发明名称 |
PROCESS FOR THE PREPARATION OF (1S,4R)-OR(1R,4S)-4-(2-AMINO-6-CHLORO-9H-PURIN-9-YL)-2-CYCLOPENTENE-1-METHANOL |
摘要 |
A novel process for the preparation of (1S,4R)- or (1R,4S)-4-(2-amino-6-chloro-9H-purin-9-yl)-2-cyclo- pentene-1-methanol of the formula: <IMG> is described. This entails in a first stage acylating (~)- 2-azabicyclo[2.2.1]hept-5-en-3-one of the formula: <IMG> to give a (~)-2-azabicyclo[2.2.1]hept-5-en-3-one derivative of the general formula: <IMG> in which R1 denotes C1-4-alkyl, C1-4-alkoxy, aryl or aryloxy, the latter being reduced in a second stage to give a cyclopentene derivative of the general formula: <IMG> in which R1 has the stated meaning. The cyclopentene derivative V is then converted in a third stage biotechnologically into a (1R,4S)- or (1S,4R)-1-amino-4- (hydroxymethyl)-2-cyclopentene of the formula: <IMG> the latter being converted in a fourth stage with N-(2- amino-4,6-dichloro-5-pyrimidinyl)formamide of the formula: <IMG> into a (1S,4R)- or (1R,4S)-4-[(2-amino-6-chloro-5- formamido-4-pyrimidinyl)amino]-2-cyclopentene-1-methanol of the formula: <IMG> Finally, the compound of forumula IX or X is cyclized in a fifth stage in a known manner to form the final product of formula I or II.
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申请公布号 |
CA2237297(C) |
申请公布日期 |
2008.03.11 |
申请号 |
CA19982237297 |
申请日期 |
1998.05.11 |
申请人 |
LONZA AG |
发明人 |
BIRCH, OLWEN MARY;BURGDORF, KURT;BRUX, FRANK;BERNEGGER, CHRISTINE;BOSSARD, PIERRE;BRIEDEN, WALTER;GUGGISBERG, YVES;URBAN, EVA MARIA;DUC, LAURENT;ETTER, KAY-SARA;GORDON, JOHN;O'MURCHU, COLM |
分类号 |
C12P13/00;C12P41/00;C07C231/02;C07C231/18;C07C231/20;C07C233/23;C07C269/06;C07C271/24;C07D209/94;C07D233/04;C07D233/74;C07D235/02;C07D237/06;C07D239/70;C07D473/40;C12P13/02;C12P17/18;C12R1/01;C12R1/05;C12R1/06;C12R1/09;C12R1/19;C12R1/38 |
主分类号 |
C12P13/00 |
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