Adding a certain compound to certain chemical reactions, such as: 1018446-95-1, name is tert-Butyl 4-amino-1H-pyrazole-1-carboxylate, belongs to pyrazoles-derivatives compound, can increase the reaction rate and produce products with better performance than those obtained under traditional synthetic methods. Here is a downstream synthesis route of the compound 1018446-95-1, Safety of tert-Butyl 4-amino-1H-pyrazole-1-carboxylate
[0607j To a solution of N-(4-(2-chloropyrimidin-4-yl)-2-methylbenzyl)-3 – isopropoxyazetidine-1-carboxamide (220 mg, 0.60 mmol) and tert-butyl 4-amino-1H-pyrazole- 1-carboxylate (132 mg, 0.72 m mol) in dry 1,4-dioxane (8 mL) was added Pd2(dba)3 (55 mg,0.06 mmol), S-phos (49 mg, 0.12 mmol) and Cs2CO3 (390 mg, 1.2 mmol). The mixture was stirred at 120 C for 4 h under N2. After cooling to rt, the mixture was diluted with EtOAc (150 mL) and washed with water (60 mL x 2). The organic phase was dried over Na2SO4, filtered and concentrated in vacuo. The residue was dissolved in 3 N HC1 in MeOH (10 mL) and the resulting mixture was stirred at rt for 1 h. After concentration in vacuo, the residue was purified by prepHPLC (CH3CN/H20 with 0.05% NH4OH as mobile phase) to give N-(4-(2-((1H-pyrazol-4- yl)amino)pyrimidin-4-yl)-2-methylbenzyl)-3 -isopropoxyazetidine- 1 -carboxamide as a white solid (88 mg, yield: 35%). ESI-MS (M+H) : 544.2. ?H NMR (400 MHz, CD3OD) 5: 8.38 (d, J= 4.8 Hz, 1H), 8.05 (s, 1H), 7.91-7.90 (m, 2H), 7.75 (s, 1H), 7.37 (d, J= 8.4 Hz, 1H), 7.16 (d, J5.2 Hz, 1H), 4.42-4.36 (m, 3H), 4.18-4.14 (m, 2H), 3.81-3.78 (m, 2H), 3.67-3.61 (m, 1H), 2.41 (s, 3H), 1.14 (d, J 6.0 Hz, 6H).
In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles, tert-Butyl 4-amino-1H-pyrazole-1-carboxylate, other downstream synthetic routes, hurry up and to see.
Reference:
Patent; BIOGEN IDEC MA INC.; SUNESIS PHARMACEUTICALS, INC.; HOPKINS, Brian, T.; MA, Bin; CHAN, Timothy, Raymond; SUN, Lihong; ZHANG, Lei; KUMARAVEL, Gnanasambandam; LYSSIKATOS, Joseph, P.; KOCH, Kevin; MIAO, Hua; WO2015/89337; (2015); A1;,
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