Introduction of a new synthetic route about 1004-17-7

Statistics shows that 1004-17-7 is playing an increasingly important role. we look forward to future research findings about 2-Methylpyrimidine-4-carbaldehyde.

1004-17-7, With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.1004-17-7, name is 2-Methylpyrimidine-4-carbaldehyde, molecular formula is C6H6N2O, molecular weight is 122.1246, as common compound, the synthetic route is as follows.

Intermediate 10 (0516) (S)-Methyl 4-(2-chloro-5-methylpyridin-4-yl)-l-(2-(((2-methylpyrimidin-4- l)methyl)amino)propyl)-lH-pyrrole-2-carboxylate (0517) (0518) 2-methylpyrimidine-4-carbaldehyde (96 mg, 0.79 mmol) was added to (5)-methyl l-(2- aminopropyl)-4-(2-chloro-5-methylpyridin-4-yl)-lH-pyrrole-2-carboxylate (0519) dihydrochloride (Intermediate 3; 250 mg, 0.66 mmol) in DCM (10 mL) at 25C under nitrogen. After stirring at 40C for 3 hours, sodium triacetoxyborohydride (278 mg, 1.31 mmol) was added. The resulting mixture was stirred at 25 C for 12 hours. The reaction mixture was quenched with saturated NaHC03 (20 mL), extracted with DCM (3 x 50 mL) and dried over Na2S04, filtered and evaporated to afford a residue. The crude product was purified by flash silica chromatography (elution gradient 0 to 5% MeOH in DCM). Pure fractions were evaporated to dryness to afford (5)-methyl 4-(2-chloro-5-methylpyridin-4- yl)- 1 -(2-(((2-methylpyrimidin-4-yl)methyl)amino)propyl)- 1 H-pyrrole-2-carboxylate (Intermediate 10; 130 mg, 47.8 %) as a solid, m/z (ES+), [M+H]+ = 414.

Statistics shows that 1004-17-7 is playing an increasingly important role. we look forward to future research findings about 2-Methylpyrimidine-4-carbaldehyde.

Reference:
Patent; ASTRAZENECA AB; WARD, Richard, Andrew; JONES, Clifford, David; FERON, James, Lyman; (80 pag.)WO2017/80980; (2017); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia