One-pot cyclization of 2-aminophenethyl alcohols: a novel and direct approach to the synthesis of N-acyl indolines.

One-pot cyclization of 2-aminophenethyl alcohols: a novel and direct approach to the synthesis of N-acyl indolines.
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DOI:
10.1021/jo701566v
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发表时间:
2007-11
期刊:
The Journal of organic chemistry
影响因子:
--
通讯作者:
Zengxue Wang;W. Wan;Haizhen Jiang;J. Hao
Zengxue Wang;W. Wan;Haizhen Jiang;J. Hao
中科院分区:
其他
文献类型:
--
作者:
Zengxue Wang;W. Wan;Haizhen Jiang;J. Hao

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在PPh 3、CCl 4和NEt 3存在下,2-氨基苯乙醇与羧酸的独特的一锅环化反应以良好至优异的产率提供了N-酰基吲哚啉的形成。这种新的方法提供了一种有效的,可扩展的,低成本的,直接获得生物学上重要的吲哚啉,其进一步氧化为吲哚和羟吲哚。
A unique one-pot cyclization of 2-aminophenethyl alcohols with carboxylic acids in the presence of PPh3, CCl4, and NEt3 furnished the formation of N-acyl indolines in good to excellent yields. This new approach provides an efficient, scalable, low-cost, and direct access to the biologically important indolines which are further oxidizable to indoles and oxindoles.