Double Capture of Difluorocarbene by 2-Aminostyrenes Enables the Construction of 3-(2,2-Difluoroethyl)-2-fluoroindoles.

doi:10.1021/acs.orglett.1c02816

Paper

Double Capture of Difluorocarbene by 2-Aminostyrenes Enables the Construction of 3-(2,2-Difluoroethyl)-2-fluoroindoles.

Published Oct 7, 2021 · Heyun Sheng, Jianke Su, Xin Li

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Abstract

We report herein an efficient strategy to construct 3-(2,2-difluoroethyl)-2-fluoroindoles from activated o-aminostyrenes with ethyl bromodi-fluoroacetate as a difluorocarbene source. Through double capture of a difluorocarbene, two different types of fluorine motifs are incorporated into the products with simultaneous construction of one C-N and two C-C bonds, without the need for transition metals. This reaction features high efficiency and excellent functional group compatibility and has great potential in the late-stage modifications of pharmaceutical molecules and natural products.

Study Snapshot

This study presents an efficient strategy for constructing 3-(2,2-difluoroethyl)-2-fluoroindoles from activated o-aminostyrenes, offering potential for late-stage modifications of pharmaceutical molecules and natural products.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Double Capture of Difluorocarbene by 2-Aminostyrenes Enables the Construction of 3-(2,2-Difluoroethyl)-2-fluoroindoles.

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Citations