Gossett L S, Habeck L L, Shackelford K A, Mendelsohn L G, Gates S B, Worzalla J F, Self T D, Theobald K S, Andis S L, Schultz R M, Shih C
Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, IN 46285, USA.
Bioorg Med Chem Lett. 1999 Jan 4;9(1):75-8. doi: 10.1016/s0960-894x(98)00683-0.
A new series of 2,4-diaminopyrido[2,3-d]pyrimidine based antifolates 1-3 were synthesized through an efficient conversion of 2-pivaloyl-4-oxo-6-ethynylpyrido[2,3-d]pyrimidine 5 to the corresponding 4-amino analog 7 via the activated 1,2,4-triazole intermediate 6. Compound 7 was used as the key intermediate for the preparation of the final products. The detailed biological evaluation of these compounds both as antineoplastic and antiarthritic agents will be discussed.
通过将2-新戊酰基-4-氧代-6-乙炔基吡啶并[2,3-d]嘧啶5经由活化的1,2,4-三唑中间体6高效转化为相应的4-氨基类似物7，合成了一系列基于2,4-二氨基吡啶并[2,3-d]嘧啶的新型抗叶酸剂1-3。化合物7用作制备最终产物的关键中间体。将讨论这些化合物作为抗肿瘤和抗关节炎药物的详细生物学评价。
