39806-90-1Relevant articles and documents
Regioselective Synthesis of C3-Hydroxyarylated Pyrazoles
O'Sullivan, Leonie,Patel, Ketul V.,Rowley, Ben C.,Brownsey, Duncan K.,Gorobets, Evgueni,Gelfand, Benjamin S.,Van Humbeck, Jeffrey F.,Derksen, Darren J.
supporting information, p. 846 - 854 (2021/12/27)
Pyrazoles are ubiquitous structures in medicinal chemistry. We report the first regioselective route to C3-hydroxyarylated pyrazoles obtained through reaction of pyrazole N-oxides with arynes using mild conditions. Importantly, this method does not requir
Method for synthesizing 1 - methyl -4 -iodo pyrazole (by machine translation)
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Paragraph 0034-0049; 0058-0065, (2020/06/16)
The invention relates to the technical field 1 - methyl -4 - iodinol synthesis, in particular to a synthesis method of 1 - methyl -4 - iodo pyrazole. The synthesis method of 1 - methyl -4 - iodinol comprises the following steps: (1) mixing 1 - methylpyrazole with iodine, heating to 40 - 80 °C, dropwise adding an oxidizing agent aqueous solution to carry out iodination reaction, and (2) adding alkali liquor to 5 - 9 DEG C to obtain a light yellow crystal, namely 1 - methyl -4 - iodo pyrazole. To 1 - methyl -4 - iodinol synthesis method, 1 - methylpyrazole raw materials are used as the iodinating agent, and an oxidizing agent, an oxidizing agent and hydrogen iodide are added to generate iodine, so that iodine is fully utilized, the reaction rate and product yield are improved, and the synthesis cost 1 - methyl -4 -iodo pyrazole is greatly reduced. (by machine translation)
Visible-Light-Induced [4+2] Annulation of Thiophenes and Alkynes to Construct Benzene Rings
Song, Chunlan,Dong, Xin,Wang, Zhongjie,Liu, Kun,Chiang, Chien-Wei,Lei, Aiwen
supporting information, p. 12206 - 12210 (2019/07/31)
The [4+2] annulation represents an elegant and versatile synthetic protocol for the construction of benzene rings. Herein, a strategy for visible-light induced [4+2] annulation of thiophenes and alkynes, to afford benzene rings, is presented. Under simple and mild reaction conditions, the ready availability and structural diversity of thiophenes and alkynes permit the facile synthesis of several substituted aromatic rings. Valuable drugs and amino acids are also well tolerated. Moreover, DFT calculations explain the high regioselectivity of the reaction.