Antipsychotic 3-trifluoromethylsulfinyl analogs of cyproheptadin

Details Antipsychotic 3-trifluoromethylsulfinyl analogs of cyproheptadin Antipsychotic 3-trifluoromethylsulfinyl analogs of cyproheptadin

1977-12-01

1979-01-02

Jiles, Henry R.

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

Parasitic organism or component thereof or substance...

546204, C07D21124, A61K 31445

Patent

active

041327969

ABSTRACT:
Cyproheptadine derivatives substituted with a trifluoromethylsulfinyl group in one of the benzo rings and having an alkyl group, either unsubstituted or substituted with a hydroxy or cycloalkyl 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 novel compounds are generally prepared by treatment of the intermediate 5-carbinol with a dehydrating reagent, or by alkylation of the piperidine nitrogen with the appropriate alkyl or substituted alkyl group.

REFERENCES:
patent: 3014911 (1961-12-01), Engelhardt
patent: 3862156 (1975-01-01), Bourquin et al.
patent: 4031222 (1977-06-01), Remy
Migrdichian, V., Organic Synthesis, vol. 1, Reinhold Pub. Corp., NY, 1957 pp. 465-467.
Yagupolskii, L. et al., Zm. Obshch. Khim. 35(2), 377-387 (1965) [Chemical Abstracts 62:14551a (1965)].
Orda, V. et al., Dopovidi Akad. Nauk. UKR RSR 1965(3), 345-348 [Chemical Abstracts, 63:1684g (1965)].
Syrova, G. et al., Zh. Org. Khim. 1970, 6(11), 2285-2289 [Chemical Abstracts, 74:52873j (1971)].

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