Smithkline Beecham Corporation

Neil Howard Baine

Robert John Mills

Conrad John Kowalski

Michael Anthony McGuire

William Morrow Clark

Yemane Woldeselassie Andemichael

Robert L Webb

Gary Edward Zuber

Donald Nathaniel Klein

Neville Lewis Holder

Marvin Sungwhan Yu

Ann Marie Eldridge

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

This invention relates to a process for making certain phenyl urea compounds by using a Lewis acid to effect the ring opening of a benzoxazolinone by an amine.

Process for preparing certain phenyl urea compounds

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

Polymorph 'A' a novel polymorphic form of N-t-butyl-androst-3,5-diene-17.beta.-carboxamide-3-carboxylic acid. Novel processes for preparing polymorph 'A' are also disclosed.

'N-T-butyl-androst-3-5-diene-17 .beta.-carboxamide-3-carboxylic' acid

N-t-butyl-androst-3,5-diene-17.beta.-carboxamide-3-carboxylic acid

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Merion, PA, United States of America

Neil Howard Baine