KOGAKUKATSUSEI11CHIKANN22AMINOPUROPANNOSEIHO

摘要

PURPOSE:To obtain the titled compound useful as a synthetic intermediate for various pharmaceuticals, either by reducing an optically active 3- substituted-2-aminopropanol derivative in the presence of a metal halide or by reacting said compound with a metal halide and reducing the reaction product. CONSTITUTION:The objective compound of formula III can be produced either by (1) reacting a compound of formula I [R<1> is (substituted) aryl or nitrogen- containing heterocyclic group; OZ is protected OH; -NHY is (protected) amino] or its salt with a reducing agent (e.g. metallic zinc) in the presence of a metal halide (e.g. sodium iodide) at 20-100 deg.C or by (2) reacting the compound of formula I or its salt with a metal halide in a mixed solvent of water and THF, etc., at 120-100 deg.C and reducing the resultant corresponding propyl halide of formula II (X is halogen). EFFECT:The objective compound can be produced from an easily available raw material in high purity and yield.