氨甲喋呤-α-苯丙氨酸的固相合成  

The Solid-Phase Synthesis of Methotrexate-α-Phe

作　　者：陈雷[1] 孙晓莉[2] 郝晓柯[3] 岳乔红[3] 

机构地区：[1]西北大学陕西省生物医药重点实验室,陕西西安710069 [2]中国人民解放军第四军医大学药学系化学教研室,陕西西安710032 [3]中国人民解放军西京医院检验科,陕西西安710032

出　　处：《解放军药学学报》2006年第4期264-266,共3页Pharmaceutical Journal of Chinese People's Liberation Army

基　　金：863课题;No.2001AA215321;国家"十五"重大课题专项;No.2002AA2Z3109

摘　　要：目的合成氨甲喋呤-α-苯丙氨酸。方法用固相肽合成法合成谷-苯丙二肽,再与喋啶对氨基苯甲酸缩合,合成了氨甲喋呤-α-苯丙氨酸。结果总收率由64%提高到90%。结论产物经简单纯化达到HPLC单峰,质谱分析相对分子量符合理论值。本方法改变了缩合剂、活化剂和投料比,缩短了反应时间,降低了合成成本。Aim To synthesize Methotrexate-α-Phe （MTX-α-Phe）. Methods Glu （OtBu）-Phe-O-Wang Resin was prepared with the technique of solid-phase peptide synthesis and was then reacted with 4-amino-4-deoxy- 10- methylpteroic acid to produce MTX-α-Phe. Results The overall yield increased from 64% to 90%. Conclusion The product was verified as a single peak by HPLC and its molecular weight was measured by mass spectrometry without further purification. The synthetic cost and time of reaction were reduced significantly.

关 键 词：固相合成 氨甲喋呤-α-苯丙氨酸 氨甲喋呤 

分 类 号：R914.5[医药卫生—药物化学]