Process for dehydrating corticosteroid intermediates

C - Chemistry – Metallurgy – 07 – J

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C07J 43/00 (2006.01) C07J 41/00 (2006.01)

Patent

CA 2069645

2069645 9108218 PCTABS00005 A process for preparing oxazoline corticosteroid intermediates of formula (V) wherein R1 represents hydrogene (H), loweralkyl, phenyl or phenylalkyl; R4 represents H or loweralkyl, preferably methyl having either the .alpha. or .beta. stereochemistry; and R9 represents hydrogen, fluoro, chloro or loweralkyl. The process comprises contacting a compound of formula (III) herein, with (A) Vilsmeier reagent, followed by acid hydrolysis to yield the compound of formula (V); or alternatively, (B) an acid having a pKa of less than 5, to yield the compound of formula (V).

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