Process for preparing a...

C - Chemistry – Metallurgy – 07 – D

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C07D 233/60 (2006.01) C07C 62/32 (2006.01) C07C 62/34 (2006.01) C07D 521/00 (2006.01) C07F 7/18 (2006.01)

Patent

CA 1305710

ABSTRACT OF THE DISCLOSURE: A process for preparing a 2,3-dihydro-1H- imidazolylethoxyindene derivative and its pharmaceutically acceptable salts comprises eight steps. 5-methoxy-1- indanone, used as a starting compound, is converted to its corresponding cyanohydrine, followed by treatment with stannous chloride to give 2,3-dihydro-5-methoxy-1H-indene-1- carboxylic acid. Subsequent demethylation of the methoxy group and protection of the carboxylic acid group by esterification precedes formation of the corresponding 2- chloroethyl ether. Lastly, reaction with imidazole and final hydrolysis yields (2,3-dihydro-5-[.beta.-(1H-imidazol-1-yl) ethoxy]-1H-indene-1-carboxylic acid. The process produces intermediates of high purity resulting in an elevated yield of end product. The derivatives produced by the above process are useful antithrombotic agents.

556216

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