16681-65-5, These common heterocyclic compound, 16681-65-5, name is 1-Methyl-1H-1,2,3-triazole, 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.
A suspension of 6-bromo-3-chloroisoquinoline (60 mg, 0.25 mmol), 1 -methyl- 1 H-1 ,2,3-triazole (41 mg, 0.50 mmol), Pd(OAc)2 (2.22 mg, 9.9 umol) and KOAc (49 mg, 0.50 mmol) in DMA (4 mL) was stirred at 150^ under microwave irradiation for 60 minutes. The reaction mixture was diluted with brine and extracted with EtOAc. The combined organic layers were washed with water and dried with Na2S04 and concentrated in vacuo. The residue was purified using Biotage silica gel column chromatography eluting with 40% EtOAc in cyclohexane to afford the title compound as a white solid (19 mg, 31 %). 1 H NMR (500 MHz, CDCI3) : delta .17 (t, J = 0.9 Hz, 1 H), 8.15 (dt, J = 8.5, 0.9 Hz, 1 H), 7.94 – 7.85 (m, 2H), 7.82 (d, J = 1 .1 Hz, 1 H), 7.67 (dd, J = 8.5, 1 .6 Hz, 1 H), 4.19 (s, 3H). LCMS (ESI) Rt = 2.00 minutes MS m/z 245 [M+H]+
Chemical properties determine the actual use. Each compound has specific chemical properties and uses. We look forward to more synthetic routes in the future to expand reaction routes of 16681-65-5.
Reference:
Patent; CANCER RESEARCH TECHNOLOGY LIMITED; HOELDER, Swen; BLAGG, Julian; CHEUNG, Jack; ATRASH, Butrus; SHELDRAKE, Peter; WO2014/37751; (2014); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics