Category: 306960-77-0

Application of 306960-77-0, The major producers of chemicals have been the Europe, Japan and China. Due to the growing call for a cleaner, greener environment, people will have to find innovative ways to maintain their relevance. Here is a compound 306960-77-0, name is 2-(Trifluoromethyl)pyrimidine-5-carboxylic acid. This compound has unique chemical properties. The synthetic route is as follows.

Example 340 W-{[1 -ethyl-6-methyl-4-(tetrahydro-2H-pyran-4-ylamino)-1 H- pyrazolo[3,4-b]pyridin-5-yl]methyl}-2-(trifluoromethyl)-5-pyrimidine carboxamideEthyl 2-(trifluoromethyl)-5-pyrimidinecarboxylate [e.g. available from J. Med. Chem., (2000), 43 (21), 3995 (49mg) in ethanol (0.63ml) was treated with 2N sodium hydroxide (0.443ml) and the solution stirred at room temperature for 24h. 2M Hydrochloric acid (0.31ml) was added and the mixture blown down to dryness. The residue was suspended in dry dichloromethane (0.5ml) and treated at room temperature with oxalyl chloride (0.019ml) and DMF (1 drop). The mixture was stirred at room temperature for 30mins and then added dropwise to a solution of Intermediate 15 (53mg) in acetonitrile (1ml). DIPEA (0.039ml) was added and the mixture was stirred at room temperature for 18h. The mixture was blown down to dryness and the residue was purified by mass directed autoprep HPLC followed by SPE cartridge (1g, aminopropyl) eluting with methanol. The eluent was blown down to dryness to give Example 340 as a beige solid (9mg). LCMS showed MH+ = 464; TRET = 2.42min.

While traditionally a conservative industry, chemical producers will need to modernize their PR strategies to stay relevant.we look forward to future research findings about 306960-77-0, 2-(Trifluoromethyl)pyrimidine-5-carboxylic acid.

Reference:
Patent; GLAXO GROUP LIMITED; WO2007/36733; (2007); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Synthetic Route of 306960-77-0, 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. 306960-77-0, name is 2-(Trifluoromethyl)pyrimidine-5-carboxylic acid, molecular formula is C6H3F3N2O2, 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.

2-(Trifluoromethyl)pyrimidine-5-carboxylic acid (44.39 g, 231 .1 mmol),methoxymethanine hydrochloride (33.8 g, 346.6 mmol) and DIPEA (119.5 mL, 924.3 mmol) were combined in DCM (750 mL) then HATU (105.4 g, 277.3 mmol) was added and the mixture stirred at RT for 2 h. The reaction mixture was washed with water (3 x 300 mL), the organic phase collected, dried (over Mg504), filtered andconcentrated in vacuo to give a viscous yellow oil. The crude material was purified by dry flash chromatography (eluting with 0 – 40 % EtOAc in heptane) to give 54.2 g (95% yield) of the title compound as a free flowing pale yellow oil.1H NMR (500 MHz, Chloroform-d): 6 [ppm] 9.22 (5, 2H), 3.61 (5, 3H), 3.43 (5, 3H). LCMS (Analytical Method A) Rt = 1 .03 mm, MS (ESipos): m/z = 235.9 (M+H).

According to the analysis of related databases, 306960-77-0, the application of this compound in the production field has become more and more popular.

Reference:
Patent; EVOTEC AG; DAVENPORT, Adam James; BRAEUER, Nico; FISCHER, Oliver Martin; ROTGERI, Andrea; ROTTMANN, Antje; NEAGOE, Ioana; NAGEL, Jens; GODINHO-COELHO, Anne-Marie; (703 pag.)WO2016/91776; (2016); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia