研究1-苯基吡唑啉类化合物的合成及其EcMetAP酶活抑制活性。以查尔酮衍生物与苯肼为原料合成啉类化合物。利用IR、1 H NMR和MS对它们进行表征。利用分光光度法测试化合物的EcMetAP酶活性抑制作用,利用生物分子结构分析软件FieldTemplate...研究1-苯基吡唑啉类化合物的合成及其EcMetAP酶活抑制活性。以查尔酮衍生物与苯肼为原料合成啉类化合物。利用IR、1 H NMR和MS对它们进行表征。利用分光光度法测试化合物的EcMetAP酶活性抑制作用,利用生物分子结构分析软件FieldTemplater和FieldAlign计算化合物和已知的EcMetAP酶抑制剂的空间作用力场的相似性。共合成了6个1-苯基-3-(2-羟基苯基-5-芳基)-2-吡唑啉类化合物,但只有化合物5对EcMetAP酶活性有抑制作用,抑制率为31.62%,空间作用力场的相似度为0.615。说明化合物5可作为先导化合物进行结构优化,得到优良的EcMetAP酶抑制活性化合物。展开更多
Some novel spiro-acetals of 5-trimethylsilylcyclohex-2(or 3)-enone were synthesized from the reaction of silylcyclohexenones with the corresponding a, ω-diols in the presence of oxalic acid or adipic acid.
A simple and eco-friendly method for the preparation of 1,5-diaryl-3-（arylamino）-lH-pyrrol-2（5H）-ones via the cyclo-condensation reaction of aldehydes, amines and ethyl pyruvate in the presence of silica supported...A simple and eco-friendly method for the preparation of 1,5-diaryl-3-（arylamino）-lH-pyrrol-2（5H）-ones via the cyclo-condensation reaction of aldehydes, amines and ethyl pyruvate in the presence of silica supported ferric chlo- ride （SiO2-FeCl3） as reusable heterogeneous catalyst is described. The present methodology offers several advantages such as excellent yields, simple procedure and short reaction times.展开更多
A series of（Z）-2-chloro-1,3-diarylpropen-1-ones were unexpectedly synthesized in moderate yields by treatment of easily available 2,3-epoxy-1,3-diarylpropan-1-ones with Vilsmeier reagent,which was derived from bis（...A series of（Z）-2-chloro-1,3-diarylpropen-1-ones were unexpectedly synthesized in moderate yields by treatment of easily available 2,3-epoxy-1,3-diarylpropan-1-ones with Vilsmeier reagent,which was derived from bis（trichloromethyl） carbonate（BTC, triphosgene） and DMF.A possible mechanism was also proposed,where sequential ring-opening,halogenation and elimination reactions were involved.展开更多
A convenient and efficient method was developed for the synthesis of 2,2＇-（arylmethylene）bis（3-hydrox- ycyclohex-2-enone） derivatives via the oleylamine-catalyzed tandem Knoevenagel/Michael addition reactions of ...A convenient and efficient method was developed for the synthesis of 2,2＇-（arylmethylene）bis（3-hydrox- ycyclohex-2-enone） derivatives via the oleylamine-catalyzed tandem Knoevenagel/Michael addition reactions of aromatic aldehydes and cyclohexane-1,3-diones. This transformation proceeded without any metal catalyst in non-toxic solvent at room temperature with high isolated yields. A plausible mechanism for this process was pro- posed.展开更多
文摘研究1-苯基吡唑啉类化合物的合成及其EcMetAP酶活抑制活性。以查尔酮衍生物与苯肼为原料合成啉类化合物。利用IR、1 H NMR和MS对它们进行表征。利用分光光度法测试化合物的EcMetAP酶活性抑制作用,利用生物分子结构分析软件FieldTemplater和FieldAlign计算化合物和已知的EcMetAP酶抑制剂的空间作用力场的相似性。共合成了6个1-苯基-3-(2-羟基苯基-5-芳基)-2-吡唑啉类化合物,但只有化合物5对EcMetAP酶活性有抑制作用,抑制率为31.62%,空间作用力场的相似度为0.615。说明化合物5可作为先导化合物进行结构优化,得到优良的EcMetAP酶抑制活性化合物。
基金Supported by NSFC and Youth Foundation of Tianjin
文摘Some novel spiro-acetals of 5-trimethylsilylcyclohex-2(or 3)-enone were synthesized from the reaction of silylcyclohexenones with the corresponding a, ω-diols in the presence of oxalic acid or adipic acid.
文摘A simple and eco-friendly method for the preparation of 1,5-diaryl-3-（arylamino）-lH-pyrrol-2（5H）-ones via the cyclo-condensation reaction of aldehydes, amines and ethyl pyruvate in the presence of silica supported ferric chlo- ride （SiO2-FeCl3） as reusable heterogeneous catalyst is described. The present methodology offers several advantages such as excellent yields, simple procedure and short reaction times.
基金the National Natural Science Foundation of China(Nos.20806073 and 20876147)the National Key Technology Research and Development Program(No.2007BAI34B06) for financial support
文摘A series of（Z）-2-chloro-1,3-diarylpropen-1-ones were unexpectedly synthesized in moderate yields by treatment of easily available 2,3-epoxy-1,3-diarylpropan-1-ones with Vilsmeier reagent,which was derived from bis（trichloromethyl） carbonate（BTC, triphosgene） and DMF.A possible mechanism was also proposed,where sequential ring-opening,halogenation and elimination reactions were involved.
基金Supported by the National Natural Science Foundation of China（Nos.21772001, 21372008）, the Natural Science Foundation of Education Administration of Anhui Province, China（No.KJ2016A267）, the Special and Excellent Research Fund of Anhui Normal Universit and the Doctoral Scientific Research Foundation of Anhui Normal University, China（No.2016XJJ110）.
文摘A convenient and efficient method was developed for the synthesis of 2,2＇-（arylmethylene）bis（3-hydrox- ycyclohex-2-enone） derivatives via the oleylamine-catalyzed tandem Knoevenagel/Michael addition reactions of aromatic aldehydes and cyclohexane-1,3-diones. This transformation proceeded without any metal catalyst in non-toxic solvent at room temperature with high isolated yields. A plausible mechanism for this process was pro- posed.
