Application of 578008-32-9, These common heterocyclic compound, 578008-32-9, name is tert-Butyl 3-amino-5-methyl-1H-pyrazole-1-carboxylate, 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.
The product of the previous step (6.6 g, 14.8 mmol), tert-butyl 3-amino-S-methyl- 1H-pyrazole-1-carboxylate (3.5 g, 17.7 mmol), cesium carbonate (9.61 g, 29.6 mmol) andPd Xphos (2.32 g, 2.95 mmol) were dissolved in dioxane (130 mL) and purged with nitrogen. The reaction mixture was stirred at 110 C for 12 h. The product was combined with the product of a similar reaction, extracted with EtOAc (600 mL) and washed with brine (3 x 300 mL). The organic layer was evaporated. The residue was crystallized to provide the title intermediate (5 g, 58 % yield) and 2 g of cmde product which waspurified by preparative HPLC (method 2).
Statistics shows that tert-Butyl 3-amino-5-methyl-1H-pyrazole-1-carboxylate is playing an increasingly important role. we look forward to future research findings about 578008-32-9.
Reference:
Patent; THERAVANCE BIOPHARMA R&D IP, LLC; HUDSON, Ryan; KOZAK, Jennifer; FATHEREE, Paul R.; PODESTO, Dante D.; BRANDT, Gary E.L.; FLEURY, Melissa; BEAUSOLEIL, Anne-Marie; HUANG, Xiaojun; THALLADI, Venkat R.; (121 pag.)WO2016/191524; (2016); A1;,
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