Synthesis of (+/-)-4'-ethynyl and 4'-cyano carbocyclic analogues of stavudine (d4T).
Synthesis of (+/-)-4'-ethynyl and 4'-cyano carbocyclic analogues of stavudine (d4T).
复制标题
司他夫定 (d4T) 的 (l-)-4-乙炔基和 4-氰基碳环类似物的合成。
DOI：
10.1081/ncn-51900
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发表时间：
2005
期刊：
影响因子：
--
通讯作者：
Kato,Keisuke
中科院分区：
文献类型：
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作者：
Kumamoto,Hiroki;Haraguchi,Kazuhiro;Tanaka,Hiromichi;Nitanda,Takao;Baba,Masanori;Dutschman,GingerE;Cheng,Yung-Chi;Kato,Keisuke
报道了抗HIV药物司他夫定（5，d4 T）的（±）-4′-乙炔基（8）和4′-氰基（9）碳环类似物的合成。碳环单元（16）由容易获得的β-酮酯10构成。在16位上引入胸腺嘧啶碱基后，通过对酯基的修饰，使8位和9位分别得到乙炔基或氰基。对8和9的抗HIV活性进行了评价。
The synthesis of (±)-4′-ethynyl (8) and 4′-cyano (9) carbocyclic analogues of the anti-HIV agent stavudine (5, d4T) is reported. The carbocyclic unit (16) was constructed from readily available β-keto ester10. The ethynyl or cyano group of8and9were prepared, after the introduction of thymine base to16, by manipulation of the ester function. Evaluation of the anti-HIV activity of8and9was also carried out.