Application of Picolinimidamide

In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles. 52313-50-5, Picolinimidamide, other downstream synthetic routes, hurry up and to see.

Synthetic Route of 52313-50-5 ,Some common heterocyclic compound, 52313-50-5, molecular formula is C6H7N3, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route.

A mixture of 1-(4-benzyloxy-3-fluoro-phenyl)piperidin-4-one (4.17 g, 13.94 mmol) and DMFDMA (20 mL) in acetonitrile (10 mL) was heated with stirring at 90 C for 2 hrs. The resulting reaction mixture was concentrated in vacuo and the residue was dissolved in EtOH (40mL). To the solution was added pyridine-2-carboxamidine (1.8 g, 14.96 mmol) and potassium carbonate (4.1 g, 2992 mrnol) successively. After being heated with stirring at 90 C overnight, the resulting reaction mixture was cooled to rt, diluted with water (60 mL) and extracted with EA (30 mL) for three times. The combined organic layer was washed with brine, dried over anhydrous Na2SO4 and concentrated in vacuo. The residue was purified by columnchromatography (eluting with 5% MeOH in DCM) to give 6-(4-benzyloxy-3-fluoro-phenyl)-2-(2-pyridyl)-7 , 8-dihydro-5H-pyrido [4,3-d]pyrimidine (2.33 g). ?H NMR (400MHz, CDC13):8.96 – 8.85 (m, 1 H), 8.69 (s, 1 H), 8.53 (d, 1 H), 7.89 (t, 1 H), 7.52 – 7.32 (m, 6 H), 6.98 (t, 1 H),6.85 (dd, 1 H), 6.77 – 6.63 (m, 1 H), 5.12 (s, 2 H), 4.38 (s, 2 H), 3.61 (t, 2 H), 3.28 (t, 2 H). MSobsd. (ESf) [(M+H)]: 413.

In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles. 52313-50-5, Picolinimidamide, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; CHENG, Zhanling; WANG, Min; YANG, Song; (208 pag.)WO2016/107832; (2016); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem