Lithium Hydroxide → HCID 178516679, compound

Participants

Reaction Steps

Heat a solution of (3R,5S)-Trifluoro-methanesulfonic acid 3,5-dichloro-4-[2-oxo-1-(2-trifluoromethanesulfonyl-4,5,6,7-tetrahydro-2H-indazol-5-yl)-pyrrolidin-3-ylmethyl]-phenyl ester (Preparation 43) (0.10 g, 0.155 mmol) and 4-phenylpiperidine (0.063 g, 0.39 mmol) in 1-methyl-2-pyrrolidine (2.5 mL) to 201° C. for 1.5 hours in a microwave reactor. Cool the reaction to room temperature and treat with 2M LiOH (1 mL) and stir for 16 hours at room temperature. Dilute the reaction with ethyl acetate and wash with water. Dry the organic layer (Na2SO4) and remove the solvent in vacuo to afford crude product. Purify with a 0 to 5% methanol in CH2Cl2 gradient to afford 0.039 g (48%) of the title compound. MS (m/z): 523 (M+).

Provenance & Evidence