Preparation of mibefradil via a naphthalenylacetic acid

Details Preparation of mibefradil via a naphthalenylacetic acid Preparation of mibefradil via a naphthalenylacetic acid

1998-04-14

1998-09-22

Stockton, Laura L.

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C07D23514

Patent

active

058115560

ABSTRACT:
A method of preparing pyl-1,2,3,4-tetrahydronaphthalen-2-yl methoxyacetate comprises contacting (6-fluoro-2-hydroxy-1-isopropyl-1,2,3,4-tetrahydronaphthalen-2-yl)acetic acid or an activated derivative of (6-fluoro-2-hydroxy-1-isopropyl-1,2,3,4-tetrahydronaphthalen-2-yl)acetic propyl!-2-(6-fluoro-2-hydroxy-1-isopropyl-1,2,3 ,4-tetrahydronaphthalen-2- yl)-N-methylacetamide, reducing this to pyl-1, 2,3,4-tetrahydronaphthalen-2-ol, and treating the propyl!-methylamino}ethyl!-6-fluoro-1-isopropyl-1,2,3,4-tetrahydronaphthal en-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-yl)-N-methylacetamide is new.

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