Electrophilic fluoroalkylthiolation induced diastereoselective and stereospecific 1,2-metalate migration of alkenylboronate complexes,Chemical Science

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Electrophilic fluoroalkylthiolation induced diastereoselective and stereospecific 1,2-metalate migration of alkenylboronate complexes
Chemical Science ( IF 7.6 ) Pub Date : 2020-07-07 , DOI: 10.1039/d0sc03039b
Feng Shen _{1,

2,

3,

4,

5} , Long Lu _{2,

4,

6} , Qilong Shen _{1,

2,

3,

4,

5}

Affiliation

A transition metal free process for conjunctive functionalization of alkenylboron ate-complexes with electrophilic fluoroalkylthiolating reagents is described, affording β-trifluoroalkylthiolated and difluoroalkylthiolated boronic esters in good yield and excellent diastereoselectivity. The potential applicability of the method was demonstrated by the preparation of a difluoromethylthiolated mimic 12 of a potential drug molecule PF-4191834 for the treatment of asthma.

中文翻译：

亲电性氟代烷基硫醇化诱导烯基硼酸酯络合物的非对映选择性和立体有规的1,2-金属盐迁移

描述了用亲电子的氟代烷基硫醇化试剂对链烯基硼酸酯配合物进行联合官能化的无过渡金属工艺，能够以良好的收率和优异的非对映选择性提供β-三氟烷基硫代和二氟烷基硫代硼酸酯。该方法的潜在适用性通过制备潜在药物分子PF-4191834的二氟甲基硫醇化模拟物12来证明，可用于治疗哮喘。

更新日期：2020-08-05

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