Electric Literature of 7170-01-6, New Advances in Chemical Research in 2021. The prevalence of solvent effects in heterogeneous catalysis in condensed media has motivated developing quantitative kinetic,A common heterocyclic compound, 7170-01-6, name is 3-Methyl-1H-1,2,4-triazole, molecular formula is C3H5N3, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, below Introduce a new synthetic route.
General procedure: In a 10 mL round-bottomed flask, (2S,4R)-4-(2-chloro-4-fluorophenylsulfonyl)-N-(1- cyanocyclopropyl)- 1- (1- (trifluoromethyl)cyclopropanecarbonyl)pyffolidine-2-carboxamide (example 8b)) (400 mg, 788 imol, Eq: 1.00) was combined with DMA (5 mL) to give a colorless solution. 1H-1,2,4-triazole (111 mg, 1.58 mmol, Eq: 2.00) and cesium carbonate (513 mg, 1.58 mmol, Eq: 2.00) were added. The reaction mixture was heated to 80 C and stilTed for 3h. The reaction mixture was poured into water and extracted with EtOAc (2x). The organic layers were combined, washed with saturated aqueous NaHCO3 solution (lx),water (3x) and brine (lx). The organic layers were dried over Na2SO4 and concentrated in vacuo.The crude material was purified twice by flash chromatography (silica gel, 20g, DCM/MeOH 98/2, 19/1) and (silica gel, 20g, Heptan/AcOEt 1/2, 1/3, 1/4) to yield the title compound as a white foam (264 mg; 60%).: _Example 11 was obtained as a byproduct during the synthesis of example 10 as a white solid (34 mg; 7%).
Therefore, this conceptually novel strategy might open impressive avenues to establish green and sustainable chemistry platforms.In my other articles, you can also check out more blogs about 3-Methyl-1H-1,2,4-triazole.
Reference:
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; HAAP, Wolfgang; KUHN, Bernd; LUEBBERS, Thomas; PETERS, Jens-Uwe; (93 pag.)WO2017/144483; (2017); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics