In the chemical reaction process, reaction time, type of solvent, can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product. An updated downstream synthesis route of 16681-70-2 as follows. Application In Synthesis of 1H-[1,2,3]Triazole-4-carboxylic acid
A solution of Compound 1 (18.1 mg, 37 mumol) in HCl (185 muL, 740 mumol) was stirred at room temperature for 30 minutes. After this time, LCMS indicated that the boc group had been cleaved so the solution was concentrated in vacuo. A solution of 3H-[1,2,3]triazole-4-carboxylic acid (5.0 mg, 44 mumol) and HATU (17 mg, 44 mumol) in DMF (370 muL) was stirred at room temperature for 30 minutes. After this time, a solution of the crude amine in DMF (370 muL) was added, followed by DIPEA (19 muL, 111 mumol). The resulting mixture was stirred at room temperature for 1 hour, and then concentrated in vacuo. The crude residue was purified by preparative HPLC to yield 3 products with identical masses (2 of which are diastereomers): isomer a (3.5 mg; purity 97%), isomer b (1.2 mg; purity 100%), and isomer c (1.1 mg; purity 100%). MS m/z [M+H]+ calc’d for C24H23ClFN5O33, 484.15. found 484.2.
According to the analysis of related databases, 16681-70-2, the application of this compound in the production field has become more and more popular.
Reference:
Patent; THERAVANCE BIOPHARMA R&D IP, LLC; Fleury, Melissa; Beausoliel, Anne-Marie; Hughes, Adam D.; Long, Daniel D.; Wilton, Donna A.A.; US2015/209352; (2015); A1;,
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