Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps, and cheap raw materials. 821767-61-7, name is tert-Butyl 4-formyl-1H-pyrazole-1-carboxylate, A new synthetic method of this compound is introduced below., Safety of tert-Butyl 4-formyl-1H-pyrazole-1-carboxylate
Tert-Butyl 4-formyl-1H-pyrazole-1-carboxylate (CAS [821767-61-7]), (122 mg, 0.62 mmol) was added at 10 C, under N2 to a solution of intermediate 15 (183 mg, 0.55 mmol) in MeOH (7 mL). The mixture was stirred at rt for 5 h. Then NaBH4 (31 mg, 0.83 mmol) was added portionwise and the mixture was stirred at rt for 15 h. The mixture was poured into ice water, extracted with DCM. The organic layer was dried over MgSO4, filtered and evaporated to dryness giving 0.35g of crude compound. The residue was purified by chromatography over silica gel (Stationary phase: irregular SiOH 15-40mum 40g, Mobile phase: Gradient from 0.1% NH4OH, 97% DCM, 3% MeOH to 0.1% NH4OH, 95% DCM, 5% MeOH). The fractions containing product were collected and evaporated to dryness yielding 150 mg (yield 39%) of intermediate 17.
The synthetic route of 821767-61-7 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; JANSSEN PHARMACEUTICA NV; ANGIBAUD, Patrick, Rene; PANDE, Vineet; HERKERT, Barbara; KROSKY, Daniel, Jason; QUEROLLE, Olivier, Alexis, Georges; PATRICK, Aaron, Nathaniel; PILATTE, Isabelle, Noelle, Constance; (157 pag.)WO2018/109088; (2018); A1;,
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics