p-Toluenesulfonic acid monohydrate → Repaglinide

Participants

Reaction Steps

102 mg (0.20 mMol) of tert.butyl (S)-2-ethoxy-4-[N-(1-(2-piperidino-phenyl)-3-methyl-1-butyl)-aminocarbonylmethyl]-benzoate (melting point: 122°-123° C.; [α]D20 =+8.7°; c=1 in methanol) are refluxed in 5 ml of benzene together with a few crystals of p-toluenesulphonic acid hydrate, for half a day. The desired product is then obtained, according to thin layer chromatography, according to the RF value and mass spectrum.

Provenance & Evidence