Synthetic Route of 16681-70-2, New Advances in Chemical Research in 2021. The transformation of simple hydrocarbons into more complex and valuable products via catalytic C–H bond functionalisation has revolutionised modern synthetic chemistry. 16681-70-2, name is 1H-[1,2,3]Triazole-4-carboxylic acid, molecular formula is C3H3N3O2, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, below Introduce a new synthetic route.
To a mixture of (E)-3-(4-chloro-2-((5-methyl-2 H-tetrazol-2-yl)methyl)phenyl)- 1 -(4-(pi peridi n-4- yl)piperazin-i-yl)prop-2-en-i-one, dihydrochloride salt (Example 149, step 2)(130 mg, 0.259 mmol), DIPEA (0.316 ml, 1.810 mmol) and 1H-i ,2,3-triazole-4-carboxylic acid (38.0 mg, 0.336 mmol) in DMF (1.5 ml) was added T3P, 50% solution in EtOAc (0.302 ml, 0.517mmol). The resultant mixture was stirred at room temperature over the weekend. Water (0.5 ml) was added and the solvent removed in vacuo. The residue was purified by reverse phase preparative HPLC to afford the title compound as the trifluoroacetate salt;LC-MS: Rt 0.87 mins; MS mlz 525.3 (M+H)+; Method 2minLowpHvo2
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Reference:
Patent; NOVARTIS AG; BEATTIE, David; BAETTIG, Urs; LEGRAND, Darren Mark; LISTER, Andrew Stuart; MCKENNA, Jeffrey; PEARCE, David William; SANDHAM, David Andrew; STEWARD, Oliver Ross; THOMSON, Christopher; WO2015/8230; (2015); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics