The stereoselective synthesis of oxazolidine derivatives was accomplished,starting from ephedrine,pseudo-ephedrine and substituted benzaldehyde.Seven kinds of new substituted phenyl-3,4-dimethyl-5 phenyloxazolidine we...The stereoselective synthesis of oxazolidine derivatives was accomplished,starting from ephedrine,pseudo-ephedrine and substituted benzaldehyde.Seven kinds of new substituted phenyl-3,4-dimethyl-5 phenyloxazolidine were first reported.At the same time,the stereochemical structures and the spectral characteristics were studied for these oxazolidines.展开更多
以吡啶甲酸和氨基醇为原料,1-乙基-3-(3-二甲基丙胺)碳二亚胺盐酸盐(EDCI)和1-羟基苯并三氮唑一水物(HOBt.H2O)为缩合剂,得到β-羟基酰胺,产率在95%以上;再用三氯氧磷处理,得到β-氯代酰胺,产率在69%以上;最后在超声-微波辅助条件下,用N...以吡啶甲酸和氨基醇为原料,1-乙基-3-(3-二甲基丙胺)碳二亚胺盐酸盐(EDCI)和1-羟基苯并三氮唑一水物(HOBt.H2O)为缩合剂,得到β-羟基酰胺,产率在95%以上;再用三氯氧磷处理,得到β-氯代酰胺,产率在69%以上;最后在超声-微波辅助条件下,用NaOH的甲醇溶液处理β-氯代酰胺10min,合成2-吡啶基噁唑啉化合物,产率在86%以上。目标化合物的结构经1 H NMR及13 C NMR高分辨质谱确认。考察β-氯代酰胺、氢氧化钠的物质的量比、水和甲醇用量、辐照时间、微波功率以及反应温度对合成2-吡啶基噁唑啉化合物的影响,当氯代酰胺为1.6mmol时,其较优结果分别为1∶40、10和25mL、10min、80W以及50℃。展开更多
文摘The stereoselective synthesis of oxazolidine derivatives was accomplished,starting from ephedrine,pseudo-ephedrine and substituted benzaldehyde.Seven kinds of new substituted phenyl-3,4-dimethyl-5 phenyloxazolidine were first reported.At the same time,the stereochemical structures and the spectral characteristics were studied for these oxazolidines.
文摘以吡啶甲酸和氨基醇为原料,1-乙基-3-(3-二甲基丙胺)碳二亚胺盐酸盐(EDCI)和1-羟基苯并三氮唑一水物(HOBt.H2O)为缩合剂,得到β-羟基酰胺,产率在95%以上;再用三氯氧磷处理,得到β-氯代酰胺,产率在69%以上;最后在超声-微波辅助条件下,用NaOH的甲醇溶液处理β-氯代酰胺10min,合成2-吡啶基噁唑啉化合物,产率在86%以上。目标化合物的结构经1 H NMR及13 C NMR高分辨质谱确认。考察β-氯代酰胺、氢氧化钠的物质的量比、水和甲醇用量、辐照时间、微波功率以及反应温度对合成2-吡啶基噁唑啉化合物的影响,当氯代酰胺为1.6mmol时,其较优结果分别为1∶40、10和25mL、10min、80W以及50℃。
