Preparation of mibefradil via an acetamide anion

Details Preparation of mibefradil via an acetamide anion Preparation of mibefradil via an acetamide anion

1998-04-14

1998-09-15

Stockton, Laura L.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C07D23514

Patent

active

058080880

ABSTRACT:
A method of preparing opyl-1,2,3,4-tetrahydronaphthalen-2-yl methoxyacetate comprises contacting 6-fluoro-1-isopropyl-3,4-dihydro-1H-naphthalen-2-one with the dianion of ,4-tetrahydronaphthalen-2-yl)-N-methylacetamide, reducing this to pyl-1,2,3,4-tetrahydronaphthalen-2-ol, and treating the pyl-1,2,3,4-tetrahydronaphthalen-2-ol with methoxyacetic acid or an activated derivative of methoxyacetic acid. The invention is particularly applicable to the preparation of mibefradil, 1-isopropyl-1,2,3,4-tetrahydronaphthalen-2-yl methoxyacetate, and its dihydrochloride salt. ,2,3,4-tetrahydronaphthalen-2-ol dioxalate, are new.

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