2,2,2-Trichloroethyl 3-tert-butyl-1-P-tolyl-1H-pyrazol-5-ylcarbamate → 1-(5-tert-Butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-{(1S,4R)-4-[1-(2-hydroxy-ethyl)-1H-indazol-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl}-urea

Participants

Reaction Steps

The title compound was prepared starting from Intermediate 11b and (5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-carbamic acid 2,2,2-trichloro-ethyl ester (Synthetic Communications, 2009, 39, 3999-4009, which is incorporated herein by reference in its entirety; 315 mg, 0.78 mmol) by using an analogous procedure to that described in Example 1 step d. LCMS (Method 5): Rt 4.99 min, m/z 578 [MH+]. 1H NMR (400 MHz, d6-DMSO): 1.22 (9H, s), 1.81-1.92 (2H, m), 2.02-2.06 (2H, m), 2.31 (3H, s), 3.74-3.75 (2H, m), 4.34 (2H, t, J 5.75), 4.78 (2H, m), 5.53 (1H, t, J 4.8), 6.28 (1H, s), 6.74 (1H, dd, J 8.75 and 2.03), 7.08 (1H, d, J 8.53), 7.27-7.28 (9H, m), 7.57 (1H, d, J 8.75), 7.89 (1H, s), 7.96 (1H, s).

Provenance & Evidence