Category: 863704-60-3

Reference of 863704-60-3, 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.863704-60-3, name is 6-(4-Fluorophenyl)picolinic acid, molecular formula is C12H8FNO2, molecular weight is 217.2, as common compound, the synthetic route is as follows.

A mixture of Intermediate 3-07 (156 mg, 0.72 mmol), HATU (394 mg, 1.0 mmol) and DIPEA (0.639 mL, 3.66 mmol) in DCM (6 mL) was stirred at RT for 15 min. A solution of Intermediate 3-04 (155 mg, 0.72 mmol) in DCM (4 mL) was added and the reaction mixture was stirred at RT for 14 h. The mixture was washed with water, and the organic layer was dried over sodium sulfate, filtered and concentrated. The residue was purified by column chromatography (Biotage, cHex:EtOAc, 85:15 to 50:50) to afford Intermediate 3-09 (298 mg, 100%).

Statistics shows that 863704-60-3 is playing an increasingly important role. we look forward to future research findings about 6-(4-Fluorophenyl)picolinic acid.

Reference:
Patent; CENTRO NACIONAL DE INVESTIGACIONES ONCOLOGICAS (CNIO); PASTOR FERNANDEZ, Joaquin; ALVAREZ ESCOBAR, Rosa Maria; GARCIA GARCIA, Ana Belen; RIESCO FAGUNDO, Rosario Concepcion; BLANCO APARICIO, Carmen; WO2012/98387; (2012); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Adding a certain compound to certain chemical reactions, such as: 863704-60-3, 6-(4-Fluorophenyl)picolinic acid, can increase the reaction rate and produce products with better performance than those obtained under traditional synthetic methods. Here is a downstream synthesis route of the compound, Quality Control of 6-(4-Fluorophenyl)picolinic acid, blongs to pyridine-derivatives compound. Quality Control of 6-(4-Fluorophenyl)picolinic acid

A mixture of picolinic acid derivative (1.0 g, 4.6 mmol), Na2HPO4 (1.2 g) and m-CPBA (1.1 g, 70% from Aldrich) in CH2ClCH2Cl (30 mL) was stirred at rt for 2 h. Additional Na2HPO4 (0.8 g) and m-CPBA (1.0 g) was added to the reaction mixture and it was stirred for 3 h at rt. Another Na2HPO4 (0.5 g) and m-CPBA (0.5 g) was added to the reaction mixture and it was stirred at rt overnight. CHCl3 (160 mL) and 2 N aq. HCl solution (50 mL) were added to the reation mixture and the organic layer was separated, dried over MgSO4 and concentrated in vacuo. The residue was purified by flash column chromatography on silica gel eluting with EtOAc/MeOH/HOAc//700:240:60 to obtain the desired product which was contaminated with m-CPBA. This impure material was purified by preparative HPLC to obtain the desired product (175 mg, 16%) as a white solid. 1H NMR (DMF-d7) 8.45 (dd, 1H, J=8.3, 2.2 Hz), 8.15 (d, 1H, J=2.2 Hz), 8.13-8.00 (m, 4H), 7.45 (t, 2H, J=8.7 Hz).

At the same time, in my other blogs, there are other synthetic methods of this type of compound,863704-60-3, 6-(4-Fluorophenyl)picolinic acid, and friends who are interested can also refer to it.

Reference:
Patent; Borzilleri, Robert M.; Cornelius, Lyndon A.M.; Schmidt, Robert J.; Schroeder, Gretchen M.; Kim, Kyoung S.; US2005/245530; (2005); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Application of 863704-60-3 ,Some common heterocyclic compound, 863704-60-3, molecular formula is C12H8FNO2, 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.

B) 6-(4-Fluorophenyl)picolinic acid-N-oxide A mixture of picolinic acid derivative (1.0 g,, 4.6 mmol), Na2HPO4 (1.2 g) and mCPBA (1.1 g, ~70% from Aldrich) in CH2ClCH2Cl (30 mL) was stirred at rt for 2 h. Additional Na2HPO4 (0.8 g) and mCPBA (1.0 g, ~70% from Aldrich) was added to the reaction mixture and it was stirred for 3 h at rt. Another Na2HPO4 (0.5 g) and mCPBA (0.5 g, ~70% from Aldrich) was added to the reaction mixture and it was stirred at rt overnight. Next morning CHCl3 (160 mL) and 2N aq HCl (50 mL) were added to the reation mixture, the organic layer was separated, dried over MgSO4 and concentrated. The residue was purified by flash column on silica gel eluding with EtOAc/MeOH/HOAc//700:240:60 to obtain the desired product contaminated by mCPBA. This impure material was purified by preparative HPLC to obtain the desired product (175 mg, 16%) as a white solid. 1H NMR (DMF-d7) 8.45 dd, 1H, J=8.3, 2.2 Hz), 8.15 (d, 1H, J=2.2 Hz), 8.13-8.00 (mn, 4H), 7.45 (t, 2H, 8.7 Hz).

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. 863704-60-3, 6-(4-Fluorophenyl)picolinic acid, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; Bristol-Myers Squibb Company; US2007/60613; (2007); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Reference of 863704-60-3 ,Some common heterocyclic compound, 863704-60-3, molecular formula is C12H8FNO2, 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.

B) 6-(4-Fluorophenyl)picolinic acid-N-oxide A mixture of picolinic acid derivative (1.0 g,, 4.6 mmol), Na2HPO4 (1.2 g) and mCPBA (1.1 g, ~70% from Aldrich) in CH2ClCH2Cl (30 mL) was stirred at rt for 2 h. Additional Na2HPO4 (0.8 g) and mCPBA (1.0 g, ~70% from Aldrich) was added to the reaction mixture and it was stirred for 3 h at rt. Another Na2HPO4 (0.5 g) and mCPBA (0.5 g, ~70% from Aldrich) was added to the reaction mixture and it was stirred at rt overnight. Next morning CHCl3 (160 mL) and 2N aq HCl (50 mL) were added to the reation mixture, the organic layer was separated, dried over MgSO4 and concentrated. The residue was purified by flash column on silica gel eluding with EtOAc/MeOH/HOAc//700:240:60 to obtain the desired product contaminated by mCPBA. This impure material was purified by preparative HPLC to obtain the desired product (175 mg, 16%) as a white solid. 1H NMR (DMF-d7) 8.45 dd, 1H, J=8.3, 2.2 Hz), 8.15 (d, 1H, J=2.2 Hz), 8.13-8.00 (mn, 4H), 7.45 (t, 2H, 8.7 Hz).

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. 863704-60-3, 6-(4-Fluorophenyl)picolinic acid, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; Bristol-Myers Squibb Company; US2007/60613; (2007); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem