建立了一种简单、实用的光诱导一锅法高选择性N-甲基喹喔啉酮类化合物和苯乙酮类化合物合成一系列3-烷基化喹唑啉-2(1H)-酮类化合物的方法。该方法在室温条件下,以玫瑰红作为光催化剂,在18 W 460 nm的蓝色LED下照射8 h,通过直接C3-H活...建立了一种简单、实用的光诱导一锅法高选择性N-甲基喹喔啉酮类化合物和苯乙酮类化合物合成一系列3-烷基化喹唑啉-2(1H)-酮类化合物的方法。该方法在室温条件下,以玫瑰红作为光催化剂,在18 W 460 nm的蓝色LED下照射8 h,通过直接C3-H活化的方案,较好收率获得一系列相应的3-烷基化喹喔啉-2(1H)-酮类化合物,最高产率可达到76%。反应体系具有经济实用性和底物适用范围广的特点,为3-烷基化喹喔啉-2(1H)-酮类化合物类化合物的合成提供了一种简便经济的方法。展开更多
The important synthetic precursor(Ⅲ), 1-(prop-2-yn-1-yl)-7,8-dihydro-1Hbenzo[d][1,3]thiazine-2,5(4H,6H)-dione(C(11)H(11)NO2S), was prepared through a three-component reaction, which was further transferre...The important synthetic precursor(Ⅲ), 1-(prop-2-yn-1-yl)-7,8-dihydro-1Hbenzo[d][1,3]thiazine-2,5(4H,6H)-dione(C(11)H(11)NO2S), was prepared through a three-component reaction, which was further transferred into cytotoxic triazoles by alkylation and "click" synthesis in satisfactory yields of 87%^95%. Their structures were characterized by IR, H-RESI-MS and NMR analysis. Meanwhile, the crystal of Ⅲ was obtained and determined by X-ray single-crystal diffraction. Crystal data: orthorhombic system, space group P212121, a = 5.189(4), b = 8.661(6), c = 23.498(17) A, V = 1056.2(13) A^3, Z = 4, F(000) = 464, Dc = 1.392 g/cm^3, μ =0.284 mm^-1, R = 0.0637 and wR = 0.1668 for 8182 independent reflections(R(int) = 0.1580) and 2166 observed ones(I 〉 2σ(I)).展开更多
文摘建立了一种简单、实用的光诱导一锅法高选择性N-甲基喹喔啉酮类化合物和苯乙酮类化合物合成一系列3-烷基化喹唑啉-2(1H)-酮类化合物的方法。该方法在室温条件下,以玫瑰红作为光催化剂,在18 W 460 nm的蓝色LED下照射8 h,通过直接C3-H活化的方案,较好收率获得一系列相应的3-烷基化喹喔啉-2(1H)-酮类化合物,最高产率可达到76%。反应体系具有经济实用性和底物适用范围广的特点,为3-烷基化喹喔啉-2(1H)-酮类化合物类化合物的合成提供了一种简便经济的方法。
基金Supported by the National Natural Science Foundation of China(No.21272136)Scientific Foundation from graduate school(2015CX131)Youth Talent Development Foundation of China Three Gorges University
文摘The important synthetic precursor(Ⅲ), 1-(prop-2-yn-1-yl)-7,8-dihydro-1Hbenzo[d][1,3]thiazine-2,5(4H,6H)-dione(C(11)H(11)NO2S), was prepared through a three-component reaction, which was further transferred into cytotoxic triazoles by alkylation and "click" synthesis in satisfactory yields of 87%^95%. Their structures were characterized by IR, H-RESI-MS and NMR analysis. Meanwhile, the crystal of Ⅲ was obtained and determined by X-ray single-crystal diffraction. Crystal data: orthorhombic system, space group P212121, a = 5.189(4), b = 8.661(6), c = 23.498(17) A, V = 1056.2(13) A^3, Z = 4, F(000) = 464, Dc = 1.392 g/cm^3, μ =0.284 mm^-1, R = 0.0637 and wR = 0.1668 for 8182 independent reflections(R(int) = 0.1580) and 2166 observed ones(I 〉 2σ(I)).