Resolution of racemic mixtures

Details Resolution of racemic mixtures Resolution of racemic mixtures

1989-07-28

1990-11-06

Lone, Werren B.

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

Organic compounds

Carboxylic acids and salts thereof

564304, C07B 5700

Patent

active

049688375

ABSTRACT:
Racemic 2-(N-propylamino)-5-methoxytetralin is resolved by treating it with a chiral diaroyltartaric acid in an organic solvent at an elevated temperature to form a salt of the amine and chiral diaroyltartaric acid which is soluble in the solvent at the elevated temperature, cooling to precipitate the salt, isolating it, and converting it to the free amine. The product is useful as an intermediate in the synthesis of optionally-active pharmaceutical, such as N-0437.

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Brunner et al., Angew. Chem. Int. Ed. Engl., vol. 18, No. 8, pp. 620-621, (1979).
Howe et al., J. Org. Chem., vol. 50, pp. 4508-4514, (1985).
Seiler et al., Journal of Medicinal Chemistry, vol. 29, pp. 912-917, (1986).
Gerding et al., Journal of High Resolution Chromatography & Chromatography Communications, vol. 10, pp. 523-525, Sep. 1987.

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