The Direct Asymmetric Alkylation of α-Amino Aldehydes with 3-Indolylmethanols by Enamine Catalysis
The Direct Asymmetric Alkylation of α-Amino Aldehydes with 3-Indolylmethanols by Enamine Catalysis
复制标题
烯胺催化α-氨基醛与3-吲哚甲醇的直接不对称烷基化
DOI：
10.1021/ol503318c
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发表时间：
2014-12-19
期刊：
影响因子：
5.2
通讯作者：
Guo, Qi-Xiang
中科院分区：
文献类型：
--
作者：
Guo, Zhi-Lei;Xue, Jia-Hui;Guo, Qi-Xiang
本工作描述了α-氨基醛与3-吲哚基甲醇的高效α-烷基化反应。在催化剂3f的促进下，目标产物的产率高达99%，非对映选择性高达88：12，对映选择性高达96% ee。直接烷基化产物可以容易地转化为其它色氨酸衍生物而不损失立体选择性。
This work describes an efficient alpha-alkylation reaction of a-amino aldehydes with 3-indolylmethanols. In the promotion of catalyst 3f, the target products were obtained in high yields (up to 99%), good diastereoselectivities (up to 88:12), and excellent enantioselectivities (up to 96% ee). The direct alkylation products can be readily converted into other tryptophan derivatives without the loss of stereoselectivities.