Li Hua, Yoo Jin Cheol, Hong Joon Hee
BK-21 Project Team, College of Pharmacy, Chosun University, Kwangju, Republic of Korea.
Nucleosides Nucleotides Nucleic Acids. 2008 Dec;27(12):1238-49. doi: 10.1080/15257770802458246.
The exomethylene of 6 was successfully constructed from the aldehyde 5 using Eschenmoser's reagents. A triene compound 7 was cyclized successfully using Grubbs' II catalyst to give an exomethylene carbocycle nucleus for the target compound. A Mitsunobu reaction was successfully used to condense the natural bases (adenine, thymine, uracil, and cytosine). The synthesized cytosine analogue 20 showed moderate anti-HIV activity (EC(50) = 10.67 microM).
6的亚甲基外双键成功地由醛5使用埃申莫瑟试剂构建而成。三烯化合物7使用格拉布催化剂II成功环化，得到目标化合物的亚甲基外双键碳环核。成功利用光延反应缩合天然碱基（腺嘌呤、胸腺嘧啶、尿嘧啶和胞嘧啶）。合成的胞嘧啶类似物20显示出中等的抗HIV活性（半数有效浓度EC(50) = 10.67微摩尔）。
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