US 12,391,694 B2
Process for the preparation of 2-fluoroadenine
John Y. L. Chung, Edison, NJ (US); Cynthia Marilyn Hong, Harrison, NJ (US); Guy R. Humphrey, Hillsborough, NJ (US); Kevin M. Maloney, Metuchen, NJ (US); Yingju Xu, Edison, NJ (US); and Richard J. Varsolona, Scotch Plains, NJ (US)
Assigned to Merck Sharp & Dohme LLC
Appl. No. 17/618,687
Filed by Merck Sharp & Dohme LLC, Rahway, NJ (US)
PCT Filed Jun. 18, 2020, PCT No. PCT/US2020/038304
§ 371(c)(1), (2) Date Dec. 13, 2021,
PCT Pub. No. WO2020/263660, PCT Pub. Date Dec. 30, 2020.
Claims priority of provisional application 62/865,610, filed on Jun. 24, 2019.
Prior Publication US 2022/0242866 A1, Aug. 4, 2022
Int. Cl. C07D 473/40 (2006.01)
CPC C07D 473/40 (2013.01) 10 Claims
 
1. A process of preparing compound (4),

OG Complex Work Unit Chemistry
comprising:
(a) treating compound (2)

OG Complex Work Unit Chemistry
with a substituted amine reagent and a fluoride salt to provide compound (3), wherein the substituted amine reagent is trimethylamine; and

OG Complex Work Unit Chemistry
(b) treating compound (3) with an ammonia reagent to provide compound (4).