Trifluoroacetic acid → 3-(4-(3-(4-fluorophenoxy)azetidin-1-yl)pyrimidin-2-ylamino)-N-methylbenzamide

Participants

Reaction Conditions

Reaction Steps

To 2-chloro-4-(3-(4-fluorophenoxy)azetidin-1-yl)pyrimidine (90.0 mg, 0.322 mmol) and 3-amino-N-methylbenzamide (53.2 mg, 0.354 mmol) in a disposable sealed tube in 2-propanol (2.50 mL) was added trifluoroacetic acid (0.074 mL, 0.965 mmol). The resulting reaction mixture was heated at 84° C. for 18 h, cooled to RT, concentrated, taken up in MeOH-DCM, filtered through an SCX-2 column with MeOH. The product was eluted with 2.0 M NH3 in MeOH. Fractions containing the product were concentrated to afford 3-(4-(3-(4-fluorophenoxy)azetidin-1-yl)pyrimidin-2-ylamino)-N-methylbenzamide (123.9 mg).

Provenance & Evidence