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. 1001401-62-2, name is 2-(2H-1,2,3-Triazol-2-yl)benzoic acid belongs to triazoles compound, it is a common compound, a new synthetic route is introduced below. name: 2-(2H-1,2,3-Triazol-2-yl)benzoic acid
Step 2: (2-(2H-l ,2,3-triazol-2-yl)phenyl)((2i?,56 -5-hvdroxy-2-methylpiperidin-l-yl)methanone (3) A solution of (3S, 6i?)-6-methylpiperidin-3-ol (3.46 g, 30.0 mmol), 2-(2H- 1,2,3- triazol-2-yl)benzoic acid (6.82 g, 36.0 mmol), EDC (11.52 g, 60.1 mmol), l-hydroxy-7- azabenzotriazole (8.18 g, 60.1 mmol), and triethylamine (12.6 mL, 90 mmol) in DMF (200 mL) was stirred at 50 C overnight, then diluted with saturated aqueous sodium bicarbonate and extracted 3x with ethyl acetate. The organics were washed with brine, dried over magnesium sulfate, filtered, and concentrated. The crude material was purified by silica gel gradient chromatography (0-100% ethyl acetate in hexanes), providing the titled compound as a yellow-white solid. LRMS m/z (Mu+Eta) 287.3 found, 287.1 required.
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Reference:
Patent; MERCK SHARP & DOHME CORP.; KUDUK, Scott, D.; SKUDLAREK, Jason, W.; WO2015/88865; (2015); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics