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process for the production of penamderivaten from cephamderivaten

机译:头孢氨苄生产戊酰胺的方法

摘要

The present invention relates to a process for preparing 2alpha-methyl-2beta-substituted methyl penam derivatives from cepham derivatives, more particularly the present invention provides a novel process for preparing 2beta-heterocyclyl methyl penam derivatives of the formula (I) by reacting a cepham compound with a heterocylic amine to form an intermediate compound, and oxidizing the intermediate compound to produce the 2beta-heterocyclyl methyl penam derivatives of the formula (I), wherein RSUB1 /SUBrepresents carboxylic acid protecting group; RSUB2 /SUBand RSUB3 /SUBmay be same or different and independently represent hydrogen, halogen, NHSUB2/SUB, acylamino, phthalimido with a proviso that both RSUB2 /SUBand RSUB3 /SUBare not NHSUB2/SUB, acylamino, phthalimido; Het represents a 5 or 6 membered nitrogen containing heterocycle ring system having one or more heteroatoms selected from O, S, or N.
机译:本发明涉及由cepham衍生物制备2α-甲基-2β-取代的甲基penam衍生物的方法,更具体地说,本发明提供了一种通过使cepham反应制备式(I)的2β-杂环基甲基penam衍生物的新方法。该化合物与杂环胺形成中间体化合物,并将该中间体化合物氧化以制备式(I)的2β-杂环基甲基戊烯衍生物,其中R SUB 1代表羧酸保护基; R 2 和R 3 可以相同或不同,分别代表氢,卤素,NH 2 ,酰氨基,邻苯二甲酰亚胺,但前提是两个R 2 和R 3 不是NH 2 ,酰氨基,邻苯二甲酰亚胺; Het代表5或6元含氮杂环系统,具有一个或多个选自O,S或N的杂原子。

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