Dimethylsulphamoyl chloride → Rac-n-(3-{4-[5-(5-diethylaminomethyl-4-methyl-thiophen-2-yl)-[1,2,4]oxadiazol-3-yl]-phenyl}-2-hydroxy-propyl)-sulfamic acid dimethyl-amide

Participants

Reaction Steps

The title compound (21 mg) is prepared in analogy to Example 166 starting from rac-1-amino-3-{4-[5-(5-diethylaminomethyl-4-methyl-thiophen-2-yl)-[1,2,4]oxadiazol-3-yl]-phenyl}-propan-2-ol (50 mg, 125 μmol) and dimethylsulfamoyl chloride (22 mg, 150 μmol); LC-MS: tR=0.76 min; [M+1]+=508.18; 1H NMR (CDCl3): δ1.11 (t, J=7.0 Hz, 6H), 2.25 (s, 3H), 2.64 (q, J=7.0 Hz, 4H), 2.83 (s, 6H), 2.85-2.94 (m, 2H), 3.03-3.10 (m, 1H), 3.24-3.30 (m, 1H), 3.73 (s, 2H), 4.04-4.11 (m, 1H), 7.37 (d, J=8.3 Hz, 2H), 7.66 (s, 1H), 8.10 (d, J=8.3 Hz, 2H).

Provenance & Evidence