Application of 13273-53-5, New Advances in Chemical Research in 2021. The dynamic chemical diversity of the numerous elements, ions and molecules that constitute the basis of life provides wide challenges and opportunities for research. 13273-53-5, name is 4-Bromo-1-methyl-1H-1,2,3-triazole, molecular formula is C3H4BrN3, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, below Introduce a new synthetic route.
A mixture of tert-butyl 4-({[2-amino-5-(4,4,5,5-tetramethyl-1 ,3,2-dioxaborolan-2-yl)pyridin-3-yl]oxy}methyl)piperidine-1 -carboxylate (I-55) (580 mg, 1 .34 mmol), 4-bromo-1 -methyl-1 /-/-1 ,2,3-triazole (260 mg, 1 .61 mmol), Cs2C03 (2 N, 1 .34 mL, 2.68 mmol) in toluene (2 mL) and EtOH (6 mL) was added Pd(PPh3)4 (30.9 mg, 0.0268 mmol). The mixture was thoroughly degassed before heating under nitrogen at 80 C for 18 hr. TLC (EtOAc) indicated the reaction was completed. The mixture was concentrated under vacuum to dryness, and the residue purified by silica gel chromatography (petroleum ether/ EtOAc = 1/1 to 0/1) to give tert-butyl 4-({[2-amino-5-(1 -methyl-1 /-/-1 ,2, 3-triazol-4-yl)pyridin-3-yl]oxy}methyl)piperidine-1 -carboxylate (I-60) (503 mg, 97%) as a white solid.
I am very proud of our efforts over the past few months and hope to 4-Bromo-1-methyl-1H-1,2,3-triazole help many people in the next few years.
Reference:
Patent; PFIZER INC.; JOHNSON, Ted William; RICHARDSON, Paul Francis; COLLINS, Michael Raymond; RICHTER, Daniel Tyler; BURKE, Benjamin Joseph; GAJIWALA, Ketan; NINKOVIC, Sacha; LINTON, Maria Angelica; LE, Phuong Thi Quy; HOFFMAN, Jacqui Elizabeth; (335 pag.)WO2016/97918; (2016); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics