发明名称 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
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.
申请公布号 US7229981(B2) 申请公布日期 2007.06.12
申请号 US20030695930 申请日期 2003.10.29
申请人 LONZA AG 发明人 BRIEDEN WALTER;SCHROEER JOSEF;BERNEGGER-EGLI CHRISTINE;URBAN EVA MARIA;PETERSEN MICHAEL;RODUIT JEAN-PAUL;BERCHTOLD KATJA;BREITBACH HOLGER
分类号 A01N43/00;C07D473/40;C07B53/00;C07B57/00;C07C213/00;C07C213/02;C07C213/08;C07C213/10;C07C215/26;C07C215/42;C07C233/23;C07C271/24;C07C275/64;C07D473/00;C07D473/02;C07D473/32;C12P13/00;C12P41/00 主分类号 A01N43/00
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