An efficient synthesis of 3,4-dihydropyrimidine 2 （1H）-ones and thiones （3,4-DHPMs） core was prepared by one-pot threecomponent Biginelli condensation and which was catalyzed by trifluoromethane sulfonic acid. The...An efficient synthesis of 3,4-dihydropyrimidine 2 （1H）-ones and thiones （3,4-DHPMs） core was prepared by one-pot threecomponent Biginelli condensation and which was catalyzed by trifluoromethane sulfonic acid. The classical BigneUi reaction has been extended by the use of N-substituted benzoxazolyl semicarbazides and thiosemicarbazides and this method has the advantage of excellent yields and short reaction times. ？2009 M. Saranga Pard. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.展开更多
Aspartic acid and glutamic acid with protected α-amino and α-carboxyl groups had been used to react with the activated hydroxyl group of N-substituted 3,4-fullero pyrrolidine. The products were deprotected, affordin...Aspartic acid and glutamic acid with protected α-amino and α-carboxyl groups had been used to react with the activated hydroxyl group of N-substituted 3,4-fullero pyrrolidine. The products were deprotected, affording two monofuUerene α-amino acids, monofullerene aspartic acid （mFas） and monofullerene glutamic acid （mFgu）. Then a bifullerene glutamic acid conjugate （bFguC） was synthesized by reaction of mFgu containing protected amino group with N-substituted 3,4-fullero pyrrolidine.展开更多
Eleven novel triterpenoid saponins,N-substituted-β-D-glucosaminide derivatives of oleanolic acid,were designed and synthesized via a stepwise glycosylation strategy.These compounds were evaluated for in vitro cytotox...Eleven novel triterpenoid saponins,N-substituted-β-D-glucosaminide derivatives of oleanolic acid,were designed and synthesized via a stepwise glycosylation strategy.These compounds were evaluated for in vitro cytotoxic activity against six different tumor cell lines.Most of the compounds inhibited the growth of,at least,one tumor cell line effectively at micromolar concentrations.Preliminary structure-activity relationships（SARs） indicate that acylation of the nitrogen of the glucosamine-bearing triterpenoid saponins affords the compounds that are highly cytotoxic towards specific tumor cell lines.展开更多
美味猕猴桃(Actinidia deliciosaa C.F.liang et A. R. Ferguson)的试管苗离体腋芽,在附加.BA(3.0μg/g)、IBA(0.5μg/g)、GA(0.5μg/g)的MS培养基上,腋芽的萌发率达100%,可以代替昂贵的玉米素(ZT);用5μg/g NAA加在MS培养基中,促使小...美味猕猴桃(Actinidia deliciosaa C.F.liang et A. R. Ferguson)的试管苗离体腋芽,在附加.BA(3.0μg/g)、IBA(0.5μg/g)、GA(0.5μg/g)的MS培养基上,腋芽的萌发率达100%,可以代替昂贵的玉米素(ZT);用5μg/g NAA加在MS培养基中,促使小苗生根,生根率达100%,平均每株生根数19.9条;待茎木质化后移栽,移栽成活率在80%以上。美味猕猴桃种质试管苗,在MS培养基中附加50μg/g的B_9(N-dimethyl-succinamic acid),室温(8℃～34℃)下保存9个月后存活率达85%。展开更多
An efficient regioselective Friedel-Crafts hydroxyalkylation of N-substituted glyoxylamide with various indoles catalyzed by Lewis acids was developed. The reactions proceeded smoothly at room temperature and the 2-hy...An efficient regioselective Friedel-Crafts hydroxyalkylation of N-substituted glyoxylamide with various indoles catalyzed by Lewis acids was developed. The reactions proceeded smoothly at room temperature and the 2-hydroxy-2-（1H-indol-3-yl）-N-substituted acetamide resulted from the reactions catalyzed by FeSO4 were synthesized in excellent yields （up to 93%）. While the bisindole compounds were obtained when FeCl3 was used as a catalyst in excellent yields （up to 92%）. A possible mechanism was proposed.展开更多
文摘An efficient synthesis of 3,4-dihydropyrimidine 2 （1H）-ones and thiones （3,4-DHPMs） core was prepared by one-pot threecomponent Biginelli condensation and which was catalyzed by trifluoromethane sulfonic acid. The classical BigneUi reaction has been extended by the use of N-substituted benzoxazolyl semicarbazides and thiosemicarbazides and this method has the advantage of excellent yields and short reaction times. ？2009 M. Saranga Pard. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.
基金the National Natural ScienceFoundation of China(No.20672012).
文摘Aspartic acid and glutamic acid with protected α-amino and α-carboxyl groups had been used to react with the activated hydroxyl group of N-substituted 3,4-fullero pyrrolidine. The products were deprotected, affording two monofuUerene α-amino acids, monofullerene aspartic acid （mFas） and monofullerene glutamic acid （mFgu）. Then a bifullerene glutamic acid conjugate （bFguC） was synthesized by reaction of mFgu containing protected amino group with N-substituted 3,4-fullero pyrrolidine.
基金Supported by the National Natural Science Foundation of China（Nos.21142010, 81273358） and the PhD Scientific Research Opening Foundation Projects of Liaoning Province of China（No.20091081）.
文摘Eleven novel triterpenoid saponins,N-substituted-β-D-glucosaminide derivatives of oleanolic acid,were designed and synthesized via a stepwise glycosylation strategy.These compounds were evaluated for in vitro cytotoxic activity against six different tumor cell lines.Most of the compounds inhibited the growth of,at least,one tumor cell line effectively at micromolar concentrations.Preliminary structure-activity relationships（SARs） indicate that acylation of the nitrogen of the glucosamine-bearing triterpenoid saponins affords the compounds that are highly cytotoxic towards specific tumor cell lines.
文摘美味猕猴桃(Actinidia deliciosaa C.F.liang et A. R. Ferguson)的试管苗离体腋芽,在附加.BA(3.0μg/g)、IBA(0.5μg/g)、GA(0.5μg/g)的MS培养基上,腋芽的萌发率达100%,可以代替昂贵的玉米素(ZT);用5μg/g NAA加在MS培养基中,促使小苗生根,生根率达100%,平均每株生根数19.9条;待茎木质化后移栽,移栽成活率在80%以上。美味猕猴桃种质试管苗,在MS培养基中附加50μg/g的B_9(N-dimethyl-succinamic acid),室温(8℃～34℃)下保存9个月后存活率达85%。
基金the National Natural Science Foundation of China (Nos. 21472130, 81373259) for financial support of this study
文摘An efficient regioselective Friedel-Crafts hydroxyalkylation of N-substituted glyoxylamide with various indoles catalyzed by Lewis acids was developed. The reactions proceeded smoothly at room temperature and the 2-hydroxy-2-（1H-indol-3-yl）-N-substituted acetamide resulted from the reactions catalyzed by FeSO4 were synthesized in excellent yields （up to 93%）. While the bisindole compounds were obtained when FeCl3 was used as a catalyst in excellent yields （up to 92%）. A possible mechanism was proposed.
