Catalytic amination of 5-iodouracil derivatives
Catalytic amination of 5-iodouracil derivatives
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DOI：
10.1016/s0040-4039(00)02315-7
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发表时间：
2001-02-19
影响因子：
1.8
通讯作者：
Gonzalez, AM
中科院分区：
文献类型：
--
作者：
Arterburn, JB;Pannala, M;Gonzalez, AM
用（CuOTf）（2）催化1，3-二苄基-5-碘尿嘧啶的胺化反应制备了杂环5-氨基尿嘧啶衍生物。PhH，1，10-菲咯啉，二亚苄基丙酮，和Cs2 CO 3作为碱，在二甲苯中，95 ℃。使用铜催化剂时，咪唑和2-氨基噻唑啉存在问题，但使用Ni（COD）（2）、dppf和（NaOBu）-O-t在甲苯中在100摄氏度下有效偶联。这些是用尿嘧啶底物催化胺化的第一个例子。(C)2001爱思唯尔科技有限公司版权所有。
Heterocyclic 5-amino uracil derivatives were prepared by catalytic amination of 1,3-dibenzyl-5-iodouracil using (CuOTf)(2). PhH, 1,10-phenanthroline, dibenzylidene acetone, and Cs2CO3 as base in xylenes at 95 degreesC. Imidazole and 2-amino thiazoline were problematic using the Cu catalyst, but were effectively coupled using Ni(COD)(2), dppf, and (NaOBu)-O-t in toluene at 100 degreesC. These are the first examples of catalytic amination with a uracil substrate. (C) 2001 Elsevier Science Ltd. All rights reserved.