Simple exploration of 4-(Trifluoromethyl)-1H-pyrazole

The synthetic route of 52222-73-8 has been constantly updated, and we look forward to future research findings.

52222-73-8, name is 4-(Trifluoromethyl)-1H-pyrazole, belongs to pyrazoles-derivatives compound, is considered to be a conventional heterocyclic compound, which is widely used in drug synthesis. The chemical synthesis route is as follows. Application In Synthesis of 4-(Trifluoromethyl)-1H-pyrazole

To a solution of 7′-(2,6-difluoro-4-iodo-phenyl)spiro[cyclopropane-l,5′-imidazo[l,2- a]imidazole]-6′-one (Example A.3) (300 mg, 0.770 mmol, 1 eq.) and 4-(trifluoromethyl)-lH- pyrazole (158 mg, 1.16 mmol, 1.5 eq.) in toluene (1.5 mL) was added K3P04 (494 mg, 2.32 mmol, 3 eq.) and 1,2-N,N’ dimethyl- 1 ,2-cyclohexanediamine (23 mg, 0.160 mmol, 0.21 eq.) and degassed with nitrogen for 10 min. Cul (15 mg, 0.080 mmol, 0.1 eq.) was added, the reaction mixture again degassed with nitrogen for 10 mins, and stirred at 130 C in the microwave for 1 h. The reaction mixture was diluted with EtOAc (50 ml), the organics washed with water (2 x 20 mL) and brine (20 mL), dried over Na2S04, concentrated in vacuo and purified by flash chromatography over silica gel (50 % EtOAc in hexane) to yield 7′-[2,6-difluoro-4-[4- (trifluoromethyl)pyrazol-l-yl]phenyl]spiro[cyclopropane-l,5′-imidazo[l,2-a]imidazole]-6′-one (40 mg, 0.1 mmol, 13 % yield) as a sticky gel. M+H+ = 396.0.

The synthetic route of 52222-73-8 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; JAESCHKE, Georg; O`HARA, Fionn; VIEIRA, Eric; (85 pag.)WO2019/34713; (2019); A1;,
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics