发明申请
- 专利标题： Process For Preparing Dipeptidyl Peptidase IV Inhibitors And Intermediates Therefor
- 专利标题（中）： 制备二肽基肽酶IV抑制剂及其中间体的方法
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申请号： US13523733申请日： 2012-06-14
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公开(公告)号： US20120276600A1公开(公告)日： 2012-11-01
- 发明人: Michael Politino , Matthew M. Cadin , Paul M. Skonezny , Jason G. Chen
- 申请人： Michael Politino , Matthew M. Cadin , Paul M. Skonezny , Jason G. Chen
- 申请人地址： US NJ Princeton
- 专利权人： BRISTOL-MYERS SQUIBB COMPANY
- 当前专利权人： BRISTOL-MYERS SQUIBB COMPANY
- 当前专利权人地址： US NJ Princeton
- 主分类号： C07D209/52
- IPC分类号： C07D209/52 ; C12P13/00
摘要：
A process for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV is provided which employs a BOC-protected amine of the structure prepared by subjecting an acid of the structure to reduce amination by treating the acid with ammonium formate, nicotinamide adenine dinucleotide, dithiothreitol and partially purified phenylalanine dehydrogenase/formate dehydrogenase enzyme concentrate (PDH/FDH) and without isolating treating the resulting amine of the structure 2 with di-tert-butyl dicarbonate to form the BOC-protected amine
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