Synthesis of Indolizine Derivatives Utilizing [1,2]-Phospha-Brook Rearrangement/Cycloisomerization Sequence
Synthesis of Indolizine Derivatives Utilizing [1,2]-Phospha-Brook Rearrangement/Cycloisomerization Sequence
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DOI：
10.1246/cl.170377
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发表时间：
2017-05
影响因子：
1.6
通讯作者：
Azusa Kondoh;Kazumi Koda;Y. Kamata;M. Terada
中科院分区：
文献类型：
--
作者：
Azusa Kondoh;Kazumi Koda;Y. Kamata;M. Terada
在Bronsted碱催化下，利用[1,2]-磷酸-布鲁克重排法合成了吲哚嗪衍生物。该方法不使用过渡金属催化剂，通过[1,2]-磷酸-布鲁克重排和随后的环异构化反应，由2-炔基吡啶酮生成烯基吡啶。该方法可以以一锅方式进行，并直接提供具有可作为进一步操作手柄的磷酸盐部分的吲哚嘧啶衍生物。
A new synthesis of indolizine derivatives was developed by utilizing the [1,2]-phospha-Brook rearrangement under Bronsted base catalysis. The method involves the generation of allenylpyridine from alkynyl 2-pyridyl ketones through the [1,2]-phospha-Brook rearrangement and the following cycloisomerization without using transition-metal catalysts. The method can be performed in a one-pot fashion and directly provides indolizine derivatives having a phosphate moiety that can function as a handle for further manipulation.