Practical Synthesis of (+)-Biotin Key Intermediate by Calcium Borohydride Reduction and Temperature-Dependent Purity Upgrade during Crystallization,Organic Process Research & Development

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Practical Synthesis of (+)-Biotin Key Intermediate by Calcium Borohydride Reduction and Temperature-Dependent Purity Upgrade during Crystallization
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2021-07-16 , DOI: 10.1021/acs.oprd.1c00196
Masahiko Seki ₁ , Yusuke Takahashi ₁

Affiliation

An expedient synthesis of a key intermediate for (+)-biotin has been accomplished through high-yielding reduction of chiral imide with calcium borohydride and efficient isolation of the desired isomer by crystallization at a specific temperature where only undesired isomer was converted to soluble anhydrate while the desired isomer kept unchanged as a less soluble monohydrate.

中文翻译：

在结晶过程中通过硼氢化钙还原和温度依赖性纯度升级实际合成 (+)-生物素关键中间体

通过用硼氢化钙高产率还原手性酰亚胺并通过在特定温度下结晶有效分离所需异构体，完成了（+）-生物素关键中间体的便利合成，其中只有不需要的异构体转化为可溶性无水物，同时所需的异构体保持不变，为溶解度较低的一水合物。

更新日期：2021-08-20

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