摘要
5-氟尿嘧啶N^1-甲酰氯分别与Gly、Val、Leu、Ile、Phe、Asp和Glu的苄酯反应,制备了7种5-氟尿嘧啶-N^1-甲酰基氨基酸苄酯。氢解后得到了相应的5-氟尿嘧啶N^1-甲酰氨基酸。将其进一步与氨基酸甲酯或二肽甲酯缩合,制备了5-氟尿嘧啶N^1-甲酰基二肽甲酯和三肽甲酯。5-氟尿嘧啶-N^1-甲酰基二肽甲酯也可采用5-氟尿嘧啶-N^1-甲酰氯与二肽甲酯直接反应制备。
Seven 5-fluorouracil-N'-carbonyl amino acid benzyl esters(1a-g) were respectively prepared by the reaction of 5-fluorouracil-N'-carbonyl chloride with benzyl esters of glycine, valine, leucine, phenylalanine and bisbenzyl esters of aspartic and glutamic acids. These esters were then hydrogenated to obtain the corresponding 5-fluorouracil-N'-carbonyl aminoacids (2a-c). 2C and 2e were further coupled with aminoacid methyl esters or dipeptide methyl esters by DCC-mediated coupling reaction to afford 5-fluorouracil-N'-carbonyl dipeptide or tripeptide methyl esters (3a-d, 4a,b). 5-Fluorouracii-N1-Carbonyl dipeptide methyl esters (5n-d) were also obtained directly by the reaction of 5-fluorouracil-N'-carbonyl chloride with dipeptide methyl esters. The antitumor activity of some of the above compounds was tested against EAC or S180 in mice.
出处
《高等学校化学学报》
SCIE
EI
CAS
CSCD
北大核心
1991年第4期555-559,共5页
Chemical Journal of Chinese Universities
关键词
氨基酸
5-氟脲嘧啶
短肽
抗肿瘤性
Aminoacid, Oligopeptide, 5-Fluorouracil, Antitumor activity
