Trifluoroacetic acid → (3R,5S)-5-(benzylamino-methyl)-1-methanesulfonyl-pyrrolidine-3-thiol trifluoro-acetate

Participants

Reaction Conditions

Reaction Steps

(Method 2): 100 mg (0.24 mmol) of (2S,4R)-benzyl-[1-methanesulfonyl-4-(4-methoxy-benzylsulfanyl)-pyrrolidin-2-ylmethyl]-amine was dissolved in 8.5 ml TFA and treated at 0° C. with 0.38 ml (2.38 mmol) triethylsilane. The reaction was warmed up over night, heated 1.5 h at 80° C. and evaporated, partitioned between water (10 ml)/Et2O (2×10 ml). The water was lyophilized to give 90 mg (91%) of (3R,5S)-5-(benzylamino-methyl)-1-methanesulfonyl-pyrrolidine-3-thiol trifluoro-acetate, MS: 301 (MH+).

Provenance & Evidence