Water → (S)-6-(3-Methoxypyrrolidin-1-yl)-2-phenylpyrimidine-4-carboxylic acid

Participants

Reaction Conditions

Reaction Steps

6-chloro-2-phenyl-pyrimidine-4-carboxylic acid (14.3 g; prepared as described in WO 2006/114774, Example 24, intermediate 24.3), intermediate 1.7 (10 g) and DIPEA (23 mL) were dissolved in THF (191 mL). The reaction mixture was stirred at 60° C. for 48 h. Water and DCM were added and the phases were separated. The aq. phases were washed with DCM and the combined org. phases were dried (Na2SO4) and evaporated off. CC (DCM/MeOH 9/1) of the crude yielded the desired compound (13.2 g).

Provenance & Evidence