Methylamine → 1,1,1-trifluoro-2-(4-((2S)-2-((methylamino)methyl)-4-(2-thiophenylsulfonyl)-1-piperazinyl)phenyl)-2-propanol

Participants

Reaction Steps

This compound was synthesized following the procedure outlined for Example 84 The reaction of ((2R)-4-(2-thiophenylsulfonyl)-1-(4-(2,2,2-trifluoro-1-hydroxy-1-methylethyl)phenyl)-2-piperazinyl)methyl methanesulfonate (Intermediate B) and methanamine (10 equivalents of a 1.0M solution in THF, Sigma-Aldrich, St. Louis, Mo.) followed by purification via column chromatography on silica gel (0 to 10% MeOH in CH2Cl2) delivered 1,1,1-trifluoro-2-(4-((2S)-2-((methylamino)methyl)-4-(2-thiophenylsulfonyl)-1-piperazinyl)phenyl)-2-propanol as a mixture of two isomers after column chromatography on silica gel (0-10% MeOH in CH2Cl2)

Provenance & Evidence