Organic compounds -- part of the class 532-570 series – Organic compounds – Unsubstituted hydrocarbyl chain between the ring and the -c-...
Patent
1989-11-20
1990-10-16
Bond, Robert T.
Organic compounds -- part of the class 532-570 series
Organic compounds
Unsubstituted hydrocarbyl chain between the ring and the -c-...
510 17, 562431, C07D28110
Patent
active
049636715
ABSTRACT:
This process enables preparation of the preferred (+)-threo enantiomer by resolution of its racemic mixture of a compound of the formula ##STR1## wherein Y.sup.1 and Y.sup.2 are each independently lower alkyl and R.sup.1 is hydrogen or lower alkyl. The compound is treated with a chiral acid (tartaric aicd preferred) in an organic solvent (ethanol preferred) to yield the (+)-threo enantiomer, which is then recovered from the reaction mixture. This enantiomer may then be used to produce the preferred (+)-cis enantiomer of certain benzothiazepine cardiovascular agents.
REFERENCES:
patent: 3562257 (1971-02-01), Kugita et al.
Kugita et al., "Synthesis of 1,5-Benzothiazepine Derivatives", I Chem. Pharm. Bull. vol. 19 pp. 2028 to 2037 (1970).
Barrack Donald J.
Bond Robert T.
E. R. Squibb & Sons Inc.
Gaul Timothy J.
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