PROCESS FOR THE PREPARATION OF BENZYL ALCOHOL DERIVATIVES

PROCESS FOR THE PREPARATION OF BENZYL ALCOHOL DERIVATIVES

PROCESS FOR THE PREPARATION OF BENZYL ALCOHOL DERIVATIVES The invention relates to a process for the preparation of benzyl alcohol derivatives of the formula: which compounds have an excellent blood sugar lowering activity and a cardiotonic acitivity. The process comprises subjecting an .alpha.-halo...

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Bibliographische Detailangaben
Hauptverfasser: OHISHI, TOKURO, UMINO, NORIHIDE, IKEZAKI, MUNEYOSHI
Format: Patent
Sprache:eng ; fre
Schlagworte:
ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
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Zusammenfassung:PROCESS FOR THE PREPARATION OF BENZYL ALCOHOL DERIVATIVES The invention relates to a process for the preparation of benzyl alcohol derivatives of the formula: which compounds have an excellent blood sugar lowering activity and a cardiotonic acitivity. The process comprises subjecting an .alpha.-halogenoacetophenone derivative of the formula: wherein R1 is a hydroxy group-protecting group and x is a halogen atom, and a 3,4-dimethoxyphenethylamine derivative of the formula: 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 disadvantages of the previously known processes.