Epinine → N-(3-Amino-propyl)-N-[3-(2-{[2-(3,4-dihydroxy-phenyl)-ethyl]-methyl-amino}-pyrimidin-4-yl)-benzyl]-methanesulfonamide

Participants

Reaction Steps

Intermediate 4 from above was coupled with 4-(2-Methylamino-ethyl)-benzene-1,2-diol following procedure F and the resulting product deprotected following procedure G. LC-MS showed the product had the expected M+H+ of 486. 1H NMR (Varian 300 MHz, CDCl3—CD3OD, shifts relative to the solvent peak at 7.24 ppm) δ 8.2 (m, 2H) 8.0 (m, 2H) 7.6 (d, 1H) 7.5 (m, 1H) 6.6 (m, 1H) 6.4 (m, 2H) 4.4 (s, 2H) 4.0 (m, 2H) 3.2 (m, 5H) 2.9 (s, 3H) 2.8 (m, 4H) 1.7 (m, 2H).

Provenance & Evidence