81912-50-7Relevant articles and documents
Weak coordinated nitrogen functionality enabled regioselective C-H alkynylationviaPd(ii)/mono-N-protected amino acid catalysis
Liu, Bifu,Ouyang, Wensen,Nie, Jianhong,Gao, Yang,Feng, Kejun,Huo, Yanping,Chen, Qian,Li, Xianwei
, p. 11255 - 11258 (2020/10/06)
The exploration of weak coordinated amine derivative enabled regioselective C-H functionalization remains challenging due to the elusive achievement of reactivity and selectivity simultaneously. Herein, regioselective C-H alkynylation of various readily transformable nitrogen functionalities was developed with great efficiency, with the assistance of the mono-N-protected amino acid (MPAA) ligandviaPd(ii) catalysis proceedingvia5, 6 and 7-membered palladacycle intermediates.
A novel method for synthesizing N-alkoxycarbonyl aryl α-imino esters and their applications in enantioselective transformations
Qian, Yu,Jing, Changcheng,Zhai, Changwei,Hu, Wen-Hao
, p. 301 - 307 (2012/04/04)
A new strategy for the synthesis of N-alkoxycarbonyl aryl α-imino esters in the presence of dirhodium tetraacetate [Rh2(OAc) 4] is reported to produce the desired compounds in high yield (up to 96%) under mild reaction conditions. The application of the synthetic method is demonstrated in enantioselective reduction and Friedel-Crafts reaction of indoles to afford the corresponding chiral arylglycines and indole derivatives, respectively, in high yield and excellent ee. Copyright
Tricyclononene carboxamide derivatives as novel anti-HIV-1 agents
Dong, Ming-Xin,Zhang, Jian,Peng, Xu-Qing,Lu, Hong,Yun, Liu-Hong,Jiang, Shibo,Dai, Qiu-Yun
scheme or table, p. 4096 - 4103 (2010/10/02)
By modifying the chemical structure of anti-orthopoxvirus compound ST-246, we designed and synthesized a series of tricyclononene carboxamide derivatives and tested their anti-HIV-1 activity and cytotoxicity. We found that benzoimidazol-containing compound 7g was highly effective in inhibiting HIV-1 R5 infection with an IC50 value of 0.41 μM and a selectivity index of 292, but it exhibited no significant inhibitory activity on HIV-1 reverse transcriptase, integrase and protease. CoMFA was used to analyze structure-activity relationships with good predictive power (r2 = 0.921; q2 = 0.582). Moreover, the CoMFA model showed that the length of the molecule, the amide, and the amine moieties all played crucial roles in anti-HIV activity. These results suggest that 7g may serve as a lead for the development of novel anti-HIV-1 therapies. A series of tricyclononene carboxamide derivatives based on anti-orthopoxvirus compound ST-246 were synthesized and characterized as novel anti-HIV-1 agents.