Isosteviol-amino acid conjugates were synthesized and used as chiral catalysts for the asymmetric three-component Mannich reaction with hydroxyacetone as donor molecule. Good yields （up to 98%） and excellent stereoselectivities （up to 97 ： 3 dr and 99% ee） were achieved in a short reaction time. In addition, syn- or anti-configurations of a-hydroxy-β-amino carbonyl compounds were obtained as main products with different chiral catalysts.
Isosteviol deravative with formyl group and vinyl moiety 1,an useful and easily available bioactive compound o...
An,Yajie Wu,Ya Liu,Congjun Yang,Jinghua Tao,Jingchao~* (Department of Chemistry,New Drug Research & Development center,Zhengzhou University,Zhengzhou 450052)
＜正＞The asymmetric aldol reaction is one of the most powerful methods for the construction of complex chiral po...
Liu Yu-Xia, SunYa-Nan, Tan Hao-Han, Wu Ya, Ma Zhi-Wei, Tao Jing-Chao Department of Chemistry, New Drug Research and Development Center, Zhengzhou University, Zhengzhou, 450052
A series of novel pyrazole fused heterocyclic derivatives were synthesized via a two-step procedure or a one-pot two step method, and their catalytic DNA cleavage abilities and anti-BVDV activities were also evaluated. The results obtained indicated that compounds 3b-3c could catalyze the cleavage of supercoiled DNA （pUC 19 plasmid DNA） to nicked DNA under physiological conditions with high yields via a hydrolytic mechanism. The studies on anti-viral activities against bovine viral diarrhea virus （BVDV） demonstrated that some of the pyrazole derivatives showed pronounced anti-BVDV activity with interesting ECso values and no significant cytotoxicity. Among them, compound 31 showed the highest antiviral activity （ECso = 0.12 μmol/L） and was 10 fold more than that of the positive control ribavirin （ECso = 1.3 μmol/L）, which provided a potential candidate for the development of anti-BVDV agents.
Chao HanYan-Chun GuoDan-Dan WangXing-Jie DaiFeng-Juan WuHuan-Fei LiuGui-Fu DaiJing-Chao Tao
＜正＞Asymmetric Mannich reactions provide a powerful method for synthesizing optically active β-amino carbonyl u...
An Ya-Jie,Zhang Yun-Xiao,Liu Zhao-Min,Zhang Tao,Tao Jing-Chao Department of Chemistry, New Drug Research and Development Center, Zhengzhou University, Zhengzhou 450052
＜正＞Isosteviol（ent-16-ketobeyeran-19-oic acid 1）,obtained by acid hydrolysis of stevioside,is a tetracyclic dit...
Tao Zhang,Li-Hong Gao,Yan-Ling Yang,Hai-Long Du,Zhong-Tai Song,Jing-Chao Tao~* Department of Chemistry,New Drug Research & Development Center,Zhengzhou University, Zhengzhou 450052,PR China
A large amount of interests have been raised in pyrazole derivatives that exhibit wide applications in the fie...
Liu,Congjun Wu,Ya Xu,Hao Lan,Yubao Zhao,Hua Tao,Jingchao~* (Department of Chemistry,New Drug Research & Development center,Zhengzhou University,Zhengzhou 450052)
