Reference of 16681-70-2, In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 16681-70-2, name is 1H-[1,2,3]Triazole-4-carboxylic acid belongs to triazoles compound, it is a common compound, a new synthetic route is introduced below.
[0458] 3-[(R)-2-Amino-3-(5?-chloro-2?-fluorobiphenyl-4-yl)-propyl]pyrrolidine-1,3-dicarboxylic acid 1-benzyl ester (isomer a; 14 mg, 35 mumol, 1.0 eq.) was dissolved in DMF. 1H-1,2,3-triazole-4-carboxylic acid (2 eq.), DIPEA (2 eq.), and HATU (1 eq.) were also dissolved in DMF and stirred at room temperature for a few minutes. The solutions were then combined and the resulting mixture stirred at room temperature and when the reaction was complete (as determined by LC/MS analysis), the mixture was concentrated in vacuo to yield crude Compound 1a. LCMS (ESI): calc. C31H29ClFN5O5=605; obs. M+H=606.1. Retention time: 5.82 min. (LC/MS Method 1) [0459] 3-[(R)-2-Amino-3-(5?-chloro-2?-fluorobiphenyl-4-yl)-propyl]pyrrolidine-1,3-dicarboxylic acid 1-benzyl ester (isomer b; 170 mg, 320 mumol, 1.0 eq.) and DIPEA (200 muL, 1150 mumol, 3.6 eq.) were dissolved in DMF (1 mL). 1H-1,2,3-triazole-4-carboxylic acid (100 mg, 880 mumol, 2.8 eq.), DIPEA (200 muL, 1150 mumol, 3.6 eq.) and HATU (200 mg, 530 mumol, 1.6 eq.) were dissolved in DMF (3 mL) and stirred at room temperature for a few minutes. The solutions were then combined and the resulting mixture stirred at room temperature and when the reaction was complete (as determined by LC/MS analysis), the mixture was concentrated in vacuo to yield crude Compound 1b. LCMS (ESI): calc. C31H22ClFN5O4=605; obs. M+H=606.2. Retention time: 5.73 min. (LC/MS Method 1).
In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles, 1H-[1,2,3]Triazole-4-carboxylic acid, other downstream synthetic routes, hurry up and to see.
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;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics