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: (see formula I) in racemic or optically active form, 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 formula: (see formula XI) or (see formula XII) 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: (see formula XIII) to give (1S,4R)- or (1R,4S)-4-[(2-amino-6-chloro-5- formamido-4-pyrimidinyl)amino]-2-cyclopentenyl-1-methanol of the formula: (see formula XIV) or (see formula XV) which is then cyclized to give the desired end compound.
|
申请公布号 |
CA2254693(C) |
申请公布日期 |
2009.06.30 |
申请号 |
CA19982254693 |
申请日期 |
1998.11.25 |
申请人 |
LONZA AG |
发明人 |
BERCHTOLD, KATJA;BREITBACH, HOLGER;BRIEDEN, WALTER;SCHROER, JOSEF;URBAN, EVA MARIA;BERNEGGEREGLI, CHRISTINE;PETERSEN, MICHAEL;RODUIT, JEAN-PAUL |
分类号 |
C07C215/42;C07D473/40;C07B53/00;C07B57/00;C07C213/00;C07C213/02;C07C213/08;C07C213/10;C07C215/26;C07C233/23;C07C271/24;C07C275/64;C07D239/50;C07D473/00;C07D473/02;C07D473/32;C12P13/00;C12P41/00 |
主分类号 |
C07C215/42 |
代理机构 |
|
代理人 |
|
主权项 |
|
地址 |
|