23564-83-2Relevant academic research and scientific papers
An eco-friendly approach for the synthesis of 1,2,5-trisubstituted and 4-amino-1,2,5-tetrasubstituted imidazoles via a multi-component condensation
Mehrabi, Hossein,Alizadeh-Bami, Farzaneh,Meydani, Azam,Besharat, Soheila
, p. 86 - 95 (2021/04/02)
The synthesis of 1,2,5-trisubstituted and 4-amino-1,2,5-tetrasubstituted imidazoles was demonstrated via a two-step cyclo-condensation reaction of aryl amines, carbonitriles, and ethyl bromopyruvate or aryl amines and arylglyoxals in ethanol heated under
Synthesis of 1,2,4,5-tetrasubstituted imidazoles and 2,4,5,6-tetrasubstituted pyrimidines: three-component, the one-pot reaction of arylamidines, malononitrile, and arylglyoxals or aryl aldehydes
Alizadeh-Bami, Farzaneh,Hajipour, Mina,Mehrabi, Hossein,Rezazadeh-Jabalbarezi, Fatemeh
, (2020/07/16)
A highly efficient one-pot synthesis of the 1,2,4,5-tetrasubstituted imidazoles and 2,4,5,6-tetrasubstituted pyrimidines through an arylamidine, malononitrile, and carbonyl compound by using Et3N in CH3CN at reflux conditions was dev
Nickel-Catalyzed Annulation of o-Haloarylamidines with Aryl Acetylenes: Synthesis of Isoquinolone and 1-Aminoisoquinoline Derivatives
Xie, Hao,Xing, Qiaoyan,Shan, Zhifei,Xiao, Fuhong,Deng, Guo-Jun
supporting information, p. 1896 - 1901 (2019/03/07)
An efficient method for the synthesis of substituted 1(2H)-isoquinolone derivatives via nickel-catalyzed annulation of substituted 2-halobenzamidines with aryl alkynes in the presence of water is described. Benzo[4,5]imidazo[2,1-a]isoquinolines were formed as the dominated products when dry dimethyl sulfoxide was used as the solvent. Furthermore, when benzyl substituted amidines were used as the substrates, debenzylation reaction occured to provide various 1-aminoisoquinoline products. (Figure presented.).
Efficient synthesis of 1,2-benzisothiazoles from: O -haloarylamidines and elemental sulfur via N-S/C-S bond formation under transition-metal-free conditions
Xie, Hao,Li, Guozheng,Zhang, Feng,Xiao, Fuhong,Deng, Guo-Jun
supporting information, p. 827 - 831 (2018/03/02)
An efficient method for the synthesis of 1,2-benzisothiazoles from amidines and elemental sulfur via N-S/C-S bond formation under transition-metal-free conditions is described. This reaction is performed smoothly under simple conditions to give the corresponding products in good to high yields with good functional group tolerance.
Optimization of imidazole amide derivatives as cannabinoid-1 receptor antagonists for the treatment of obesity
Smith, Roger A.,Fathi, Zahra,Achebe, Furahi,Akuche, Christiana,Brown, Su-Ellen,Choi, Soongyu,Fan, Jianmei,Jenkins, Susan,Kluender, Harold C.E.,Konkar, Anish,Lavoie, Rico,Mays, Ronald,Natoli, Jennifer,O'Connor, Stephen J.,Ortiz, Astrid A.,Su, Ning,Taing, Christy,Tomlinson, Susan,Tritto, Theresa,Wang, Gan,Wirtz, Stephan-Nicholas,Wong, Wai,Yang, Xiao-Fan,Ying, Shihong,Zhang, Zhonghua
, p. 2706 - 2711 (2008/12/20)
Several imidazole-based cyclohexyl amides were identified as potent CB-1 antagonists, but they exhibited poor oral exposure in rodents. Incorporation of a hydroxyl moiety on the cyclohexyl ring provided a dramatic improvement in oral exposure, together with a ca. 10-fold decrease in potency. Further optimization provided the imidazole 2-hydroxy-cyclohexyl amide 45, which exhibited hCB-1 Ki = 3.7 nM, and caused significant appetite suppression and robust, dose-dependent reduction of body weight gain in industry-standard rat models.
