Preparation of omega-substituted alkanamide

Details Preparation of omega-substituted alkanamide Preparation of omega-substituted alkanamide

1991-03-04

1993-05-18

Lee, Mary C.

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

5483241, C07D23384, C07D40512

Patent

active

052123189

ABSTRACT:
A method for the preparation of omega-arylthioalkanamides, especially omega-imidazolylthioalkanamides useful, for example, in the preparation of certain antihypercholesterolemic agents is disclosed. The method involves three steps including an addition reaction between a lactone and an amine to produce an omega-hydroxyalkanamide; a condensation reaction between said omega-hydroxyalkanamide and an alkanesulfonic acid halide or anhydride to produce an alkanesulfonate ester; reaction of said alkanesulfonate ester with a salt of an aromatic mercaptan, especially an imidazole-2-thiol, to produce the omega-imidazolylthioalkanamides.

REFERENCES:
patent: 3271451 (1966-09-01), Tushler et al.
patent: 3536721 (1970-10-01), Soong et al.
patent: 3715363 (1973-02-01), Dickman
Kita et al., Chem. Pharm. Bull., 38 (6) 1473-1478 (1990).

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