1-(4-fluorophenyl)-N-methylmethanamine → 2-{6-[(3-Methoxy-benzyl)-methyl-amino]-pyrazin-2-yl}-4-methyl-thiazole-5-carboxylic acid 4-fluoro-benzylamide

Participants

Reaction Steps

Following the procedure described in Example 14, making variations as required to replace 4-fluoro-N-methyl-benzylamine with (3-methoxy-benzyl)-methyl-amine to react with 2-(6-iodo-pyrazin-2-yl)-4-methyl-thiazole-5-carboxylic acid 4-fluoro benzylamide, the title compound was obtained in 75% yield. 1H NMR (400 MHz, CD2Cl2) δ 8.55 (s, 1H), 8.07 (s, 7.27-7.37 (M, 2H), 7.18-7.26 (m, 1H), 6.90-7.08 (m, 2H), 6.70-6.88 (m, 3H), 6.21 (bs, 1H), 4.79 (s, 2H), 4.53 (d, J=4.0 Hz, 2H), 3.72 (s, 3H), 3.15 (s, 3H), 2.69 (s, 3H); MS (ES+) m/z 478.2 (M+1), Rt=1.58 min.

Provenance & Evidence