Sepracor, Inc.

Pharmacia Corporation

G.d. Searle LLC

Robert Hett

Chris Hugh Senanayake

Samuel J Tremont

Yun Gao

Mark John Pozzo

Jon P Lawson

Kevin J Koeller

Claire A Przybyla

James C Peterson

Stephen Alan Wald

Payman N Farid

Kevin Babiak

Pierre-Jean Colson

Grace Mary Wagner

Benxin Zhi

Jay S Trivedi

Kevin Q Fang

Gerald A Weisenburger

Andrew Carpenter

Eduardo K Mar

Vladislav Orlovski

Lawrence M Miller

Shine Chou

Christian H Huber

James J Li

Martin P Redmon

James Li

Among its several embodiments, the present invention provides an improved process for the preparation of tetrahydrobenzothiepine-1,1-dioxide compounds; the provision of a process for preparing a diastereomeric mixture of tetrahydrobenzothiepine-1,1-dioxide compounds from a single diastereomer of such compounds; the provision of a process for the preparation of 3-bromo-2-substituted propionaldehyde compounds; and the provision of a process for the preparation of 3-thio-2-substituted propionaldehyde compounds.

Method for the preparation of tetrahydrobenzothiepines

A method is disclosed for the preparation of optically pure isomers of formoterol by the reaction of an optically pure 4-benzyloxy-3-formamidostyrene oxide with an optically pure 4-methoxy-&agr;-methyl-N-(phenylmethyl)benzeneethanamine followed by debenzylation. Useful intermediates in the process are also disclosed, as are the novel L-tartrate salt of R,R-formoterol and pharmaceutical compositions thereof.

Formoterol process

A method is disclosed for the preparation of optically pure isomers of formoterol by the reaction of an optically pure 4-benzyloxy-3-formamidostyrene oxide with an optically pure 4-methoxy-.alpha.-methyl-N-(phenylmethyl)benzeneethanamine followed by debenzylation. Useful intermediates in the process are also disclosed, as are the novel L-tartrate salt of R,R-formoterol and pharmaceutical compositions thereof.

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Aarau, Switzerland

Robert Hett