Process for preparing optically active benzothiazepine compound

Organic compounds -- part of the class 532-570 series – Organic compounds – Unsubstituted hydrocarbyl chain between the ring and the -c-...

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C07D28102

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active

059455330

ABSTRACT:
Powdery aggregate of 2-phenyl-1,5-benzothiazepin-3,4(2H,5H)-dione compound: ##STR1## wherein Ring A and Ring B are benzene ring having optionally substituent selected from lower alkyl, lower alkoxy and halogen, which is prepared by admixing solution of the compound (II) in polar organic solvent with solvent which does not substantially dissolve the compound (II) but is miscible with said polar organic solvent, and separating and collecting the resultant particles of the compound (II). Said aggregate of the compound (II) can be converted into optically active 3-hydroxy-2-phenyl-2,3-dihydro-1,5-benzothiazepin-4(5H)-one compounds (I) on industrial scale, which are useful as intermediate for various medicaments.

REFERENCES:
patent: 5102999 (1992-04-01), Giordano et al.
Matsumae et al., "Microbial Asymmetric Reduction of (RS)-2-(4-Methoxyphenyl)-1,5-benzothiazepin-3, 4(2H,5H)-dione, the Key Intermediate in the Synthesis of Diltiazem Hydrochloride", Journal of Fermentation and Bioengineering, vol. 79, No. 1, pp. 28-32, 1995.
Kometani et al., "Production of (2S,3S0-2,3-Dihydro-3-hydroxy-2-(4-methoxyphenyl)-1,5-benzothiazepin-4(5H) -one, a Key Intermediate for Diltiazem Synthesis," J. Fermentation and Bioengineering, vol. 84, No. 3, pp. 195-199, Mar. 1997.

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