Process for the preparation of benzyl alcohol derivatives

Details Process for the preparation of benzyl alcohol derivatives Process for the preparation of benzyl alcohol derivatives

A - Human Necessities

61

K

260/602.3

A61K 31/13 (2006.01)

Patent

CA 1150316

PROCESS FOR THE PREPARATION OF BENZYL ALCOHOL DERIVATIVES Abstract of the Disclosure The invention relates to a process for the preparation of benzyl alcohol derivatives of the formula: Image which compounds have an excellent blood sugar lowering activity and a cardiotonic acitivity. The process com- prises subjecting an .alpha.-halogenoacetophenone derivative of the formula: Image wherein R1 is a hydroxy group-protecting group and x is a halogen atom, and a 3,4-dimethoxyphenethylamine derivative of the formula: Image wherein R2 is an amino group-protecting group, to a condensation reaction to give an .alpha.-(3,4-dimethoxyphen- ethylamino)acetophenone derivative, followed by catalytic hydrogenation thereof directly or after converting it to an .alpha.-(3,4-dimethoxyphenethylaminomethyl)benzyl alcohol derivative. This process is found to avoid the dis- advantages of the previously known processes.

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