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1. 发明授权

US07507814B2 Process for preparation of imipenem 有权
标题翻译：亚胺培南的制备方法
公开(公告)号：US07507814B2
公开(公告)日：2009-03-24
申请号：US10563250
申请日：2004-12-09
申请人： Hyun Seop Bae , Tae Seop Hwang , Chan Yong Ahn , Chang Hoon Oh , Moo Sung Kim
发明人： Hyun Seop Bae , Tae Seop Hwang , Chan Yong Ahn , Chang Hoon Oh , Moo Sung Kim
IPC分类号： C07D477/20 , C07D477/18
CPC分类号： C07D477/06 , C07D477/20 , C07D487/04
摘要： The invention provides a novel compound of Formula II which is useful in the preparation of imipenem monohydrate of Formula I, wherein R1 is a p-nitrobenzyl or p-methoxybenzyl group; and R2 and R3 may be identical to or different from each other and are each independently a C1-6alkyl or aryl group, or a derivative thereof, and a process for preparing the compound of Formula II by coupling (5R,6S) p-nitrobenzyl-3-(diphenylphosphono)-6-[(1R)-1-hydroxyethyl]-1-azabicyclo[3.2.0]hept-2-ene-7-one-2-carboxylate with 2-aminoetahnethiol hydrocloride in the presence of a base, followed by a reaction with a ketone. Further, the invention provides a process for preparing the compound of Formula I by reacting a compound of Formula II with isopropylformimidate or benzylformimidate in the presence of a base, followed by hydrogenation, separation and crystallization.
摘要翻译：本发明提供了一种新的式II化合物，其可用于制备式I的亚胺培南一水合物，其中R 1为对硝基苄基或对甲氧基苄基; 并且R 2和R 3可以彼此相同或不同，并且各自独立地为C 1-6烷基或芳基或其衍生物，以及通过将（5R，6S）对硝基苄基 -3-（二苯基膦酰基）-6 - [（1R）-1-羟乙基] -1-氮杂双环[3.2.0]庚-2-烯-7-酮-2-羧酸叔丁酯与2-氨基乙脑二醇氢氯化物碱，然后与酮反应。此外，本发明提供了通过在碱的存在下使式II化合物与异丙基甲酰亚胺酯或苄基甲酰亚氨酸酯反应，然后氢化，分离和结晶来制备式I化合物的方法。

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