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Traceless solid-phase synthesis of 2,4-diaminoquinazolines
1Procter & Gamble Pharmaceuticals, Healthcare Research Center, Mason, Ohio 45040, USA. lwilson3@prius.jnj.com
Organic Letters
|February 17, 2001
Abstract:
[reaction: see text] The solid-phase synthesis of 2,4-diaminoquinazolines is presented. The chemistry involves the sequential condensation of 2-aminobenzonitriles and amines starting from an acyl isothiocyanate resin via a traceless cleavage and cyclization. The alpha-1 antagonist prazosin was synthesized, as well as several other examples, in good yields and purity.