A new synthesis of the GPIIb/IIIa receptor antagonist SB-214857-A

被引:23
作者
Andrews, IP [1 ]
Atkins, RJ [1 ]
Badham, NF [1 ]
Bellingham, RK [1 ]
Breen, GF [1 ]
Carey, JS [1 ]
Etridge, SK [1 ]
Hayes, JF [1 ]
Hussain, N [1 ]
Morgan, DO [1 ]
Share, AC [1 ]
Smith, SAC [1 ]
Walsgrove, TC [1 ]
Wells, AS [1 ]
机构
[1] GlaxoSmithKline Pharmaceut, Synthet Chem, Tonbridge TN11 9AN, Kent, England
关键词
asymmetric synthesis; benzodiazepine; carbonylation; enzyme reaction; epimerisation; hydrogenation;
D O I
10.1016/S0040-4039(01)00843-7
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A new synthesis of lotrafiban SB-214857-A is reported. The key steps are the preparation of racemic (4-melhyl-3-oxo-2,3,4,5-tetrahydro-1H-benzo[c][1,4]diazepin-2-yl)-acid methyl ester from 2-nitrobenzyl alcohol, a resolution using an immobilised lipase enzyme and a palladium-catalysed aminocarbonylation reaction. (C) 2001 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:4915 / 4917
页数:3
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