Ethanolamine → Rac-1-{4-[5-(5-diethylaminomethyl-4-methyl-thiophen-2-yl)-[1,2,4]oxadiazol-3-yl]-phenyl}-3-(2-hydroxy-ethylamino)-propan-2-ol

Participants

Reaction Steps

The title compound (16 mg) is prepared starting from rac-methanesulfonic acid 3-{4-[5-(5-diethylaminomethyl-4-methyl-thiophen-2-yl)-[1,2,4]oxadiazol-3-yl]-phenyl}-2-hydroxy-propyl ester (100 mg, 208 μmol) and ethanolamine (64 mg, 1.04 mmol) in analogy to Example 168 step b); LC-MS: tR=0.63 min; [M+1]+=445.07; 1H NMR (CDCl3): δ1.10 (t, J=7.0 Hz, 6H), 2.25 (s, 3H), 2.53 (s br, 2H), 2.59-2.67 (m, 5H), 2.77-2.90 (m, 5H), 3.69 (t, J=5.0 Hz, 2H), 3.72 (s, 2H), 3.95-4.03 (m, 1H), 7.37 (d, J=8.3 Hz, 2H), 7.66 (s, 1H), 8.08 (d, J=8.0 Hz, 2H).

Provenance & Evidence