Adding a certain compound to certain chemical reactions, such as: 1029413-51-1, name is 4-Amino-1-(1-boc-azetidin-3-yl)-1H-pyrazole, 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 1029413-51-1, Quality Control of 4-Amino-1-(1-boc-azetidin-3-yl)-1H-pyrazole
General procedure: [0 140j To a solution of tert-butyl 2-methyl-4-(4,4,5 ,5 -tetramethyl- 1,3 ,2-dioxaborolan-2- yl)benzylcarbamate (3.47 g, 10 mmol) and 2,4-dichloropyrimidine (1.79 g, 12 mmol) in 1,4- dioxane (28 mL) and H20 (7 mL), Pd(dppf)C12.DCM (815 mg, 1.0 mmol) and K2C03 (2.76 g,mmol) were added under N2. The mixture was stirred at 90 C for 2 h. After cooling to rt, the mixture was diluted with H20 (80 mL) and extracted with EA (80 mL x2). The organic layers were dried and concentrated. The residue was purified by column chromatography (silica,petroleum ether/EtOAc = 5:1 to 2:1) to give tert-butyl 4-(2-chloropyrimidin-4-yl)-2- methylbenzylcarbamate (2.67 g, yield 80%) as white solid. [0231j Synthesis of tert-butyl 3 -(4-((4-(4-((2-(tert-butyl)thiazole-5 – carboxamido)methyl)-3 -methylphenyl)pyrimidin-2-yl)amino)- 1 H-pyrazol- 1 -yl)azetidine- 1- carboxylate was similar to that of tert-butyl 4-(2-chloropyrimidin-4-yl)-2- methylbenzylcarbamate. Purified through silica gel column chromatography with (MeOH/DCM= 1/20) to give tert-butyl 3 -(4-((4-(4-((2-(tert-butyl)thiazole-5 – carboxamido)methyl)-3 -methylphenyl)pyrimidin-2-yl)amino)- 1 H-pyrazol- 1 -yl)azetidine- 1- carboxylate (150 mg, yield: 69%) as a yellow solid. ESI-MS (M+H) : 603.2. ?H NMR (400 MHz, CDC13) (5: 8.45 (d, J= 5.2 Hz, iH), 8.i2 (s, iH), 8.05 (s, iH), 7.88 (s, iH), 7.85 (d, J 8.0 Hz, iH), 7.64 (s, iH), 7.42 (d, J= 8.0 Hz, iH), 7.10 (d, J 5.6 Hz, iH), 6.94 (s, iH), 6.i 1-6.09 (m, iH), 5.08-5.01 (m, iH), 4.68 (d, J= 5.2 Hz, 2H), 4.42-4.33 (m, 4H), 2.46 (s, 3H), 1.56 (s,
At the same time, in my other blogs, there are other synthetic methods of this type of compound, 4-Amino-1-(1-boc-azetidin-3-yl)-1H-pyrazole, and friends who are interested can also refer to it.