7556-37-8Relevant articles and documents
Application of metallide/palladium compound catalytic reduction system in reaction of removing allyl groups and deuteration reaction
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Paragraph 0041, (2018/07/30)
The invention discloses application of a metallide/palladium compound catalytic reduction system in reaction of removing allyl groups of a compound containing the allyl groups and deuteration reaction. The reaction comprises the following steps: under protection of nitrogen gas, suspending a palladium compound and a metallide in a solvent, stirring for 5 minutes, adding the compound containing theallyl groups, reacting for 0.5-36 hours at the temperature of minus 50-120 DEG C, adding ice water to stop reaction, regulating a pH value to 3.5 by using diluted hydrochloric acid, and carrying outsolvent extraction, drying by steaming and column-chromatography purification on reaction liquid to finish the reaction.
Pd-Catalyzed debenzylation and deallylation of ethers and esters with sodium hydride
Mao, Yujian,Liu, Ye,Hu, Yanwei,Wang, Liang,Zhang, Shilei,Wang, Wei
, p. 3016 - 3020 (2018/04/14)
Herein we demonstrate simply that the addition of Pd(OAc)2 as a promotor switches the reactivity of a commonly used base NaH to a nucleophilic reductant. The reactivity is engineered into a palladium-catalyzed reductive debenzylation and deallylation of aryl ethers and esters. This operationally simple, mild protocol displays a broad substrate scope and a broad spectrum of functional group tolerance (>50 examples) and high chemoselectivity toward aryl ethers over aliphatic structures. Moreover, the dual reactivity of NaH as a base and a reductant is demonstrated in efficient synthetic elaboration.
Scaffold hopping of sampangine: Discovery of potent antifungal lead compound against Aspergillus fumigatus and Cryptococcus neoformans
Jiang, Zhigan,Liu, Na,Dong, Guoqiang,Jiang, Yan,Liu, Yang,He, Xiaomeng,Huang, Yahui,He, Shipeng,Chen, Wei,Li, Zhengang,Yao, Jianzhong,Miao, Zhenyuan,Zhang, Wannian,Sheng, Chunquan
, p. 4090 - 4094 (2014/09/17)
Discovery of novel antifungal agents against Aspergillus fumigatus and Cryptococcus neoformans remains a significant challenge in current antifungal therapy. Herein the antifungal natural product sampangine was used as the lead compound for novel antifungal drug discovery. A series of D-ring scaffold hopping derivatives were designed and synthesized to improve antifungal activity and water solubility. Among them, the thiophene derivative S2 showed broad-spectrum antifungal activity, particularly for Aspergillus fumigatus and Cryptococcus neoformans. Moreover, compound S2 also revealed better water solubility than sampangine, which represents a promising antifungal lead compound for further structural optimization.