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A Two-Step, One-Pot, and Multigram-Scale Synthesis of N-Difluoromethylthiophthalimide
Organic Process Research & Development ( IF 3.4 ) Pub Date : 2017-07-18 00:00:00 , DOI: 10.1021/acs.oprd.7b00203
Dianhu Zhu 1 , Xin Hong 1 , Dezhi Li 1 , Long Lu 1 , Qilong Shen 1
Affiliation  

A new method for the 100 g scale synthesis of N-difluoromethylthiophthalimide 1 from cheap commodity chemical benzyl mercaptan and HCF2Cl or other difluorocarbene precursors was described. Reagent 1 is an excellent electrophilic difluoromethylthiolating reagent as demonstrated by the gram-scale synthesis of five difluoromethylthiolated derivatives of structurally complicated drug-like molecules and natural products.

中文翻译:

N-二氟甲基硫代邻苯二甲酰亚胺的两步一锅多克级合成

描述了一种从廉价的商品化学苄硫醇和HCF 2 Cl或其他二氟卡宾前体100 g规模合成N-二氟甲基硫代邻苯二甲酰亚胺1的新方法。试剂1是一种优异的亲电二氟甲基硫醇化试剂,结构复杂的药物样分子和天然产物的五种二氟甲基硫醇化衍生物的克级合成证明了这一点。
更新日期:2017-07-19
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