A class of pyrazole amide derivatives, its preparation method and application
A kind of technology of pyrazole amide and carboxamide group, applied in the field of pyrazole amide derivatives, can solve the problems such as no disclosure
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Embodiment 1
[0085] The preparation of embodiment 1 intermediate (C-1)
[0086] Dry the reaction device, put 3.75 g of s-2-amino-1-propanol (B), 6.3 g of triethylamine, and 100 ml of dichloromethane into a single-necked flask, slowly drop in 9.73 g of 3-difluoromethyl- 1-Methyl-1H-pyrazole-4-formyl chloride (A) in 30ml of dichloromethane solution, stirred at room temperature for 1 hour after dropping, left for 3 hours, separated by TLC after precipitation (developer: ethyl acetate), A white solid (C-1) was obtained. (S)-3-(difluoromethyl)-N-(1-hydroxypropan-2-yl)-1-methyl-1H-pyrazole-4-carboxamide (B) above can also be replaced by 2-amino-1-propanol ( vortex), 2-amino-2-methyl-1-propanol, aminoethanol, etc. to prepare the corresponding intermediate (C-1).
Embodiment 2
[0087] The preparation of embodiment 2 target compound (E-2)
[0088] Weigh 10mmol of the intermediate (C-1) prepared in Example 1 and 10mmol of 4-chlorophenylisocyanate (D) in a single-necked flask, use 20ml of tetrahydrofuran as a solvent, stir overnight at room temperature, concentrate, and separate by TLC (developing agent is V (Ethyl acetate): V (petroleum ether)=4:1 mixed solution), obtain target product (E-2), its NMR data is as follows:
[0089] NMR 1 H-NMR(ppm)δ9.75(s,1H),8.26(s,1H),8.07(d,J=8.2Hz,1H),7.52–7.12(m,4H),7.32(t,J=54.1 Hz,1H),4.23(s,1H),4.08(d,J=5.3Hz,2H),3.91(s,3H),1.16(d,J=6.7Hz,3H).
[0090] All compounds from E-1 to E-299 can be synthesized using the same method.
[0091] 2. Preparation
Embodiment 3
[0092] Embodiment 3 wettable powder formula
[0093] 15% of compounds (E-a, E-b, E-c), 5% of lignosulfonate (M q ), 1% lauryl polyoxyethylene ether (JFC), 40% diatomaceous earth and 44% light calcium carbonate are evenly mixed and pulverized to obtain a wettable powder.
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