Smithkline Beecham Corporation

William Morrow Clark

Robert John Mills

Conrad John Kowalski

Michael Anthony McGuire

Neil Howard Baine

Yemane Woldeselassie Andemichael

Ivan Lantos

Lendon Norwood Pridgen

Ann Marie Tickner

Invented is an improved process for preparing aromatic ring-fused cyclopentane derivatives. Preferred compounds prepared by this invention are indane carboxylates and cyclopentano&lsqb;b&rsqb;pyridine derivatives. The most preferred compounds prepared by this inventino are (&plus;)(1S, 2R, 3S)-3-&lsqb;2-(2-hydroxyeth-1-yloxy)-4-methoxyphenyl&rsqb;-1-(3,4-methylenedioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof and (&plus;)(1S, 2R, 3S)-3-&lsqb;(2-carboxymethoxy-4-methoxyphenyl)-1- (3,4-methylenedioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof. Also invented are novel intermediates useful in preparing these compounds.

Process of making 3-phenyl-1-methylenedioxyphenyl-indane-2-carboxylic acid derivatives

Invented is an improved process for preparing aromatic ring-fused cyclopentane derivatives. Preferred compounds prepared by this invention are indane carboxylates and cyclopentanopyridine derivatives. The most preferred compounds prepared by this invention are (&plus;)(1S, 2R, 3S)-3-&lsqb;2-(2-hydroxyeth-1-yloxy)-4-methoxyphenyl&rsqb;-1-(3,4-methylenedioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof and (&plus;)(1S, 2R, 3S)-3-(2-carboxymethoxy-4-methoxyphenyl)-1-(3,4-methylenedioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof. Also invented are novel intermediates useful in preparing these compounds.

process of making 3-phenyl-1-methylenedioxyphenyl-indane-2-carboxylic acid derivatives

Invented is an improved process for preparing aromatic ring-fused cyclopentane derivatives. Preferred compounds prepared by this invention are indane carboxylates and cyclopentano&lsqb;b&rsqb;pyridine derivatives. The most preferred compounds prepared by this invention are (&plus;)(1S, 2R, 3S)-3-&lsqb;2-(2-hydroxyeth-1-yloxy)-4-methoxyphenyl&rsqb;-1-(3,4-methylenedioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof and (&plus;)(1S, 2R, 3S)-3-(2-carboxymethoxy-4-methoxyphenyl)-1-(3,4-methylenedioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof. Also invented are novel intermediates useful in preparing these compounds.

Process of making 3-phenyl-1-methylenedioxyphenyl-indane-2-carboxylic

3-phenyl-1-methylenedioxyphenyl-indane-2-carboxylic acid derivatives

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Philadelphia, PA, United States of America

William Morrow Clark