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.624734-22-1, name is 2-Chloro-5-(trifluoromethyl)nicotinonitrile, molecular formula is C7H2ClF3N2, molecular weight is 206.55, as common compound, the synthetic route is as follows.HPLC of Formula: C7H2ClF3N2
To a suspension of NaH (7.8 g, 200 mmol) in tetrahydrofuran (100 mL) under nitrogen was added dropwise a solution of tert-butyl methyl malonate (20 mL, 120 mmol) in anhydrous tetrahydrofuran (100 mL) via syringe. The reaction mixture was stirred for 0.5 h before a solution of the intermediate prepared in Step D, Intermediate 11 (20.1 g, 97.6 mmol) in tetrahydrofuran (200 mL) was added slowly via syringe. The reaction was stirred at room temperature overnight, then quenched with a saturated solution of NH4Cl. The organic layer was separated and the aqueous layer was extracted with ethyl acetate (3 x). The combined organic layers were washed with water (3 x), dried over Na2S04, filtered, and evaporated in vacuo. Flash chromatography afforded 31.76 g (95%) of the pure desired product.
At the same time, in my other blogs, there are other synthetic methods of this type of compound,624734-22-1, 2-Chloro-5-(trifluoromethyl)nicotinonitrile, and friends who are interested can also refer to it.
Reference:
Patent; MERCK & CO., INC.; WO2005/105092; (2005); A2;,
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