Process for the preparation of steroidal 17.alpha.-arylcarboxyla

Details Process for the preparation of steroidal 17.alpha.-arylcarboxyla Process for the preparation of steroidal 17.alpha.-arylcarboxyla

1981-05-13

1982-04-06

Roberts, Elbert L.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

C07J 100

Patent

active

043235123

ABSTRACT:
17-Arylcarboxylate esters of 9,11-unsubstituted 4-pregnene-17.alpha.,21-diol-3,20-diones are prepared by reaction of the corresponding 17.alpha.-hydroxy derivative with alkyl lithium and an anhydride or acyl halide reagent in the presence of 4-(di-lower alkyl)aminopyridine at low temperatures. A preferred mode of the process is the preparation of 16.beta.-methyl-1,4-pregnadiene-17.alpha.,21-diol3,20-dione 17.alpha.-m-iodobenzoate 21-benzoate, a valuable intermediate in the manufacture of betamethasone.

REFERENCES:
patent: 4252719 (1981-02-01), Breslow et al.
patent: 4260464 (1981-04-01), Kerb et al.

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