94066-12-3Relevant academic research and scientific papers
New catalytic effect of thiourea on the oxidative cyanation of N-aryltetrahydroisoquinolines
Ullah, Bakhtar,Zhou, Yuli,Chen, Jingwen,Bao, Zongbi,Yang, Yiwen,Yang, Qiwei,Ren, Qilong,Zhang, Zhiguo
, p. 348 - 351 (2019)
Thiourea itself has been introduced as a mild and efficient organocatalyst for the oxidative α -cyanation of N-aryltetrahydroisoquinolines (THIQs) with trimethylsilyl cyanide (TMSCN), giving the corresponding products in good to excellent yields. Experime
Electrochemically promoted oxidative α-cyanation of tertiary and secondary amines using cheap AIBN
Cai, Tian-Cheng,Gui, Qing-Wen,Hu, Wenxia,Li, Qiang,Liu, Xiaoying,Teng, Fan,Wang, Xiaoli,Xiong, Zhi-Yuan,Yu, Jialing
supporting information, p. 8254 - 8258 (2021/10/12)
The electrochemical α-cyanation of tertiary and secondary amines has been developed by using a cheap cyanide reagent, azobisisobutyronitrile (AIBN). The CN radical, generated throughn-Bu4NBr-meidated electrochemical oxidation, participates in a novel α-cyanation reaction under exogenous oxidant-free conditions.
A class of promising acaricidal tetrahydroisoquinoline derivatives: Synthesis, biological evaluation and structure-activity relationships
Yang, Rui,Ruan, Qiao,Zhang, Bing-Yu,Zheng, Zuo-Lue,Miao, Fang,Zhou, Le,Geng, Hui-Ling
, p. 8051 - 8066 (2014/07/08)
As part of our continuing research on isoquinoline acaricidal drugs, this paper reports the preparation of a series of the 2-aryl-1-cyano-1,2,3,4- tetrahydroisoquinolines with various substituents on the N-phenyl ring, their in vitro acaricidal activities against Psoroptes cuniculi, a mange mite, and discusses their SAR as well. The structures of all compounds, including 12 new ones, were elucidated by analysis of UV, IR, NMR, ESI-MS, HR-MS spectra and X-ray diffraction experiments. All target compounds showed varying degrees of activity at 0.4 mg/mL. Compound 1 showed the strongest activity, with a 50% lethal concentration value (LC50) of 0.2421 μg/mL and 50% lethal time value (LT50) of 7.79 h, comparable to the standard drug ivermectin (LC50 = 0.2474 μg/mL; LT50 = 20.9 h). The SAR showed that the substitution pattern on the N-aromatic ring exerted a significant effect on the activity. The substituents 2′-F, 3′-F, 2′-Cl, 2′-Br and 2′-CF3 remarkably enhanced the activity. Generally, for the isomers with the same substituents at different positions, the order of the activity was ortho > meta > para. It was concluded that the target compounds represent a class of novel promising candidates or lead compounds for the development of new tetrahydroisoquinoline acaricidal agents.
