These common heterocyclic compound, 1239363-40-6, name is 1-Cyclopropyl-4-iodo-1H-pyrazole, 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. Product Details of 1239363-40-6
Intermediate 10: To a stirred solution of Intermediate 1OA (460 mg, 1.965 mmol) in THF (5 mL) at 0 C was added iPrMgCl (1.08 1 mL, 2.162 mmol) quickly. After 30 mm, additional 0.15 eq of iPrMgCl was added and after 30 mm, the mixture was cooled to -78 C. N-Methoxy-N-methylacetamide (304 mg, 2.95 mmol) was added quickly andthe reaction was warmed to RT for 3h. The reaction mixture was concentrated in vacuo and diluted with EtOAc. The organic layer was washed with H20. The organic layer was dried over MgSO4, filtered and concentrated in vacuo. The crude product was purified to give Intermediate 10 (250mg, 1.665 mmol, 85% yield) as a clear liquid. LCMS Anal. Calc?d for C8H,0N20 150.8, found [M+H] 151.0.
The synthetic route of 1-Cyclopropyl-4-iodo-1H-pyrazole has been constantly updated, and we look forward to future research findings.
Reference:
Patent; BRISTOL-MYERS SQUIBB COMPANY; MENG, Wei; ZHAO, Guohua; WO2015/134701; (2015); A1;,
Pyrazole – Wikipedia,
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