Invention Grant
US07659409B2 3-Hydroxy-3-(2-thienyl) propionamides and production method thereof, and production method of 3-amino-1-(2-thienyl)-1-propanols using the same 失效
3-羟基-3-(2-噻吩基)丙酰胺及其制备方法和使用其的3-氨基-1-(2-噻吩基)-1-丙醇的制备方法

3-Hydroxy-3-(2-thienyl) propionamides and production method thereof, and production method of 3-amino-1-(2-thienyl)-1-propanols using the same
Abstract:
The object of the present invention is to provide 3-hydroxy-3-(2-thienyl)propionamides useful as synthesis intermediates of pharmaceutical preparations and the like and a method for obtaining optically active 3-amino-1-(2-thienyl)-1-propanols using the same with high reaction yield, high optical yield and industrially low cost.According to the present invention, 3-amino-1-(2-thienyl)-1-propanols are obtained by carrying out asymmetric reduction of a β-ketocarbonyl compound having thiophene ring in the presence of a catalyst constituted from a compound of a group VIII or IX metal in the periodic table (e.g., a ruthenium compound) and an asymmetric ligand represented by a specified optically active diamine derivative (e.g., a diphenylethylenediamine derivative), or using a cell, a treated product of said cell or the like of a microorganism, and as occasion demands, carrying out amidation of the ester group and then carrying out reduction of the amido group. (each of the substituents is as described in claim 1).
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