105273-93-6Relevant articles and documents
Method for synthesizing 1,5-benzodiazepine compound
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Paragraph 0078-0080, (2019/12/25)
The invention discloses a method for synthesizing a 1,5-benzodiazepine compound. The method specifically comprises the following steps: dissolving a gold catalyst, an additive, alkyne of a formula IIshown in the specification, an o-phenylenediamine derivative of a formula III shown in the specification into an organic solvent, putting the solution into a pressure-resistant reaction tube, performing a stirring reaction for 6-24 hours at 25 DEG C so as to obtain a reaction liquid, and performing aftertreatment on the reaction liquid so as to obtain the 1,5-benzodiazepine compound of a formula IV shown in the specification, wherein the mass ratio of the gold catalyst of a formula I shown in the specification to the additive to the alkyne of the formula II shown in the specification to the o-phenylenediamine derivative of the formula III shown in the specification is (0.01-0.07):(0-0.1):(2.0-3.0):1. By adopting the method disclosed by the invention, a double-functional catalyst is used, the reaction can be performed under a room temperature condition, and thus energy consumption can be reduced; and the method has the advantages of being small in catalyst amount, high in yield, good insubstrate universality, simple and convenient in operation, and the like.
Gold(I)-catalyzed synthesis of 1,5-benzodiazepines directly from o-phenylenediamines and alkynes
Qian, Jianqiang,Liu, Yunkui,Cui, Jianhai,Xu, Zhenyuan
experimental part, p. 4484 - 4490 (2012/06/18)
A unique gold(I)-catalyzed highly atom-economic synthesis of 1,5-benzodiazepines directly from o-phenylenediamines and alkynes has been achieved for the first time.
