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US07829699B2 Process for the preparation of CGRP antagonist 失效
制备CGRP拮抗剂的方法

  • Patent Title: Process for the preparation of CGRP antagonist
  • Patent Title (中): 制备CGRP拮抗剂的方法
  • Application No.: US12226244
    Application Date: 2007-04-06
  • Publication No.: US07829699B2
    Publication Date: 2010-11-09
  • Inventor: Kevin BelykNelo Rivera
  • Applicant: Kevin BelykNelo Rivera
  • Applicant Address: US NJ Rahway
  • Assignee: Merck Sharp & Dohme Corp.
  • Current Assignee: Merck Sharp & Dohme Corp.
  • Current Assignee Address: US NJ Rahway
  • Agent Gerard Devlin; Raynard Yuro
  • International Application: PCT/US2007/008702 WO 20070406
  • International Announcement: WO2007/120591 WO 20071025
  • Main IPC: C07D471/04
  • IPC: C07D471/04
Process for the preparation of CGRP antagonist
Abstract:
An efficient synthesis for the preparation of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1 -carboxamide, by coupling (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one and 2-oxo-1-(4-piperidinyl)-2,3-dihydro-1H-imidazo[4,5-b]pyridine dihydrochloride with 1,1′-carbonyldiimidazole (“CDI”) as carbonyl source; and an efficient preparation of the potassium salt of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide.
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