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.
出处
《解放军药学学报》
CAS
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
