2-Methylnicotinic acid → 1-Ethyl-3-(4-(7-(2-methylnicotinoyl)-4-morpholino-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-yl)phenyl)urea

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Reaction Steps

The compound oy was obtained following the general procedure in Example 213, substituting 3-methyloxetane-3-carboxylic acid for 2-methylnicotinic acid and substituting (S)-1-ethyl-3-(4-(4-(3-methylmorpholino)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-yl)phenyl)urea hydrochloride salt (jk) for 1-ethyl-3-(4-(4-morpholino-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-yl)phenyl)urea hydrochloride salt (bf). The desired product oy (74 mg, 58% yield) was obtained as white solid: 1H NMR (400 MHz, DMSO) δ 8.64 (s, 1H), 8.20 (m, 2H), 7.42 (m, 2H), 6.15 (m, 1H), 4.61 (m, 2H), 3.82 (m, 1H), 3.73 (m, 4H), 3.49 (m, 5H), 3.20-3.04 (m, 2H), 2.76 (m, 2H), 2.53 (s, 3H, overlapping with DMSO peak), 1.06 (t, J=7.1 Hz, 3H); LC-MS m/z=502 (M+H).

Provenance & Evidence