Enabling synthesis in fragment-based drug discovery by reactivity mapping: photoredox-mediated cross-dehydrogenative heteroarylation of cyclic amines
Author:
Affiliation:
1. Astex Pharmaceuticals
2. Cambridge
3. UK
4. Department of Chemistry
5. University of Cambridge
6. Cambridge CB2 1EW
7. Novartis Pharma AG
Abstract
A nanogram-to-gram workflow has been established for the identification and development of synthetic transformations which are enabling in Fragment-Based Drug Discovery (FBDD). In this study, we disclose a method for the synthesis of privileged sp2–sp3 architectures via direct cross-dehydrogenative coupling of heterocycles.
Publisher
Royal Society of Chemistry (RSC)
Subject
General Chemistry
Link
http://pubs.rsc.org/en/content/articlepdf/2019/SC/C8SC04789H
Reference57 articles.
1. Twenty years on: the impact of fragments on drug discovery
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3. Opportunity Knocks: Organic Chemistry for Fragment-Based Drug Discovery (FBDD)
4. Fragment-to-Lead Medicinal Chemistry Publications in 2015
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