Process for racemizing an enantiomer of 5,6-dihydro-4-alkylamino

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

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C07D49506

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active

050119427

ABSTRACT:
Compounds classified as 5,6-dihydro-4-alkylamino-4H-thieno (or furo) [2,3-b]thiopyran-2-sulfonamide-7,7-dioxide are carbonic anhydrase inhibitors useful in the treatment of ocular hypertension, and most of the carbonic anhydrase inhibitory activity resides in only one of the enantiomers. The undesired enantiomer is utilized by racemization by thermolysis of an N-acyl derivative in a basic environment followed by removal of the acyl group. The racemate may then be resolved into the enantiomers.

REFERENCES:
patent: 4096186 (1978-06-01), Ichikawa et al.
patent: 4226803 (1980-10-01), Klingler et al.
patent: 4252744 (1981-02-01), Bison et al.
patent: 4339603 (1982-07-01), Raghu et al.
patent: 4677115 (1987-06-01), Baldwin et al.

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