Unsymmetrical hybrid chiral phosphine-aminophosphine ligand derived from 1,2,3,4-tetrahydro-l-naphthyl- amine has been found to be highly efficient in the Ir-catalyzed asymmetric hydrogenation of various 3-aryl-2H-1,4...Unsymmetrical hybrid chiral phosphine-aminophosphine ligand derived from 1,2,3,4-tetrahydro-l-naphthyl- amine has been found to be highly efficient in the Ir-catalyzed asymmetric hydrogenation of various 3-aryl-2H-1,4-benzoxazines, providing good enantioselectivities （up to 95% ee） and high catalytic activity （S/C up to 5000）.展开更多
转录反式激活因子(trans-activator of transcription,Tat)在HIV-1的转录中起着重要的调控作用,针对HIV-1 Tat中的β-转角结构,采用2H-1,4-苯并二氮-2-酮作为β-转角肽链骨架的模拟结构,分别以对硝基氯苯/苯乙腈、对甲基苯胺/苯甲酰氯...转录反式激活因子(trans-activator of transcription,Tat)在HIV-1的转录中起着重要的调控作用,针对HIV-1 Tat中的β-转角结构,采用2H-1,4-苯并二氮-2-酮作为β-转角肽链骨架的模拟结构,分别以对硝基氯苯/苯乙腈、对甲基苯胺/苯甲酰氯以及硝西泮为起始原料,采用不同合成路线得到了19个2H-1,4-苯并二氮-2-酮类化合物(10～18、21～24、26～31)。初步活性评价表明,化合物30在没有明显细胞毒作用的浓度下对Tat介导的荧光素酶的表达显示了较好的抑制作用,其半数有效浓度EC50为25.0μmol·L-1。展开更多
2H-3, 1-Benzoxazine derivatives were synthesized by cyclocondensation of 5-nitro-2- cyanoaniline with relative ketone or aldehyde with ZnCl2 as a catalyst. This is a new efficient synthetic route of 2H-3, 1-benzoxazin...2H-3, 1-Benzoxazine derivatives were synthesized by cyclocondensation of 5-nitro-2- cyanoaniline with relative ketone or aldehyde with ZnCl2 as a catalyst. This is a new efficient synthetic route of 2H-3, 1-benzoxazine cyclic compounds.展开更多
The synthesis of an new photochromical compound,1,3,3 trimethyl 6′ (1 piperidinyl) spiro[2h indole 2,3′ [3H]pyridobenzoxazine (SP3),and an improved way for the synthesis of 6 hydroxyquinoline were descrided.The abso...The synthesis of an new photochromical compound,1,3,3 trimethyl 6′ (1 piperidinyl) spiro[2h indole 2,3′ [3H]pyridobenzoxazine (SP3),and an improved way for the synthesis of 6 hydroxyquinoline were descrided.The absorption spectrum of the colored metastable form SP3 shows prominent absorption peak at 560nm at 60℃?展开更多
文摘Unsymmetrical hybrid chiral phosphine-aminophosphine ligand derived from 1,2,3,4-tetrahydro-l-naphthyl- amine has been found to be highly efficient in the Ir-catalyzed asymmetric hydrogenation of various 3-aryl-2H-1,4-benzoxazines, providing good enantioselectivities （up to 95% ee） and high catalytic activity （S/C up to 5000）.
文摘转录反式激活因子(trans-activator of transcription,Tat)在HIV-1的转录中起着重要的调控作用,针对HIV-1 Tat中的β-转角结构,采用2H-1,4-苯并二氮-2-酮作为β-转角肽链骨架的模拟结构,分别以对硝基氯苯/苯乙腈、对甲基苯胺/苯甲酰氯以及硝西泮为起始原料,采用不同合成路线得到了19个2H-1,4-苯并二氮-2-酮类化合物(10～18、21～24、26～31)。初步活性评价表明,化合物30在没有明显细胞毒作用的浓度下对Tat介导的荧光素酶的表达显示了较好的抑制作用,其半数有效浓度EC50为25.0μmol·L-1。
文摘2H-3, 1-Benzoxazine derivatives were synthesized by cyclocondensation of 5-nitro-2- cyanoaniline with relative ketone or aldehyde with ZnCl2 as a catalyst. This is a new efficient synthetic route of 2H-3, 1-benzoxazine cyclic compounds.
文摘The synthesis of an new photochromical compound,1,3,3 trimethyl 6′ (1 piperidinyl) spiro[2h indole 2,3′ [3H]pyridobenzoxazine (SP3),and an improved way for the synthesis of 6 hydroxyquinoline were descrided.The absorption spectrum of the colored metastable form SP3 shows prominent absorption peak at 560nm at 60℃?
