1,2-Dichloroethane → 6-Chloro-N-[(4,6-dimethyl-2-oxo-1,2-dihydro-3-pyridinyl)methyl]-3-methyl-1-(1-methylethyl)-1H-pyrazolo[3,4-b]pyridine-4-carboxamide

関与物質

反応手順

The title compound was prepared in the same manner as described in example 17 using 6-chloro-3-methyl-1-(1-methylethyl)-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid (486.6 mg, 1.92 mmol), 3-(aminomethyl)-4,6-dimethyl-2(1H)-pyridinone HCl (489 mg, 2.59 mmol), 1-hydroxy-7-azabenzotriazole (392 mg, 2.88 mmol), N-methylmorpholine (0.84 ml, 7.67 mmol) and EDC (552 mg, 2.88 mmol). An additional 10 mL DMSO was added to the reaction mixture to facilitate stirring, and 10% K2CO3 was used instead of 50% aq. NaOH during the work up. LCMS E-S (M+H)=388.1. 1H NMR (400 MHz, DMSO-d6) δ ppm 1.44 (d, 6H), 2.12 (s, 3H), 2.22 (s, 3H), 2.40 (s, 3H), 4.34 (d, J=5.05 Hz, 2H), 5.05 (quin, J=6.63 Hz, 1H), 5.88 (s, 1H), 7.16 (s, 1H), 8.78 (t, J=4.93 Hz, 1H), 11.53 (br. s., 1H).

情報源と証拠