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1. 发明授权

US4325886A Optical resolution of acylthiopropionic acid 失效
标题翻译：酰基硫代丙酸的光学拆分
公开(公告)号：US4325886A
公开(公告)日：1982-04-20
申请号：US209680
申请日：1980-11-24
申请人： Naohito Ohashi , Hiroyuki Mizote , Isamu Maruyama , Shoji Nagata , Kikuo Ishizumi , Junki Katsube
发明人： Naohito Ohashi , Hiroyuki Mizote , Isamu Maruyama , Shoji Nagata , Kikuo Ishizumi , Junki Katsube
IPC分类号： C07C319/28 , C07C67/00 , C07C313/00 , C07C323/52 , C07C325/00 , C07C327/20 , C07C327/32 , C07C153/07 , C07C153/09
CPC分类号： C07C327/00
摘要： A process for the optical resolution of DL-.alpha.-methyl-.beta.-acylthiopropionic acid, which comprises contacting a DL-.alpha.-methyl-.beta.-acylthiopropionic acid of the formula, ##STR1## wherein R.sub.1 is acetyl or benzoyl which may be substituted with a C.sub.1 -C.sub.3 alkyl or a halogen atom, with an optically active amine of the formula, ##STR2## wherein R.sub.2 is methyl, isopropyl or isobutyl, to form diastereoisomeric salts, subjecting the formed diastereoisomeric salts to the fractional crystallization in a solvent to separate the D-acid salt from the L-acid salt, and then contacting the individual diastereoisomeric salt with acid to give D-.alpha.-methyl-.beta.-acylthiopropionic acid and L-.alpha.-methyl-.beta.-acylthiopropionic acid, the former being useful as an intermediate for synthesizing captopril useful as an antihypertensive agent.
摘要翻译：用于DL-α-甲基-β-酰基硫代丙酸的光学拆分的方法，其包括使下式的DL-α-甲基-β-酰基硫代丙酸：其中R 1是乙酰基或可以被 C 1 -C 3烷基或卤素原子，与下式的光学活性胺，其中R 2是甲基，异丙基或异丁基，形成非对映异构盐，使形成的非对映异构体盐在溶剂中进行分级结晶以分离来自L-酸盐的D-酸盐，然后将各个非对映异构体盐与酸接触，得到D-α-甲基-β-酰基硫代丙酸和L-α-甲基-β-酰基硫代丙酸，前者可用作用作合成用作抗高血压药的卡托普利的中间体。

2. 发明授权

US4241070A Analgesic benzomorphan derivatives 失效
标题翻译：镇痛苯并吗啉衍生物
公开(公告)号：US4241070A
公开(公告)日：1980-12-23
申请号：US736072
申请日：1976-10-27
申请人： Junki Katsube , Hiroyuki Mizote , Shuichi Harada , Hisao Yamamoto
发明人： Junki Katsube , Hiroyuki Mizote , Shuichi Harada , Hisao Yamamoto
IPC分类号： A61K31/435 , A61P25/04 , C07D221/26 , A61K31/445
CPC分类号： C07D221/26 , Y02P20/55
摘要： 2-Substituted-2'-methyl-6,7-benzomorphan derivatives of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen or C.sub.1 -C.sub.3 alkyl; and R.sub.3 is hydrogen, halogen or C.sub.1 -C.sub.3 alkyl, and pharmaceutically acceptable salts thereof, which are useful as non-addicting analgesics with sedative effects, are prepared by the reaction of a 6,7-benzomorphan derivative of the formula: ##STR2## wherein R.sub.1 and R.sub.2 are as defined above, with a reactive derivative of an alcohol compound of the formula: ##STR3## wherein X is an optionally protected carbonyl group; and R.sub.3 is as defined above, optionally followed by the elimination of the protective group of the carbonyl group, or by the oxidation of a 6,7-benzomorphan derivative of the formula: ##STR4## wherein R.sub.1, R.sub.2 and R.sub.3 are as defined above.
摘要翻译：具有下式的2-取代的-2'-甲基-6,7-苯并吗啉衍生物：其中R 1和R 2各自为氢或C 1 -C 3烷基; 并且R3是氢，卤素或C1-C3烷基及其药学上可接受的盐，其可用作具有镇静作用的非上瘾止痛剂，通过下式的6,7-苯并吗啉衍生物的反应制备： [II]其中R1和R2如上所定义，与下式的醇化合物的反应性衍生物：其中X是任选被保护的羰基; 并且R 3如上所定义，任选地随后消除羰基的保护基，或通过下式的6,7-苯并吗啉衍生物的氧化：其中R 1，R 2和R 3是如上所述。

3. 发明授权

US3966939A Novel 2-substituted 6,7-benzomorphan derivatives and salts thereof in analgesic compositions 失效
标题翻译：新颖的2-取代的6,7-苯并恶嗪衍生物及其盐在止痛组合物中
公开(公告)号：US3966939A
公开(公告)日：1976-06-29
申请号：US558655
申请日：1975-03-17
申请人： Kenji Kobayashi , Toshitsugu Fukumaru , Hiroyuki Mizote , Shigeho Inaba , Hisao Yamamoto
发明人： Kenji Kobayashi , Toshitsugu Fukumaru , Hiroyuki Mizote , Shigeho Inaba , Hisao Yamamoto
IPC分类号： A61K31/395 , A61K31/485
CPC分类号： A61K31/395
摘要： Novel 2-substituted 6,7-benzomorphan derivatives of the formula: ##SPC1##And acid addition salts thereof, which are useful as non-addicting analgesics, pain relieving agents and antitussives and can be prepared by reacting 6,7-benzomorphan derivatives of the formula: ##SPC2##With the reactive derivatives of alcohols of the formula: ##EQU1## [wherein R is a hydrogen atom, a hydroxyl group, an alkoxy group or an alkanoyloxy group; R.sub.1 is a hydrogen atom, an alkyl group, an alkoxyalkyl group or a substituted or unsubstituted aryl group; R.sub.3 is a hydrogen atom or a hydroxyl group; R.sub.4 is a hydrogen atom, an alkyl group or a substituted or unsubstituted aryl group, or R.sub.3 and R.sub.4 may form an alkylidene group or a carbonyl group together with the carbon atom to which these substituents are bonded; R.sub.2, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9 and R.sub.10 are each a hydrogen atom or an alkyl group; A is an alkylene group; and m is an integer of 0 to 2].
摘要翻译：具有下式的新颖的2-取代的6,7-苯并吗啉衍生物：

4. 发明授权

US3961066A 6,7-Benzomorphan derivatives 失效
标题翻译： 6,7-苯并吗啉衍生物
公开(公告)号：US3961066A
公开(公告)日：1976-06-01
申请号：US456268
申请日：1974-03-29
申请人： Toshitsugu Fukumaru , Kenji Kobayashi , Hiroyuki Mizote , Shigeho Inaba , Hisao Yamamoto
发明人： Toshitsugu Fukumaru , Kenji Kobayashi , Hiroyuki Mizote , Shigeho Inaba , Hisao Yamamoto
IPC分类号： A61K31/47 , A61P25/04 , C07D211/70 , C07D211/82 , C07D221/26
CPC分类号： C07D211/70 , C07D221/26 , Y02P20/55 , Y10S514/849
摘要： A novel 2-substituted-6,7-benzomorphan derivative of the formula: ##SPC1##And its acid addition salts, which are useful as non-addicting analgesics and antitussives and can be prepared by reacting a 2-unsubstituted-6,7-benzomorphan derivative of the formula: ##SPC2##With the reactive derivative of an alcohol of the formula:HOA',optionally followed by elimination of the protective group in the resulting product, wherein R.sub.1 is hydrogen, lower alkyl or acyl; R.sub.2 and R.sub.3 are each lower alkyl; A is lower alkyl, cyano(lower)alkyl, benzoyl(lower)alkyl, ar(lower)alkyl, lower alkenyl or cyclo(lower)alkyl(lower)alkyl; and A' is a group as mentioned in A or benzoyl(lower)alkyl of which the carbonyl group is masked with a suitable protective group.
摘要翻译：一种下式的新型2-取代-6,7-苯并吗啉衍生物：

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