论文部分内容阅读
通过W ong叠氮转化和亲核取代反应,分别合成了叠氮苯丙氨酸、叠氮丙氨酸、苄基叠氮,采用上述叠氮化物与L-炔丙基甘氨酸进行C lick反应,合成了3个1,4-取代1,2,3-三唑氨基酸衍生物:2-氨基-3-[1-(1-羧基-2-苯乙基)-1H-1,2,3-三唑-4-基]丙酸、3,3-′(1H-1,2,3-三唑-1,4-基)双(2-氨基丙酸)和2-氨基-3-(1H-1,2,3-三唑-1-苄基-4-基)丙酸,收率分别是76%、62%和68%,产物结构经核磁共振波谱、质谱、红外光谱进行了表征。1,2,3-三唑氨基酸衍生物含双功能螯合基团,是很有潜力的fac-[188Re(CO)3(H2O)3]+放射性标记配体。
Azidophenylalanine, azidoalanine and benzyl azide were synthesized by the W ong azide conversion and nucleophilic substitution reactions, respectively. C lick reaction with L-propargylglycine was carried out using the above azide and the synthesis Three 1,4-substituted 1,2,3-triazole amino acid derivatives were obtained: 2-amino-3- [1- (1-carboxy-2-phenylethyl) -1H-1,2,3-tris (2-aminopropionic acid) and 2-amino-3- (1 H-1,2,3-triazole- 1,2,3-triazol-1-benzyl-4-yl) propanoic acid was obtained in 76% yield, 62% yield and 68% yield. The product was characterized by 1H NMR, MS and IR spectra. 1,2,3-triazole amino acid derivatives with bifunctional chelating groups are potential fac- [188Re (CO) 3 (H2O) 3] + radiolabeled ligands.