Thermodynamic Understanding of an Aza-Michael Reaction Enables Five-Step Synthesis of the Potent Integrin Inhibitor MK-0429
Author:
Affiliation:
1. Department of Small Molecule Drug Discovery, Bristol Myers Squibb Company, 100 Binney Street, Cambridge, Massachusetts 02142, United States
Funder
Bristol-Myers Squibb
Publisher
American Chemical Society (ACS)
Subject
Organic Chemistry
Link
https://pubs.acs.org/doi/pdf/10.1021/acs.joc.1c02375
Reference16 articles.
1. Recent advances in the asymmetric synthesis of pharmacology-relevant nitrogen heterocycles via stereoselective aza-Michael reactions
2. Solvent- and Catalyst-Free Aza-Michael Addition of Imidazoles and Related Heterocycles
3. Mild and Efficient Procedure for Michael Addition of N-Heterocycles to α,β-Unsaturated Compounds Using Anhydrous K3PO4 as Catalyst
4. Lithium Chloride Catalyzed Aza-Michael Addition of Pyrazoles to α,β-Unsaturated Imides
5. Discovery of Potent N-Ethylurea Pyrazole Derivatives as Dual Inhibitors of Trypanosoma brucei and Trypanosoma cruzi
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