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Synthesis of useful fragments in drug discovery: 2-amino-5-tert-butylpyridine and its oxidised analogues.

Thomson, Christopher and Reilly, John and Sandham, David (2011) Synthesis of useful fragments in drug discovery: 2-amino-5-tert-butylpyridine and its oxidised analogues. Bioorganic and Medicinal Chemistry Letters, 21 (14). pp. 4281-4283. ISSN 0960-894X

Abstract

A novel and robust synthesis of the fragment, 2-amino-5-tert-butylpyridine, has been described, which has been shown to have improved physicochemical properties over 4-tert-butylaniline, when considering drug-like properties. The synthesis also yields fragments containing more highly oxidised precursors to the tert-butyl group as intermediates. These fragments can be incorporated into final target molecules, yielding pharmaceutical compounds and their putative CYP-mediated oxidative metabolites, which can aid in elucidation of metabolic clearance processes.

Item Type: Article
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Additional Information: author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
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Date Deposited: 13 Oct 2015 13:15
Last Modified: 13 Oct 2015 13:15
URI: https://oak.novartis.com/id/eprint/4158

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