138175-50-5Relevant articles and documents
Potassium exchanged layered zirconium phosphate as base catalyst in Knoevenagel condensation
Curini, Massimo,Epifano, Francesco,Marcotullio, Maria Carla,Rosati, Ornelio,Tsadjout, Andre
, p. 355 - 362 (2002)
Potassium exchanged layered zirconium phosphate catalyzed Knoevenagel condensation of aldehydes and active methylene compounds gave the corresponding E configurated olefinic derivatives in solvent free conditions.
Synthesis of 2-cyanoacrylamides through Pd-catalyzed monohydration of methylenemalononitriles
Liu, Yingtian,Dang, Xinxin,He, Yu,Bai, Hudong,Chen, Xuehong,Li, Jun-Long,Fan, Junting,Jiang, Hezhong,Li, Jiahong
, p. 662 - 671 (2019/02/20)
A straightforward and efficient method has been developed for the synthesis of 2-cyanoacrylamide from 2-methylenemalononitriles through monohydration. A series of methylenemalononitriles underwent the reaction under mild and simple reaction conditions wit
Novel soluble myeloid cell leukemia sequence 1 (Mcl-1) inhibitor (E,E)-2-(benzylaminocarbonyl)-3-styrylacrylonitrile (4g) developed using a fragment-based approach
Zhang, Zhichao,Song, Ting,Li, Xiangqian,Wu, Zhiyong,Feng, Yingang,Xie, Feibo,Liu, Chengwu,Qin, Jianquan,Chen, Hongbo
supporting information, p. 141 - 149 (2013/03/13)
Based on a known nanomolar Bcl-2 homology domain 3 (BH3) mimetic 3-thiomorpholin-8-oxo-8H-acenaphtho[1,2-b] pyrrole-9-carbonitrile (S1, MW: 331), we applied a fragment-based approach to obtain BH3 mimetics with improved affinity and improved solubility in a water-ethanol (9:1) cosolvent. After the deconstruction of 1 (S1), we obtained fragment cyanoacetamide (4), which was determined to be a ligand efficiency (LE) hot part. After a rational optimization through fragment evolution beginning with fragment 4, a smaller Mcl-1 inhibitor (E,E)-2-(benzylaminocarbonyl)-3-styrylacrylonitrile (4g, MW: 288) with a 6-fold increase in affinity compared to 1 was obtained, as predicted by our optimization curve and identified by Mcl-1 protein nuclear magnetic resonance (NMR).