New discoveries in chemical research and development in 2021. The transformation of simple hydrocarbons into more complex and valuable products via catalytic C–H bond functionalisation has revolutionised modern synthetic chemistry. 1533519-85-5, name is Methyl 2-((4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-yl)thio)acetate belongs to triazoles compound, it is a common compound, a new synthetic route is introduced below. Safety of Methyl 2-((4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-yl)thio)acetate
250mL was added to the reaction flask the product of step B (4g, 0.0118mol), tetrahydrofuran (30ml), tetramethylpiperidinePyridine (TEMPO, 0.2g, 0.1eq), an oil bath at 30 ~ 32 heating and stirring to dissolve until clear. Portionwise added N- bromosuccinimideImide (NBS, 3.2g, 0.018mol, 1.5eq), temperature does not exceed 35 . Plus complete, insulation 30 ~ 32 reaction 3h.Sample testing of raw materials after the reaction was complete, heating was stopped, the ice bath to cool. Until an internal temperature of 0 ~ 5 , water portionwise sodium sulfiteThe reaction was quenched solution was extracted with ethyl acetate, dried over anhydrous sodium sulfate, filtration, spin dry, and the resulting crude intermediate C directlyUsed in the next reaction.Samples were analyzed by column chromatography (200-300 mesh silica gel, eluting with methylene chloride: methanol = 15: 1) to giveWhite solid C.
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Reference:
Patent; Zhejiang Jingxin Pharmaceutical Co., Ltd.; Huang, yue; Xu, hui; Zhangyu, bin; Zheng, fei; (19 pag.)CN105399694; (2016); A;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics