Yu Yongping, Ostresh John M, Houghten Richard A
Torrey Pines Institute for Molecular Studies, 3550 General Atomics Court, San Diego, California 92121, USA.
J Comb Chem. 2004 Jan-Feb;6(1):83-5. doi: 10.1021/cc030017o.
A traceless approach for the solid-phase synthesis of 6-amino-1,3,5-triazine-2,4-diones is described. Reaction of resin-bound S-methylisothiourea with isocyanates yielded resin-bound iminoureas 3, which reacted with amines to afford the corresponding guanidines 4. Following intramolecular cyclizative cleavage of the resin-bound guanidines using potassium ethoxide as a base, the desired products 5 were obtained in good yields and high purities.
描述了一种用于6-氨基-1,3,5-三嗪-2,4-二酮固相合成的无痕方法。树脂结合的S-甲基异硫脲与异氰酸酯反应生成树脂结合的亚氨基脲3，其与胺反应得到相应的胍4。使用乙醇钾作为碱对树脂结合的胍进行分子内环化裂解后，以良好的产率和高纯度获得了所需产物5。
