Hydrochloric Acid → HCID 178490278, compound

Participants

Reaction Steps

By proceeding in a similar manner to Example 24(a) above but substituting, (3-{2-methoxy-6-[2-(4-methoxy-phenyl)-ethylamino]-pyrimidin-4-yl}-phenyl)-acetonitrile [Example 35(s)] for 3-{2-methoxy-6-[2-(4-methoxy-phenyl)-ethylamino]-pyrimidin-4-yl}-benzonitrile, there is prepared [2-(4-methoxy-phenyl)-ethyl]-{2-methoxy-6-[3-(1H-tetrazol-5-ylmethyl)-phenyl]-pyrimidin-4-yl}-amine. This material is treated with a solution of hydrochloric acid in EtOAc followed by lyophilization to afford [2-(4-methoxy-phenyl)-ethyl]-{2-methoxy-6-[3-(1H-tetrazol-5-ylmethyl)-phenyl]-pyrimidin-4-yl}-amine hydrochloride (134 mg, Example 24(b)]. LCMS: RT=2.62 minutes, MS: 418 (M+H). 1H NMR [300 MHz, (CD3)2SO]: □9.65 (1H, brs), 7.7-7.5 (4H, m), 7.2 (2H, d, J=8.4 Hz), 6.87 (2H, d, J=8.4 Hz), 6.68 (1H, s), 4.4 (2H, s), 4.08 (3H, s), 3.71 (3H, s), 3.6 (2H, m), 2.85 (2H, t, J=7.2 Hz). IC50=0.1 nM

Provenance & Evidence