Hydrochloric Acid → (S)-1-[3-(4-Methoxy-benzyl)-5-(2,2,2-trifluoro-ethoxy)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-7-yl]-pyrrolidin-3-ol

Participants

Reaction Conditions

Reaction Steps

A mixture of 2,2,2-trifluoroethanol (936 mg, 9.35 mmol) in THF was treated with NaH for 1 h at room temperature. (S)-1-[5-Chloro-3-(4-methoxy-benzyl)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-7-yl]-pyrrolidin-3-ol (example 109, c) was added and the mixture was stirred at 100° C. for 2 h. The reaction mixture was poured into 1 M HCl and extracted with EtOAc. The combined organic layers were dried over MgSO4 and concentrated in vacuo to yield the crude title compound which was used in the consecutive step without further purification. MS (m/e): 425.4 (MH+).

Provenance & Evidence