The medicinal chemist's toolbox for late stage functionalization of drug-like molecules

Author:

Cernak Tim1234,Dykstra Kevin D.1254,Tyagarajan Sriram1254,Vachal Petr1254,Krska Shane W.1254

Affiliation:

1. Merck Research Laboratories

2. Discovery Chemistry - Automation & Capabilities Enhancement

3. Boston

4. USA

5. Rahway

Abstract

The advent of modern C–H functionalization chemistries has enabled medicinal chemists to consider a synthetic strategy, late stage functionalization (LSF), which utilizes the C–H bonds of drug leads as points of diversification for generating new analogs.

Publisher

Royal Society of Chemistry (RSC)

Subject

General Chemistry

Reference297 articles.

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2. Alkane C–H Activation by Single-Site Metal Catalysis, ed. P. Pedros, Springer, New York, 2012

3. C–H and C–X Bond Function: Transition Metal Mediation, ed. X. Ribas, RCS Publishing, London, 2013

4. C–H Bond Activation in Organic Synthesis, ed. L. J. Jack, CRC Press, Boca Raton, 2015

5. C–H bond activation enables the rapid construction and late-stage diversification of functional molecules

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