35228-98-9Relevant academic research and scientific papers
A medicine intermediate 1H - pyrazole compound synthesis method
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Paragraph 0045; 0046; 0047; 0048; 0049, (2017/07/01)
The invention provides a method for synthesizing a 1H-pyrazole compound represented by a formula (III) in the description. The method comprises the following steps: S1, in an organic solvent and in the presence of a catalyst, an organic ligand, an additive and a base, a compound represented by a formula (I), a compound represented by a formula (II), and an amine source compound are subjected to a reaction; S2: after the step S1 is completed, acetic acid is added dropwise to the system, the reaction continues while stirring, and the compound represented by the formula (III) is obtained; in the formula (III), R1 and R2 are H, C1-C6 alkyl group, C1-C6 alkoxy or halogen independently. According to the invention, through the comprehensive selection and combination of the catalyst, additive, base, organic ligand and amine source compound, good synergistic effects are mutually achieved, so that the desired product is obtained with a high yield; the method can be used in the technical field of organic synthesis especially medicine intermediate synthesis.
Copper-catalyzed aerobic cascade cycloamination and acyloxylation: A direct approach to 4-acyloxy-1H-pyrazoles
Ding, Zhengwei,Tan, Qitao,Gao, Mingchun,Xu, Bin
, p. 4642 - 4646 (2015/04/27)
A novel direct transformation of hydrazones to acyloxylated pyrazoles by copper-catalyzed regioselective olefinic C(sp2)-H bond cycloamination and acyloxylation was performed under mild conditions, which combines the formation of the pyrazole skeleton and installation of an acyloxyl group in a single step, using facile carboxylic acids as the acyloxylation reagents.
