New downstream synthetic route of 5-Fluoro-2-picolinic acid

According to the analysis of related databases, 107504-08-5, the application of this compound in the production field has become more and more popular.

Related Products of 107504-08-5, As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 107504-08-5, name is 5-Fluoro-2-picolinic acid, molecular formula is C6H4FNO2, The compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below.

In the 0 C will be under 5-fluoropyridine-2-carboxylic acid (212 mg, 1.5 mmol) and methylene chloride (10 ml) is added to the 100 ml flask in a single port, adding N, N – diisopropyl ethylamine (0.37 ml, 2.2 mmol) and HATU (600 mg, 1.5 mmol), under the protection of nitrogen to continue the reaction 0.5 hours; then adding (R)-tert-butyl (5-(5-amino-2-fluorophenyl)-2-cyclopropyl-5-methyl-1,1-dioxo-1,2,4-thiadiazine 3-methylene)carbamate (310 mg, 0 . 75 mmol), transferred to the 25 C reaction under 2 hours; stopping the reaction, by adding water (20 ml), then dichloromethane is used for extraction (30 ml ¡Á 2), the collection of organic phase, adding anhydrous sodium sulfate (2 g) drying, filtering, the filtrate is pressure reduced turns on lathe does, column chromatography separation and purification (petroleum ether/ethyl acetate (v/v)=4/1) to obtain the title compound as a white solid (0.34 g, 84.5%).

According to the analysis of related databases, 107504-08-5, the application of this compound in the production field has become more and more popular.

Reference:
Patent; Guangdong Dongyangguang Pharmaceutical Co., Ltd.; Jin Chuanfei; Zhong Wenhe; Xu Tengfei; Xue Yaping; (40 pag.)CN109180670; (2019); A;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Brief introduction of 107504-08-5

Statistics shows that 107504-08-5 is playing an increasingly important role. we look forward to future research findings about 5-Fluoro-2-picolinic acid.

107504-08-5, 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.107504-08-5, name is 5-Fluoro-2-picolinic acid, molecular formula is C6H4FNO2, molecular weight is 141.1, as common compound, the synthetic route is as follows.

A mixture of compound 4-1 (20 mg, 0.056 mmol), 5-fluoropicolinic acid (18 mg, 0.112 mmol), and T3P (150 mg, 0.236 mmol, 50% in EtOAc) in THF (5 mL) was stirred at 25 C overnight. The mixture was diluted with water and extracted with EtOAc. The combined extracts were washed with brine, dried over Na2S04, and concentrated. The residue was purified by preperative HPLC (column: Gemini 200×25 mm, 5 muiotaeta; mobile phases A: water containing 0.075% TFA, v/v; mobile phase B: CH3CN; gradient 18-48% B, 11 min, 25 mL/min) to afford Example 4a.

Statistics shows that 107504-08-5 is playing an increasingly important role. we look forward to future research findings about 5-Fluoro-2-picolinic acid.

Reference:
Patent; MERCK SHARP & DOHME CORP.; CUMMING, Jared, N.; KAELIN, David Earl, Jr.; SCOTT, Jack, D.; WU, Wen-Lian; BURNETT, Duane, A.; WO2014/99794; (2014); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem