| A Mild and Efficient Procedure for the Preparation of Chromone-2-carboxylates |
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| 引用本文： | Juan Hong YU Yu She YANG Ru Yun JI. A Mild and Efficient Procedure for the Preparation of Chromone-2-carboxylates[J]. 中国化学快报, 2006, 17(8): 1005-1008 |
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| 作者姓名： | Juan Hong YU Yu She YANG Ru Yun JI |
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| 作者单位： | Juan Hong YU，Yu She YANG，Ru Yun JI State Key Laboratory of Drug Research，Shanghai Institute of Materia Medica，Shanghai Institutes for Biological Sciences，the Chinese Academy of Sciences，Shanghai 201203 |
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| 摘 要： | Chromone-2-carboxylates are widely used for the pharmacological activity of several of its derivatives1. The general synthesis of such chromone derivates includes two steps (Scheme 1): a Claison condensation of dialkyl oxalate with 2-hydroxyacetophenones to achieve alkyl 3-(2-hydroxyphenyl)-3-oxopropanoates in the presence of NaH, NaOEt, or NaOMe; cyclodehydration of the alkyl 3-(2-hydroxyaryl)-3-oxopropanoates to obtain chromones under acid condition. The total yield of the two steps is q…
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| 关 键 词： | 苯并-γ-吡喃酮-2-羧酸酯 制备 茶-丁基乙烷基草酸酯 二乙基草酸酯 |
| 收稿时间： | 2006-02-13 |
A Mild and Efficient Procedure for the Preparation of Chromone-2-carboxylates |
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| Juan Hong YU,Yu She YANG,Ru Yun JI. A Mild and Efficient Procedure for the Preparation of Chromone-2-carboxylates[J]. Chinese Chemical Letters, 2006, 17(8): 1005-1008 |
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| Authors: | Juan Hong YU Yu She YANG Ru Yun JI |
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| Abstract: | A mild and efficient procedure to build up various chromone-2-carboxylates was developed. Condensation of diverse 2-hydroxyacetophones with tetr-butyl oxalate in the presence of sodium ethoxide could be accomplished rapidly under mild condition. Cyclo- dehydration was carried out to achieve chromone-2-carboxylates in one-pot with impressive yield. Advantages over conventional methods with diethyl oxalate were observed in yield and reaction time. |
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| Keywords: | Chromone-2-carboxylates tert-butyl ethyl oxalate diethyl oxalate. |
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