Introduction of a new synthetic route about 16681-70-2

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.

Synthetic Route 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.

A solution of 1H-1,2,3-triazole-4-carboxylic acid (26 mg, 0.23 mmol) and HBTU (171 mg, 0.45 mmol) in a mixed solvent of dimethyl sulfoxide (2 mL) and tetrahydrofuran (4 mL) was stirred for 10 min at rt, then (+/-) -cis-6- ( (3-aminocyclohexyl) amino) -2- (5, 7-difluoro -1-tosyl-1H-indol-3-yl) -5-fluoro-4-phenylnicotinonitrile (92 mg, 0.15 mmol) and DIPEA (0.10 mL, 0.61 mmol) were added into the mixture. The resulting mixture was stirred at rt overnight. To the reaction mixture was added water (30 mL) , and the mixture was extracted with EtOAc (30 mL ¡Á 3) . The combined organic layers were washed with a saturated aqueous sodium chloride solution (60 mL) , dried over anhydrous sodium sulfate, and filtered. The filtrate was concentrated in vacuo to dry, and the residue was purified by silica gel column chromatography (PE/EtOAc (v/v) 5/1 1/5) to give the title compound as a white solid (78 mg, 73 %) . 1H NMR (400 MHz, CDCl3) delta (ppm) : 8.66 (s, 1H) , 8.20 (s, 1H) , 7.93 (d, J 8.0 Hz, 2H) , 7.71 (d, J 8.9 Hz, 1H) , 7.55 (s, 5H) , 7.31 (d, J 8.3 Hz, 2H) , 7.00 (s, 1H) , 6.84 (t, J 9.3 Hz, 1H) , 5.22 (d, J 5.7 Hz, 1H) , 4.30 (s, 1H) , 4.14 (d, J 7.2 Hz, 1H) , 2.58 (d, J 11.1 Hz, 1H) , 2.39 (s, 3H) , 2.29 (d, J 11.3 Hz, 1H) , 2.17 (d, J 11.0 Hz, 1H) , 1.97 (d, J 14.3 Hz, 1H) , 1.63 (m, 4H) .

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; SUNSHINE LAKE PHARMA CO., LTD.; TANG, Changhua; REN, Qingyun; YIN, Junjun; YI, Kai; ZHANG, Yingjun; (161 pag.)WO2018/41091; (2018); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics