Process development of CP-481715, a novel CCR1 antagonist

被引：12

作者：

Li, B ^{[1
]}

Andresen, B ^{[1
]}

Brown, MF ^{[1
]}

Buzon, RA ^{[1
]}

Chiu, CKF ^{[1
]}

Couturier, M ^{[1
]}

Dias, E ^{[1
]}

Urban, FJ ^{[1
]}

Jasys, VJ ^{[1
]}

Kath, JC ^{[1
]}

Kissel, W ^{[1
]}

Le, T ^{[1
]}

Li, ZJ ^{[1
]}

Negri, J ^{[1
]}

Poss, CS ^{[1
]}

Tucker, J ^{[1
]}

Whritenour, D ^{[1
]}

Zandi, K ^{[1
]}

机构：

[1] Pfizer Global Res & Dev, Groton Labs, Groton, CT 06340 USA

来源：

ORGANIC PROCESS RESEARCH & DEVELOPMENT | 2005年 / 9卷 / 04期

关键词：

D O I：

10.1021/op050059w

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

Process development for the synthesis of 2-quinoxalinecarboxamide, N-[(1S,2S,4R)-4-(aminocarbonyl)-1-[(3-fluorophenyl)methyl]-2,7-dihydroxy-7-methyloctyl] is described. An optimized,and streamlined process starting from lactone 2 was developed: Lactone 2 was alkylated diastereoselectively with prenyl bromide, followed by deprotection of the N-Boc group and concomitant hydration of the olefin. Aminolysis of the lactone in methanolic ammonia afforded the titled compound.

引用

页码：466 / 471

页数：6

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