Process for preparing 21-desoxyprednisolone 17-esters

Details Process for preparing 21-desoxyprednisolone 17-esters Process for preparing 21-desoxyprednisolone 17-esters

1990-10-12

1992-10-27

Bond, Robert T.

Organic compounds -- part of the class 532-570 series

Organic compounds

Cyclopentanohydrophenanthrene ring system containing

552581, C07J 7500, C07J 700

Patent

active

051590913

ABSTRACT:
A process for preparing 21-desoxyprednisolone 17-esters of formula (IV) is disclosed. ##STR1## The process comprises reacting a prednisolone 17.alpha.,21-cyclic orthoester with an acid in a 40-60% lower alcohol solution to produce a prednisolone 17-ester, sulfonylating the prednisolone 17-ester into a prednisolone 17-ester 21-sulfonate, and reacting the sulfonate with an alkali metal iodide in methyl ethyl ketone in the presence of a lower fatty acid to produce the compound of formula (IV). The process ensures economical industrial production of high purity 21-desoxyprednisolone 17-esters, an excellent local anti-inflammatory medicine, in a high yield by simple procedures.

REFERENCES:
patent: 3499081 (1970-03-01), Krakower et al.
patent: 3639434 (1972-02-01), Oxley et al.
patent: 3980680 (1976-09-01), Green
Carey and Sundberg Advanced Organic Chemistry Part A [N.Y., Plenum Press, 1984] pp. 212 to 215.
The Merck Index, 11th Ed. [Merck and Co., Rahway, N.J., 1989] p. 1358, entry 8533.
Chemical Abstracts, vol. 66, No. 7, Feb. 13, 1967, p. 2777, abstract No. 28973f, Columbus, Ohio, US; R. Vitali et al: "Substituted 17 alpha-hydroxyprogesterone esters. New synthetic routes and new derivatives", & Gazz. Chim. Ital. 96(8-9), 1115-24(1966).

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