参考标题:Studies Of Antitumor-Active 5-Fluorouracil Derivatives. I. Synthesis Of N-Phthalidyl 5-Fluorouracil Derivatives. 作者:Susumu Kamata,Nobuhiro Haga,Takeaki Matsui,Wataru Nagata 摘要:Several 5-Fluorouracil Derivatives In Which The Phthalidyl (1, 3-Dihydro-3-Oxoisobenzofuran-1-Yl) Group, Appropriately Substituted On Its Benzene Ring, Is Substituted At The N (1)-Or N (3)-Position Or At Both Positions Were Synthesized, And Their Antitumor Activities Were Evaluated. Among These Compounds, 1-(1, 3-Dihydro-3-Oxoisobenzofuran-1-Yl)-5-Fluorouracil (3A, 590-S) Was Shown To Be Markedly Active Against Several Experimental Tumor Systems. Several Methods For A Simple And Efficient Large-Scale Preparation Of 3A Were Examined. The Large-Scale Preparation Of 3A Was Effected Most Efficiently By The Condensation Of 5-Fluorouracil With The Quaternary Ammonium Salt Of 3-Bromophthalide In The Presence Of A Base. The Synthesis Of (+)- And (-)-3A Is Also Described.