and asymmetrically hydrogenating the resulting ester in the presence of a ruthenium-optically active phosphine complex as a catalyst. The desired product can be obtained in good yield at high stereoselectivity.

140. 发明授权

US4933482A Process for preparing optically active alcohol 失效
标题翻译：光学活性醇的制备方法
公开(公告)号：US4933482A
公开(公告)日：1990-06-12
申请号：US204480
申请日：1988-06-09
申请人： Noboru Sayo , Takao Saito , Hidenori Kumobayashi , Susumu Akutagawa , Ryoji Noyori , Hidemasa Takaya
发明人： Noboru Sayo , Takao Saito , Hidenori Kumobayashi , Susumu Akutagawa , Ryoji Noyori , Hidemasa Takaya
IPC分类号： C07C67/303 , B01J31/24 , C07B31/00 , C07B53/00 , C07B61/00 , C07C67/00 , C07C67/31 , C07C69/675 , C07C69/757 , C07C227/00 , C07C227/16 , C07C227/32 , C07C229/22 , C07C229/24 , C07C231/00 , C07C231/12 , C07C231/18 , C07C235/06 , C07C235/34 , C07C237/06 , C07C325/00 , C07C327/22
CPC分类号： C07C227/32 , C07C323/00
摘要： A process for preparing an optically active alcohol is disclosed, which comprises asymmetrically hydrogenating a .beta.-keto acid derivative in the presence of a ruthenium-optically active phosphine complex as a catalyst. The resulting alcohol has high optical purity.

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