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US 9,315,541 B2Granted
Process for the preparation of unsaturated trifluoromethanesulfonate steroid derivatives
AssigneeOlon S.P.A.
InventorsMarco Alpegiani, Tania Cristiano
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Abstract
Disclosed is a method for the conversion of a compound of formula 3 to a compound of formula 4, wherein R is an acetyl group or an alcohol-protecting group. The process involves reacting 3 with a triflating agent in the presence of a nicotinate (3-pyridinecarboxylate) of a C1-C4 alcohol, preferably methyl nicotinate (methyl 3-pyridinecarboxylate) or ethyl nicotinate (ethyl 3-pyridinecarboxylate), to give 4. The method can be conveniently used in a process for the preparation of Abiraterone or Abiraterone acetate.
Claims8
A process for the conversion of a compound of formula 3,
- wherein R is an acetyl group or an alcohol-protecting group, to a compound of formula 4
- wherein R is as defined above, comprising the reaction of 3 with a triflating agent in the presence of a C1-C4 alkyl nicotinate (3-pyridinecarboxylate),
- and wherein the triflating agent is trifluoromethanesulphonic anhydride.
Dependencies are inferred from the claim text.