An efficient sequence for the preparation of small secondary amine hydrochloride salts for focused library generation without need for distillation or chromatographic …

GM Dubowchik, JA Michne, D Zuev

Index: Dubowchik, Gene M.; Michne, Jodi A.; Zuev, Dmitry Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 12 p. 3147 - 3149

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Citation Number: 12

Abstract

Collections of small secondary amines for compound library generation can be efficiently prepared by amide reduction using BH3–THF or Red-Al followed by brief methanolysis, trapping with di-tert-butyl dicarbonate, and deprotection with 4M HCl in dioxane. The sequence requires no chromatography or distillation and provides multi-gram quantities of pure HCl salts in a short time.