Reference of 1157938-97-0, Each compound has different characteristics, and only by selecting the characteristics of the compound suitable for a specific situation can the compound be applied on a large scale. 1157938-97-0, name is 1-(2,5-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone, This compound has unique chemical properties. The synthetic route is as follows.
A 2-neck flask with cooler was charged with zinc (1.1 g, 17 mmol, 3.8 eq.) and heated in vacuo using a hotgun (3 nitogen-vacuum cycles). Subsequently, THF (60 mL) was added and then trimethylsilylchloride (0.15 mL). The resulting suspension was stirred under a nitrogen atmosphere at room temperature for 15 minutes, after which a solution of ketone III (Ri = F, 1.0 g, 4.5 mmol, 1.0 eq.) in THF (30 mL) was added. The reaction mixture was then heated to 66 C, after which the heating source was removed. Subsequently, a solution of ethyl-2-bromopropionate (0.87 mL, 1.2 g, 6.7 mmol, 1.5 eq.) in THF (20 mL) was added dropwise over 10 minutes. The reaction mixture was then stirred at 66 C for 1.5 hours, after which it was cooled to room temperature. The reaction was quenched by addition of a saturated aqueous ammoniumchloride solution (100 mL) and diluted with methyl-teributyl ether (MTBE, 100 mL). The layers were separated and the aquous layer was extracted with MTBE (2x 100 mL). The combined organic layers were washed with brine (100 mL), dried (Na2S04), filtered and concentrated in vacuo to give a yellow oil (1.4 g) containing racemic ester I. ^-NMR- and GC-analysis showed a conversion of ketone III (Ri = F) of 80% and a d.e. of ester I of 60% in favor of the desired RR/SS-diastereomer. The product was not purified further.
The chemical industry reduces the impact on the environment during synthesis 1-(2,5-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone. I believe this compound will play a more active role in future production and life.
Reference:
Patent; BASILEA PHARMACEUTICA AG; VAN SUMMEREN, Ruben; VAESSEN, Harrie; MINK, Daniel; WASER, Mario; WO2014/23623; (2014); A1;,
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