发明授权
US07229981B2 Process for the preparation of aminoalcohol derivatives and their further conversion to (1R,4S)-4-(2-amino-6-chloro-5-formamido-4-pyrimidinyl)-amino)-2-cyclopentenyl-1-methanol
失效
制备氨基醇衍生物的方法及其进一步转化为(1R,4S)-4-(2-氨基-6-氯-5-甲酰氨基-4-嘧啶基) - 氨基)-2-环戊烯基-1-甲醇
- 专利标题: Process for the preparation of aminoalcohol derivatives and their further conversion to (1R,4S)-4-(2-amino-6-chloro-5-formamido-4-pyrimidinyl)-amino)-2-cyclopentenyl-1-methanol
- 专利标题(中): 制备氨基醇衍生物的方法及其进一步转化为(1R,4S)-4-(2-氨基-6-氯-5-甲酰氨基-4-嘧啶基) - 氨基)-2-环戊烯基-1-甲醇
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申请号: US10695930申请日: 2003-10-29
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公开(公告)号: US07229981B2公开(公告)日: 2007-06-12
- 发明人: Walter Brieden , Josef Schröer , Christine Bernegger-Egli , Eva Maria Urban , Michael Petersen , Jean-Paul Roduit , Katja Berchtold , Holger Breitbach
- 申请人: Walter Brieden , Josef Schröer , Christine Bernegger-Egli , Eva Maria Urban , Michael Petersen , Jean-Paul Roduit , Katja Berchtold , Holger Breitbach
- 申请人地址: CH Basel
- 专利权人: Lonza AG
- 当前专利权人: Lonza AG
- 当前专利权人地址: CH Basel
- 代理机构: Darby & Darby
- 优先权: CH2739/97 19971127; CH2781/97 19971203; CH0133/98 19980121; CH0723/98 19980327; EP98118895 19981007
- 主分类号: A01N43/00
- IPC分类号: A01N43/00
摘要:
The invention relates to a novel process for the preparation of an aminoalcohol of the formula racemically or optically active, starting from 2-azabi-cyclo[2.2.1]hept-5-en-3-one, its further conversion to give the corresponding acyl derivative and its further conversion to (1S,4R)— or (1R,4S)-4-(2-amino-6-chloro-9-H-purine-9-yl)-2-cyclopentenyl-1-methanol of the formulae In the latter synthesis, the aminoalcohol is converted into the corresponding D- or L-tartrate, which is then reacted with N-(2-amino-4,6-dichloropyrimidin-5-yl) formamide of the formula to give (1S, 4R)- or (1R, 4S)-4-[(2-amino-6-chloro-5-formamido-4-pyrimidinyl)amino]-2-cyclopentenyl-1-methanol of the formulae and then cyclized to give the end compounds.
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