Back to results
US 12,391,694 B2Granted
Process for the preparation of 2-fluoroadenine
AssigneeMerck Sharp & Dohme Corp.
InventorsJohn Y. L. Chung, Cynthia Marilyn Hong, Guy R. Humphrey, Kevin M. Maloney, Yingju Xu, Richard J. Varsolona
Life of this patent
Estimating the term…
Abstract
The present invention provides processes for the preparation of 2-fluoroadenine, as well as certain intermediates useful in the preparation of 2′-deoxy-4′-C-ethynyl-2-fluoroadenosine (EFdA): EFdA.
Claims10
A process of preparing compound (4),
- comprising:
- (a) treating compound (2)
- with a substituted amine reagent and a fluoride salt to provide compound (3), wherein the substituted amine reagent is trimethylamine;
- and
- (b) treating compound (3) with an ammonia reagent to provide compound (4).
2 more elements
A process of preparing 2-fluoroadenine
- comprising:
- (a) treating compound (2)
- with a substituted amine reagent and a fluoride salt to provide compound (3)
- (b) treating compound (3) with an ammonia reagent to provide compound (4)
- and
- (c) treating compound (4) with an acid to provide 2-fluoroadenine.
3 more elements
A process for the preparation of 4′-ethynyl-2-fluoro-2′-deoxyadenosine (EFdA)
- (a) treating compound (2)
- with a substituted amine reagent and a fluoride salt to provide compound (3);
- (b) treating compound (3) with an ammonia reagent to provide compound (4)
- and
- (c) converting compound (4) to EFdA.
2 more elements
Dependencies are inferred from the claim text.