| 摘要 |
PURPOSE:To easily epimerize a compound useful as a cardiotonic agent, etc., in high yield, by reacting an optically active benzyl alcohol with a carboxylic acid, subjecting the product to intramolecular cyclization reaction and treating with a base. CONSTITUTION:An optically active benzyl alcohol derivative of formula I [ZO is (protected) OH] or its salt is made to react with a carboxylic acid compound of formula R<1>COOH (R<1>CO is acyl) or its reactive derivative by conventional method to obtain an optically active N-acylbenzyl alcohol derivative of formula II. The obtained derivative is made to react with a thionyl halide in a solvent such as methylene chloride under cooling or heating. The reaction product is made to react with a base such as sodium hydroxide in a solvent such as hydrated methanol at room temperature or under heating to enable the epimerization of the compound of formula I.
|
