28150-91-6Relevant articles and documents
A Synthesis of Spirooxindole-Isoindolinones Through Ugi Reaction Followed by Copper-Catalyzed Tandem C?N/C?C Coupling Process
Zhong, Xianqiang,Luo, Jianghao,Zhou, Wei,Cai, Qian
, p. 4969 - 4973 (2021/09/14)
A synthesis of spiroindolinone-isoindolinone skeletons is presented. The protocol is through a Ugi four-component reaction followed by highly efficient and mild copper-catalyzed intramolecular tandem C?N/C?C coupling process. Control experiments demonstra
Organocatalytic double arylation of 3-isothiocyanato oxindoles: Stereocontrolled synthesis of complex spirooxindoles
Zhang, Lin-Lin,Da, Bing-Chao,Xiang, Shao-Hua,Zhu, Shuai,Yuan, Zi-Yun,Guo, Zhen,Tan, Bin
, p. 1689 - 1696 (2018/11/25)
Quinones, precursors of aromatic structures, were firstly employed as the electrophiles for the organocatalytic Michael addition/cyclization cascade reaction with versatile 3-isothiocyanato oxindoles. Chiral bifunctional organocatalyst was appropriate for this enantioselective transformation to afford a variety of novel spirooxindoles, possessing a spirocyclic stereocenter adjacent to the aromatic ring, via asymmetric double arylation. These synthesized spirooxindoles are very difficult to access by the reported methods and were obtained in excellent chemical yields with excellent enantioselectivities.
Synthesis and in vitro evaluation of neutral aryloximes as reactivators of Electrophorus eel acetylcholinesterase inhibited by NEMP, a VX surrogate
Cavalcante, Samir F. de A.,Kitagawa, Daniel A.S.,Rodrigues, Rafael B.,Bernardo, Leandro B.,da Silva, Thiago N.,dos Santos, Wellington V.,Correa, Ana Beatriz de A.,de Almeida, Joyce S.F.D.,Fran?a, Tanos C.C.,Ku?a, Kamil,Simas, Alessandro B.C.
, (2019/06/24)
Casualties caused by nerve agents, potent acetylcholinesterase inhibitors, have attracted attention from media recently. Poisoning with these chemicals may be fatal if not correctly addressed. Therefore, research on novel antidotes is clearly warranted. Pyridinium oximes are the only clinically available compounds, but poor penetration into the blood-brain barrier hampers efficient enzyme reactivation at the central nervous system. In searching for structural factors that may be explored in SAR studies, we synthesized and evaluated neutral aryloximes as reactivators for acetylcholinesterase inhibited by NEMP, a VX surrogate. Although few tested compounds reached comparable reactivation results with clinical standards, they may be considered as leads for further optimization.
