Yaning Guo, Yu Huang, Zhedong Yuan
Jul 4, 2014
Citations
0
Influential Citations
1
Citations
Journal
Organic Preparations and Procedures International
Abstract
Dabigatran etexilate (N-[2-{4-[N-(hexyloxycarbonyl)amidino]phenylaminomethyl}-1methyl-1H-benzimidazol-5-ylcarbonyl]-N-(2-pyridyl)-β-alanine ethyl ester, 9) is a selective, reversible, and direct inhibitor of thrombin; it has been clinically developed for the prevention of venous thrombolism and cardioembolic stroke.1–3 A key intermediate in the preparation of dabigatran etexilate is reported4,5 to be 3-[(3-amino-4-methylaminobenzoyl)pyridin-2-yl-amino]propionic acid ethyl ester (6), which has been obtained from 4-methylamino-3-nitrobenzoic acid (1) in only 25∼50% overall yield (Scheme 1).4–6