5-FLUOROURACIL DERIVATIVES .21. A SYNTHESIS OF 5'-O-ACRYLOYL-5-FLUOROURIDINE BY USE OF PARA-METHOXYBENZYL GROUP AS AN N-3-IMIDE PROTECTING GROUP OF 5-FLUOROURIDINE
5-FLUOROURACIL DERIVATIVES .21. A SYNTHESIS OF 5'-O-ACRYLOYL-5-FLUOROURIDINE BY USE OF PARA-METHOXYBENZYL GROUP AS AN N-3-IMIDE PROTECTING GROUP OF 5-FLUOROURIDINE
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DOI：
10.1246/bcsj.64.2266
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发表时间：
1991-07-01
影响因子：
4
通讯作者：
OZAKI, S
中科院分区：
文献类型：
--
作者：
AKIYAMA, T;TAKESUE, Y;OZAKI, S
以对甲氧基苄基（PMB）作为5-氟尿苷的N3-酰亚胺保护基，合成了5 ′-O-丙烯酰基-5-氟尿苷。通过使用N，N-二异丙基乙胺或DBU作为碱，化学选择性地引入PMB基团。研究了一种在室温下用AlCl_3-苯甲醚体系脱保护的新方法。
5'-O-Acryloyl-5-fluorouridine was prepared by use of p-methoxybenzyl (PMB) group as an N3-imide protecting group of 5-fluorouridine. PMB group was introduced chemoselectively by use of N,N-diisopropylethylamine or DBU as a base. A new deprotection method was developed by means of AlCl3-anisole system at room temperature.