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Expedient Approach to the Synthesis of Betrixaban
SynOpen ( IF 2.0 ) Pub Date : 2020-09-04 , DOI: 10.1055/s-0040-1707267 Chada Raji Reddy 1, 2 , Sudam N. Sinare 2
中文翻译：
合成贝曲西班的权宜之计
更新日期：2020-11-03
SynOpen ( IF 2.0 ) Pub Date : 2020-09-04 , DOI: 10.1055/s-0040-1707267 Chada Raji Reddy 1, 2 , Sudam N. Sinare 2
Affiliation
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A new scalable route to synthesize the factor Xa (FXa) inhibitor betrixaban is disclosed. The product is obtained in a seven-step reaction sequence (in five stages using two one-pot reactions) starting from easily accessible 4-(N,N-dimethylcarbamimidoyl)benzoate. Effective isolation of intermediates, use of cost-effective amide formation and 2-methyltetrahydrofuran as an effective reaction solvent as well as for extraction in three of the stages, are key features. The strategy provides the desired product in 38% overall yield with high purity (>98%).
中文翻译：
合成贝曲西班的权宜之计
公开了合成因子Xa（FXa）抑制剂贝曲西班的新的可扩展途径。以容易获得的4-（N，N-二甲基氨基甲酰胺基）苯甲酸酯为起始原料，以七个步骤的反应顺序（五个阶段，使用两个一锅法反应）获得产物。关键特征是有效分离中间体，使用经济高效的酰胺形成方法和将2-甲基四氢呋喃用作有效的反应溶剂以及在三个阶段中进行萃取。该策略以38％的总产率提供了高纯度（> 98％）的所需产品。
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