Amino acid benzyl ester p-toluenesulfonic acids were synthesized under microwave irradiation condition by reaction of four amino acids with benzyl alcohol and p-toluenesulfonic acid,and then reacted with the N-phthalo...Amino acid benzyl ester p-toluenesulfonic acids were synthesized under microwave irradiation condition by reaction of four amino acids with benzyl alcohol and p-toluenesulfonic acid,and then reacted with the N-phthaloyl-L-glutamic anhydride to yield compound 3a-d,hydrogenised and treated with NH3(g) to obtain the target compounds—thalidomide ammonium salt derivatives.The microwave-assisted method was used to synthesis the thalidomide amino acid benzyl ester p-tolunensulfonic acid,the reaction time was brought down with improved yield as compared with conventional heating method.The structures were comfirmed by MS,1H-NMR and elemental analysis.展开更多
Thalidomide and its derivatives have great potentials in immune therapy. This research note presented that heating the mixture of phthalic anhydride or its chloro or nitro substituted derivatives and L-glutamine in va...Thalidomide and its derivatives have great potentials in immune therapy. This research note presented that heating the mixture of phthalic anhydride or its chloro or nitro substituted derivatives and L-glutamine in vacuum afforded thalidomide 1 and its corresponding derivatives 2—5 directly in yields 24%47%. Among them, compound 4 is the material in the synthesis of 3-amino and 3-amino-3′-fluoro substituted thalidomide. Compared with traditional methods, this method is more direct and convenient.展开更多
目的建立用于筛选具有抗肿瘤活性的沙利度胺衍生物的分子平台。方法从人胎肝c DNA文库中分别扩增cereblon(CRBN)和Ikaros家族锌指蛋白1(Ikaros family zinc finger protein 1,IKZF1)c DNA,并将其克隆入p XJ40-myc和pc DNA3-FLAG载体中,...目的建立用于筛选具有抗肿瘤活性的沙利度胺衍生物的分子平台。方法从人胎肝c DNA文库中分别扩增cereblon(CRBN)和Ikaros家族锌指蛋白1(Ikaros family zinc finger protein 1,IKZF1)c DNA,并将其克隆入p XJ40-myc和pc DNA3-FLAG载体中,将其转染293T细胞,通过检测沙利度胺及其衍生物对CRBN和IKZF1蛋白相互作用的改变,间接反映其在肿瘤抑制中的作用。结果 CRBN和IKZF1在293T细胞中均得到表达,沙利度胺及其两个衍生物可显著增强CRBN和IKZF1的结合。结论成功建立了用于筛选具有抗肿瘤活性的沙利度胺衍生物分子平台,初步发现2个沙利度胺衍生物可显著增强CRBN和IKZF1的结合,提示其具有潜在的抗癌活性。展开更多
文摘Amino acid benzyl ester p-toluenesulfonic acids were synthesized under microwave irradiation condition by reaction of four amino acids with benzyl alcohol and p-toluenesulfonic acid,and then reacted with the N-phthaloyl-L-glutamic anhydride to yield compound 3a-d,hydrogenised and treated with NH3(g) to obtain the target compounds—thalidomide ammonium salt derivatives.The microwave-assisted method was used to synthesis the thalidomide amino acid benzyl ester p-tolunensulfonic acid,the reaction time was brought down with improved yield as compared with conventional heating method.The structures were comfirmed by MS,1H-NMR and elemental analysis.
文摘Thalidomide and its derivatives have great potentials in immune therapy. This research note presented that heating the mixture of phthalic anhydride or its chloro or nitro substituted derivatives and L-glutamine in vacuum afforded thalidomide 1 and its corresponding derivatives 2—5 directly in yields 24%47%. Among them, compound 4 is the material in the synthesis of 3-amino and 3-amino-3′-fluoro substituted thalidomide. Compared with traditional methods, this method is more direct and convenient.
