jo9b02394_si_001.pdf (3.3 MB)
Synthesis of N‑Acyl Sulfamates from Fluorosulfonates and Potassium Trimethylsilyloxyl Imidates
journal contribution
posted on 2019-11-12, 19:08 authored by Shuning Zhang, Huan Xiong, Fengping Lu, Fei Ma, Yuang Gu, Peixiang Ma, Hongtao Xu, Guang YangAn
efficient and operationally simple method for the synthesis
of N-acyl sulfamates from fluorosulfonates and potassium
trimethylsilyloxyl imidates as amide precursor is reported. This approach
showed broad substrate scope, mild and base-free reaction conditions,
short reaction time, and high to excellent yields. Notably, we demonstrated
the power of this reaction in the rapid late-stage functionalization
of three complex phenol-containing bioactive molecules. Given the
prevalence of phenol-containing drugs and building blocks, this method
is applicable toward a diversity-oriented drug discovery.
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building blocksreaction timeamide precursorsubstrate scopeacyl sulfamatesbase-free reaction conditionsmethodlate-stage functionalizationpotassium trimethylsilyloxyl imidatesphenol-containing bioactive moleculesdiversity-oriented drug discoveryphenol-containing drugsPotassium Trimethylsilyloxyl Imidates
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