Diethanolamine → HCID 59371676, compound

Participants

Reaction Steps

3-[2-[5-[[1-(tert-Butoxycarbonyl)-(2S)-azetidinyl]methoxy]-3-pyridyl]ethyl]phenylmethylamine and triethylamine (1-2 equiv.) are dissolved in anhydrous CH2Cl2, and with exclusion of moisture and ice cooling a solution of methanesulfonyl chloride (1-1.5 equiv.) in CH2Cl2 is added dropwise. The mixture is stirred in the ice bath until no more starting amine is observed, then diethanolamine (0.2-0.7 equiv.) is added to quench the excess of methanesulfonyl chloride. The reaction mixture is evaporated and the residue chromatographed on silica gel with CH2Cl2/methanol. The product-containing fractions are evaporated, and the residue is dried in vacuo to obtain the sulfonamide.

Provenance & Evidence