R(-)-およびS(+)-5-[2-[[2-(2-エトキシフェノキシ)エチル]アミノ]プロピル]-2-メトキシベンゼンスルホンアミドの分離方法

Japanese Patent JP2005533094

A

The process for separating the R(-)- and S(+)-5-Ä2-ÄÄ2-(2-ethoxyphenoxy)ethylÜaminoÜpropylÜ-2-methoxybenzene-sulfonamide enantiomers comprises (a) reacting a mixture of said enantiomers with an optically active organic acid to form .diastereoisomeric salts with said enantiomers, where in said diastereoisomeric salts have different solubility and can be separated by crystallization; (b) separating the diastereoisomeric salt mixture enriched in the salt of one of the enantiomers; and (c) releasing said salts to obtain the R(-)or S(+) enantiomer. The R(-)-5-Ä2-ÄÄ2-(2-ethoxyphenoxy) ethylÜaminoÜpropylÜ-2-methoxybenzenesulfonamide enantiomer has alpha -adrenergic blocking activity and is useful as an antihypertensive agent suitable for the treatment of congestive heart failure and benign prostatic hypertrophy.

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Christina Blanco Fernandez
Antonio Lorente Bonde-Larsen
Holge Martin Juárez
Louis Octavio Silva Gizasora

JP2004520689A

November 04, 2005

July 11, 2003

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Ragitives, S.L.

C07B57/00; C07C303/40; C07C303/44; C07C311/37; (IPC1-7): C07C303/44; C07B57/00; C07C303/40; C07C311/37

JPS6327471A	1988-02-05
JPS57136561A	1982-08-23
JPH02149554A	1990-06-08
JPS56110665A	1981-09-01

WO2003037850A1

2003-05-08

Makoto Hagiwara

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