Reference of 16681-70-2, These common heterocyclic compound, 16681-70-2, name is 1H-[1,2,3]Triazole-4-carboxylic acid, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
[0841] lH-1,2,3-triazole-5-carboxylic acid (3.4 mg, 30f.tmol) and HATU (11.4 mg, 30 Imo’) were dissolved in DMF(0.5 mL) and stirred at room temperature. A solution of (2R,4 R )-4-amino-5 -( 5′ -chloro-2′-flu oro bipheny 1-4-yl )-2-(1-iso butyry loxy-ethoxycarbony amino )pentanoic acid benzy Iester (19 mg, 27 f.tmol) in DMF (0.5 mL) was added to thissolution, followed by DIPEA (14 f.LL, 82 f.tmol). The resultingsolution was stirred at room temperature for 90 minutes andthen concentrated in vacuo. The crude residue was purified bysilica gel chromatography (0-100% EtOAc:hexanes) to yieldCompound 1 (13 mg) as a clear oil.
The synthetic route of 16681-70-2 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; THERAVANCE BIOPHARMA R&D IP, LLC; Fleury, Melissa; Beausoliel, Anne-Marie; Hughes, Adam D.; Long, Daniel D.; Wilton, Donna A.A.; US2015/210690; (2015); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics