Process for the preparation of 21-hydroxy-20-keto-delta__...

C - Chemistry – Metallurgy – 07 – J

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C07J 13/00 (2006.01) C07J 33/00 (2006.01) C07J 41/00 (2006.01) C07J 43/00 (2006.01) C07J 53/00 (2006.01)

Patent

CA 1302401

ABSTRACT The invention relates to a new process for the preparation of 21-hydroxy-20-keto-.DELTA.16 steroids. A 17- isocyanosulfonylmethylene steroid is converted in one step into the new 17-(2-OR5-3-oxazolin-4-yl)-.DELTA.16 steroid using an alcohol R5OH and an aldehyde, which steroid is hydrolyzed in a subsequent step to the corresponding 21-hydroxy-20-oxo steroid. The products are known corticosteroids or inter- mediates therefor and may be applied in pharmaceutical pre- parations because of their anti-inflammatory action.

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