534599-79-6Relevant academic research and scientific papers
Catalytic asymmetric construction of C-4 alkenyl substituted pyrazolone derivatives bearing multiple stereoelements
Qu, Jingping,Wang, Baomin,Wang, Wenyao,Wei, Shiqiang,Zhang, Wande
supporting information, p. 6550 - 6553 (2021/07/07)
An organocatalytic asymmetric process was reported for the sterically precise construction of C-4 alkenyl substituted pyrazolone derivatives bearing multiple stereoelements. A series of interesting products featuring the union of a centrally chiral pyrazolone moiety and an axially chiral styrene unit were obtained in high yield with excellent diastereoselectivity and enantioselectivity (up to 99% ee, >20?:?1 dr). The process has the characteristics of mild reaction conditions, simple operation and broad substrate scope. The result of gram-scale reaction indicates that the reaction has good practicability.
Substituted 3-benzylcoumarins as allosteric MEK1 inhibitors: Design, synthesis and biological evaluation as antiviral agents
Wang, Chao,Zhang, Hao,Xu, Fengrong,Niu, Yan,Wu, Yun,Wang, Xin,Peng, Yihong,Sun, Jing,Liang, Lei,Xu, Ping
, p. 6057 - 6091 (2013/06/27)
In order to find novel antiviral agents, a series of allosteric MEK1 inhibitors were designed and synthesized. Based on docking results, multiple optimizations were made on the coumarin scaffold. Some of the derivatives showed excellent MEK1 binding affinity in the appropriate enzymatic assays and displayed obvious inhibitory effects on the ERK pathway in a cellular assay. These compounds also significantly inhibited virus (EV71) replication in HEK293 and RD cells. Several compounds showed potential as agents for the treatment of viral infective diseases, with the most potent compound 18 showing an IC 50 value of 54.57 nM in the MEK1 binding assay.
Heck reaction of Baylis-Hillman adducts with iodobenzenes using a catalytic amount of Pd/C under solvent-free conditions
Kim, Hyun-Soo,Lee, Sang-Jin,Choi, Boram,Yoon, Cheol Min
, p. 3161 - 3164 (2012/11/13)
The reaction of Baylis-Hillman adducts with iodobenzenes using commercially available palladium-on-carbon as a catalyst under solvent-free conditions afforded the corresponding coupling products, α-benzyl-β-keto esters, in high to excellent yields. The reactions are very efficient.
Nájera oxime-derived palladacycles catalyze intermolecular Heck reaction with Morita-Baylis-Hillman adducts. An improved and highly efficient synthesis of α-benzyl-β-ketoesters
Ferreira, Bruno R.V.,Pirovani, Rodrigo V.,Souza-Filho, Luis G.,Coelho, Fernando
experimental part, p. 7712 - 7717 (2009/12/03)
An improved and highly efficient synthesis of several α-benzyl-β-ketoesters from Morita-Baylis-Hillman adducts is described. These adducts were used as substrates for an intermolecular Heck reaction catalyzed by a Na?jera oxime-derived palladacycles. These efficient catalytic conditions probed to be very selective providing only the corresponding functionalized β-ketoesters in high yield with no decarboxylation product. It seems that the method herein described is one of the most efficient for the synthesis of α-benzyl-β-ketoesters.
