Phosphate catalyzed acylation of steroidal tertiary alcohols

Claim 1

A process for the preparation of a compound of the formula: ##STR15## where R 6 is a hydrogen, α or β fluorine or α or β chlorine atom, or α or β methyl, methylene or β --CH 2 --N(R' 6 ) 2 group; where R' 6 is alkyl of 1 thru 3 carbon atoms, phenyl or phenyl substituted in the para position with a chlorine atom, methyl, methoxy or nitro group with the proviso that both R' 6 's cannot be aromatic; where R 9 is a hydrogen atom; where R' 11 is (H), (H,H), (H, α --OCOR), (H, β --OCOR) or (O); where R' 16 is a hydrogen atom or α or β methyl, methylene, or α --OCOR group; where R is a hydrogen atom, alkyl of 1 thru 6 carbon atoms, cycloalkyl of 5 thru 7 carbon atoms, phenyl substituted with 0 thru 3 substituents which are the same or different and are a chlorine atom or methyl, methoxy or nitro group; where is a single or double bond with the proviso that within rings A and C only one of can be a double bond, which comprises acylating a compound of the formula: ##STR16## where R 6 , R 9 , and are defined above having the same proviso as defined above; where R 11 is (H), (H,H), (H, α --OH), (H, β --OH) or (O); where R 16 is a hydrogen atom or α or β methyl, methylene or α-hydroxyl group; where R 21 is a hydrogen atom or --OCOR group, where R is defined above; with an acylating agent selected from the group consisting of compounds of the formulas (RCO) 2 O where the two R's can be connected to form a cyclic anhydride selected from the group consisting of succinic, maleic, phthalic or glutaric anhydride; or RCOX and when the acylating agent is RCOX at least 1 equivalent of a base per equivalent of RCOX is required, where X is a chlorine or bromine atom and where R is defined above, and a phosphate catalyst.