SuFEx-Enabled Direct Deoxy-Diversification of Alcohols

We introduce a new use of sulfonyl fluoride as a bifunctional
reagent
that facilitates the one-step deoxy-diversification of complex alcohol
libraries. Our reaction design features a Sulfur­(VI) Fluoride Exchange
(SuFEx) mediated activation of alcohols and fluoride-induced activation
of silicon-bound nucleophiles. This method enables the direct conversion
of alcoholic C–O bonds in complex molecules into diverse analogues
via C–C, C–N, C–Cl, and C–Br bond formation
while suppressing any elimination side-products.

本研究提出了一种新颖的磺酰氟化物在复杂醇库中实现一步脱氧多样化反应的应用。本研究设计了一种以硫(VI)氟化物交换(SuFEx)为介导的醇活化以及氟化硅键合亲核试剂的氟化诱导活化反应体系。该方法能够将复杂分子中的醇类C-O键直接转化为多种类似物，通过形成C-C、C-N、C-Cl和C-Br键，同时抑制消除副产物的生成。