发明授权
US4033964A Imidazolylacetic acid amides, their production, antimycotic compositions
comprising said compounds and their use as antimycotic agents
失效
咪唑基乙酸酰胺,它们的生产,包含所述化合物的抗真菌组合物及其作为抗真菌剂的用途
- 专利标题: Imidazolylacetic acid amides, their production, antimycotic compositions comprising said compounds and their use as antimycotic agents
- 专利标题(中): 咪唑基乙酸酰胺,它们的生产,包含所述化合物的抗真菌组合物及其作为抗真菌剂的用途
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申请号: US594569申请日: 1975-07-09
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公开(公告)号: US4033964A公开(公告)日: 1977-07-05
- 发明人: Jurgen Wenzelburger , Karl Heinz Buchel , Manfred Plempel , Werner Meiser
- 申请人: Jurgen Wenzelburger , Karl Heinz Buchel , Manfred Plempel , Werner Meiser
- 申请人地址: DT
- 专利权人: Bayer Aktiengesellschaft
- 当前专利权人: Bayer Aktiengesellschaft
- 当前专利权人地址: DT
- 优先权: DT2247187 19720926
- 主分类号: A61K31/415
- IPC分类号: A61K31/415 ; C07D417/06 ; C07D403/12
摘要:
Imidazolylacetic acid amides of the formula: ##STR1## or pharmaceutically acceptable nontoxic salts thereof WHEREIN EITHERR.sup.1 is phenyl or cycloalkyl, unsubstituted or substituted by one or more substituents; andR.sup.2 is hydrogen;OrR.sup.1 or R.sup.2, together with the nitrogen atom to which they are attached, form a saturated 5 to 7-membered heterocyclic ring which ring may contain an --SO.sub.2 -- or --NY-- moiety wherein Y is alkoxycarbonyl, dialkylaminocarbonyl, or phenyl or diphenylmethyl, unsubstituted or substituted by one or more substituents and wherein said 5 to 7-membered heterocyclic ring itself is otherwise unsubstituted or substituted by one or more substituents; andX.sup.1, x.sup.2, and X.sup.3 and X.sup.4 are the same or different and are each hydrogen or halogen,Are produced byA. reacting a halodiphenylacetic acid amide of the formula: ##STR2## wherein R.sup.1, R.sup.2, X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are as above defined, and Hal is halogen, with imidazole; orB. reacting a halodiphenylacetic acid halide of the formula: ##STR3## wherein X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are as above defined andHal is halogen with imidazole to produce an imidazolide of the formula: ##STR4## wherein X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are as above defined which in turn is transaminated by reaction with an amine of the formula:NHR.sup.1 R.sup.2 whereinR.sup.1 and R.sup.2 are as above defined.
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