376581-24-7Relevant articles and documents
Preparation method of benzoheterocyclic boric acid
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Paragraph 0062; 0064; 0066, (2018/09/13)
The invention provides a preparation method of benzoheterocyclic boric acid. The preparation method comprises steps as follows: (1) a benzoheterocyclic compound shown in a formula I is dissolved in asolvent A, a liquor A is obtained, a boronylation reagent is dissolved in a solvent B, a liquor B is obtained, a palladium catalyst and an alkaline reagent are immobilized on a channel of a continuousflow reactor, the liquor A and the liquor B are subjected to a continuous adding reaction, the reaction is stopped after the mixture flows out of a reaction tube, and an intermediate is obtained; (2)the intermediate obtained in step (1) is subjected to a hydrolysis reaction, and benzoheterocyclic boric acid is obtained. According to the provided preparation method, the benzoheterocyclic boric acid is synthesized with a flow chemical technology. Compared with methods in the prior art, the method has the advantages that the product yield is 86% or above, the highest yield can reach 90% or above, the yield is very high, the reaction rate is high, energy consumption of a reaction is reduced greatly, and the method is high in operability, high in automation degree and favorable for productionoperation and industrial production.
Flow Chemistry on Multigram Scale: Continuous Synthesis of Boronic Acids within 1 s
Hafner, Andreas,Meisenbach, Mark,Sedelmeier, Joerg
supporting information, p. 3630 - 3633 (2016/08/16)
The benefits and limitations of a simple continuous flow setup for handling and performing of organolithium chemistry on the multigram scale is described. The developed metalation platform embodies a valuable complement to existing methodologies, as it combines the benefits of Flash Chemistry (chemical synthesis on a time scale of 1 s) with remarkable throughput (g/min) while mitigating the risk of blockages.
