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

Beteiligte Stoffe

Reaktionsschritte

Following the procedure described in Example 14, making variations as required to replace 4-fluoro-N-methyl-benzylamine with (4-difluoromethoxy-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 80% yield. 1H NMR (400 MHz, CD2Cl2) δ 8.58 (s, 1H), 8.07 (s, 1H), 7.26-7.37 (m, 4H), 7.00-7.11 (m, 4H), 6.51 (bt, J=76, 64 Hz, 1H, CH—F signal), 6.16 (bs, 1H), 4.82 (s, 2H), 4.54 (d, J=8.0 Hz, 2H), 3.14 (s, 3H), 2.70 (s, 3H); MS (ES+) m/z 514.2 (M+1), Rt=1.63 min.

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