Process for the separation of R(-)-and...

Details Process for the separation of R(-)-and... Process for the separation of R(-)-and...

2006-09-12

2006-09-12

O'Sullivan, Peter (Department: 1621)

Organic compounds -- part of the class 532-570 series

Organic compounds

Amino nitrogen containing

C562S100000, C562S401000, C562S435000

Reexamination Certificate

active

07105698

ABSTRACT:
The process for separating the R(−)- and S(+)-5-[2-[[2-(2-ethoxyphenoxy)ethyl]amino]propyl]-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-[2-[[2-(2-ethoxyphenoxy) ethyl]amino]propyl]-2-methoxybenzenesulfonamide enantiomer has α-adrenergic blocking activity and is useful as an antihypertensive agent suitable for the treatment of congestive heart failure and benign prostatic hypertrophy.

REFERENCES:
patent: 5447958 (1995-09-01), Niigata et al.
patent: 2003/0109752 (2003-06-01), Hoorn et al.
patent: 290 708 (2002-01-01), None
patent: 2 000 382 (1988-02-01), None
patent: 2 029 838 (1992-10-01), None
patent: WO 03/037856 (2003-05-01), None

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