Trifluoromethylthio (and sulfonyl) derivatives of cyproheptadine

Details Trifluoromethylthio (and sulfonyl) derivatives of cyproheptadine Trifluoromethylthio (and sulfonyl) derivatives of cyproheptadine

1975-12-22

1977-06-21

Jaisle, Cecilia M. S.

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

Parasitic organism or component thereof or substance...

26029362, C07D21170

Patent

active

040312224

ABSTRACT:
Cyproheptadine derivatives substituted with a trifluoromethylthio or trifluoromethylsulfonyl group in one of the benzo rings and having a hydroxyalkyl or cycloalkylalkyl group on the piperidine nitrogen are potent antipsychotic agents, with a low propensity to induce extrapyramidal side effects that are experienced with most major tranquilizers. The tranquilizing activity is predominantly in the levorotatory enantiomers, whereas the dextrorotatory enantiomers have anticholinergic activity. Each enantiomer is useful as a source of the other by racemization. The novel compounds are prepared by treatment of the corresponding iodo or bromo compound with bis(trifluoromethylthio)mercury and copper powder.

REFERENCES:
patent: 3851059 (1974-11-01), Prugh
Ebnother et al., Helv. Chim. Acta 48, 1237 (1965).

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