Synthetic Route of 106877-33-2, 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.106877-33-2, name is 5-Amino-2-(trifluoromethyl)pyridine, molecular formula is C6H5F3N2, molecular weight is 162.11, as common compound, the synthetic route is as follows.
A solution of sodium nitrite (213 mg, 3.08 mmol) in water (620 pL) was slowly added to a suspension of 6-(trifluoromethyl)pyridine-3-amine (500 mg, 3.08 mmol) in cone. HC1 (525 pL) and ice (620 mg) at 0 C. After five minutes of stirring at 0 C a solution of potassium ethyl xanthate (593 mg, 3.70 mmol) in EtOH/water (1/1, 2 mL) was added and the resulting yellow slurry was heated at 50-55 C for 30 minutes. Then the reaction mixture was allowed to cool to rt and was then diluted with water (10 mL) and EtiO (10 mL). The phases were separated and the water phase was extracted with EtiO (2x 10 mL). The combined organics were washed with brine (10 mL) and dried (MgSCri). After filtration and evaporation, the crude material (659 mg) was dissolved in EtOH (8 mL) and potassium hydroxide (735 mg) was added. The resulting mixture was heated at 90 C for two hours and was then allowed to cool to rt. The reaction mixture was then filtered and the filtrate was acidified with citric acid, before being diluted with EtiO. The organic phase was washed with brine and dried (MgSCri). After filtration and evaporation of the solvent, the crude was dried under vacuum at 45 C over night. The title compound (150 mg) was obtained as a yellow crude solid, which was not purified further but used directly in the next step. ‘H NMR (CDCb) S 8.80 (br s, 1H) 7.99 (br d, =8.4 Hz, 1H9 7.66 (br d, =8.4 Hz).
The chemical industry reduces the impact on the environment during synthesis 106877-33-2, I believe this compound will play a more active role in future production and life.
Reference:
Patent; RESPIRATORIUS AB (PUBL); DALENCE, Maria; JOHANSSON, Martin; THORNQVIST OLTNER, Viveca; TOFTERED, Joergen; WENSBO, Davis; (49 pag.)WO2020/9653; (2020); A1;,
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