Process for the preparation of 17-esters of 9 .alpha., 21-dihalo

Details Process for the preparation of 17-esters of 9 .alpha., 21-dihalo Process for the preparation of 17-esters of 9 .alpha., 21-dihalo

1997-06-25

1999-03-23

Dees, JoseG.

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

Organic compounds

Cyclopentanohydrophenanthrene ring system containing

552574, 552576, C07J 500

Patent

active

058862005

ABSTRACT:
The invention provides an improved process for the preparation of 17-esters of 9.alpha.,21 -dihalo-pregnane-11.beta.,17.alpha.-diol-20-ones, and in particular for the preparation of 17-esters of anti-inflammatory steroids according to the following scheme: ##STR1## wherein RCO, R.sup.1, X, Y and the dotted line are as defined in the specification. The novel process is especially suitable for the preparation of Mometasone Furoate.

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patent: 4472393 (1984-09-01), Shapiro
Hesk et al., Synthesis of Tritium Labelled Mometasone Furoate, J. Labelled Compds Radiopharm., vol. 33(5), pp. 439-442, 1993.
Popper et al., J. steroid Biochem., 1987, 27 No. 4-6, pp. 837-843: "Structure-Activity Relationships of a Series of Novel Topical Corticosteroids".
Puar et al., Steroids, 1995, 60, pp. 612-614: An unusual rearrangement product formed during production of mometasone furoate (Sch 32088).
Shapiro et al., J. Med. Chem., 1987, 30, pp. 1581-1588: "17-Heteroaroyl Esters of Cortico-steroids. 2. 11.beta.-Hydroxy Series".
Abstract of Netherlands Patent Application 8400910.

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