Sterling Drug Inc.

John L Herrmann, Jr

Malcolm R Bell

Chester J Opalka, Jr

Robert G Christiansen

Vahan Akullian

1'-Sulfonylsteroido[3,2-c]pyrazoles, for example, (5.alpha.,17.alpha.)-1'-(methylsulfonyl)-1'H-pregn-20-yno[3,2-c]pyrazol-17 -ol, which are useful as antiandrogenic agents, and processes for preparation, method of use and compositions thereof are disclosed.

Antiandrogenic sulfonylsteroidopyrazoles and processes for preparation

Compounds of the formula ##STR1## where R is hydrogen, methyl, ethyl, propyl, 2-propenyl or 2-propynyl; and R' is hydrogen or fluoro possess anti-inflammatory activity. The compounds where R is H are prepared by reacting a compound of the formula ##STR2## with (1H,3H)-pyrimidine-2,4,5,6-tetrone. The compounds where R is other than hydrogen are prepared by reacting a compound where R is hydrogen with the appropriate alkylating agent.

Pentacyclic phenylpyrazole compounds as anti-inflammatory agents

The compounds of formula ##STR1## where R is hydrogen or fluorine possess glucocorticoid activity, and are prepared by reacting a compound of the formula ##STR2## with 1,2,3-indantrione.

Anti-inflammatory

5-Ethenyl-4,4a,7,8-tetrahydro-4a-methyl-2(3H)-naphthalenone, an intermediate useful in the total synthesis of steroids, is prepared by dehydrohalogenation of 5-(2-bromoethylidene)-2(3H)-4a-methyl-4,4a,5,6,7,8-hexahydronaphthalen-2-o ne by a pyrolytic procedure or by means of dehydrohalogenating agents, for example, a mixture of lithium bromide and lithium carbonate.

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Kinderhook, NY, United States of America

John L Herrmann, Jr