An efficient sequence for the preparation of small secondary amine hydrochloride salts for focused library generation without need for distillation or chromatographic purification
Bioorganic & Medicinal Chemistry Letters(2004)
摘要
Collections of 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 HCl. The sequence requires no chromatography or distillation and provides multi-gram quantities of pure HCl salts in a short time.
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关键词
Amide reduction,Combinatorial
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