Whelligan, D. K., Thomson, D. W., Taylor, D., Hoelder, S. (2010) Two-Step Synthesis of Aza- and Diazaindoles from Chloroamino-N-heterocycles Using Ethoxyvinylborolane. JOURNAL OF ORGANIC CHEMISTRY, 75 (1). pp. 11-15. ISSN 0022-3263

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Abstract

An efficient two-step route to a broad range of aza- and diazaindoles was established, starting from chloroamino-N-heterocycles, without the need for protecting groups. The method involves an optimized Suzuki-Miyaura coupling with (2-ethoxyvinyl)borolane followed by acetic acid-catalyzed cyclization.

Item Type:	Article
Authors (ICR Faculty only):	Hoelder, Swen
All Authors:	Whelligan, D. K., Thomson, D. W., Taylor, D., Hoelder, S.
Uncontrolled Keywords:	CROSS-COUPLING REACTIONS; SUZUKI-MIYAURA REACTION; HIGHLY-ACTIVE CATALYST; CONVENIENT SYNTHESIS; KINASE INHIBITORS; ARYL CHLORIDES; REACTIVITY; AZAINDOLES; DESIGN; 7-AZAINDOLES
Funding Acknowledgement:	NHS ; Cancer Research UK [C309/A8274]
Funding Text:	We acknowledge NHS funding to the NIHR Biomedical Research Centre and funding from Cancer Research UK program Grant No. C309/A8274. We also thank Dr. Amin Mirza, Mr. Mcirion Richards, and Dr. Maggie Liu for their help with LC, NMR, and mass spectrometry.
Research teams:	ICR divisions > Cancer Therapeutics > Medicinal Chemistry 4
Depositing User:	Users 10 not found.
Date Deposited:	08 Jan 2010 14:38
Last Modified:	08 Jan 2010 14:38
URI:	http://publications.icr.ac.uk/id/eprint/9198

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