[1]胡书瑜,户晓兢,孙倩倩,等.药物中间体苯并呋喃酮与乙醛分子间羟醛缩合反应的研究[J].新乡医学院学报,2020,37(2):116-119.[doi:10.7683/xxyxyxb.2020.02.004]
　HU Shuyu,HU Xiaojing,SUN Qianqian,et al.Study on the intermolecular aldol reaction of pharmaceutical intermediate benzofuranone and aldehyde[J].Journal of Xinxiang Medical University,2020,37(2):116-119.[doi:10.7683/xxyxyxb.2020.02.004]
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药物中间体苯并呋喃酮与乙醛分子间羟醛缩合反应的研究
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《新乡医学院学报》[ISSN:1004-7239/CN:41-1186/R]

卷:
37
期数:
2020年2
页码:
116-119
栏目:
基础研究
出版日期:
2020-02-05

文章信息/Info

Title:
Study on the intermolecular aldol reaction of pharmaceutical intermediate benzofuranone and aldehyde
作者:
胡书瑜1; 户晓兢2; 孙倩倩1; 朱润青1; 赵芳菲1; 房立真1
（1.新乡医学院药学院，河南　新乡　453003；2.新乡医学院第三附属医院药剂科，河南 　新乡　453003)
Author(s):
HU Shuyu1; HU Xiaojing2; SUN Qianqian1; ZHU Runqing1; ZHAO Fangfei1; FANG Lizhen1
(1.School of Pharmacy,Xinxiang Medical University,Xinxiang 453003,Henan Province,China;2.Department of Pharmacy，The Third Affiliated Hospital of Xinxiang Medical University,Xinxiang 453003,Henan Province,China)
关键词:
羟醛缩合; 苯并呋喃酮; 单取代产物; 二取代产物; 脱水产物
Keywords:
aldol reaction; benzofuranone; monosubstituted product; disubstituted product; dehydrated product
分类号:
R914
DOI:
10.7683/xxyxyxb.2020.02.004
文献标志码:
A
摘要:
目的　探索不同条件下苯并呋喃酮与乙醛羟醛缩合反应的主要产物。方法　以不同位置带乙酰基的苯并呋喃酮为底物，使用常见的碱性盐作催化剂与乙醛发生分子间羟醛缩合反应，分别得到不同产率的单取代产物、二取代产物和脱水产物。结果　制备出6种羟醛缩合反应产物，使用CH3COONa催化在常温下反应12 h，可得到最大收率的单取代产物；使用Na2CO3催化在常温下反应4 h，可得到最大收率的二取代产物；使用p-TsOH催化在常温下反应12 h，可得到最大收率的脱水产物。结论　苯并呋喃酮与醛的羟醛缩合反应会产生单取代产物、二取代产物和脱水产物，分别使用不同的催化剂CH3COONa、Na2CO3和p-TsOH可形成相应的主要产物。
Abstract:
Objective　To explore the main products of the aldol reaction of benzofuranone and aldehyde under different conditions.Methods　The benzofuranones bearing acetyl groups at different positions were used as substrate,and some common basic salts were used as catalyzator to carry out intermolecular aldol reaction with aldehyde to obtain the monosubstituted products,disubstituted products and the dehydration products with different yields.Results　Six products of aldol reaction were prepared.The maximum yield of monosubstituted product can be obtained when the reaction was catalyzed with CH3COONa at room temperature for 12 hours.The maximum yield of disubstituted product can be obtained when the reaction was catalyzed with Na2CO3 at room temperature for 4 hours.The maximum yield of the dehydrated product can be obtained when the reaction was catalyzed with p-TsOH at room temperature for 12 hours.Conclusions　The aldol reaction of benzofuranone with aldehyde can provided the monosubstituted product,disubstituted product and the dehydrated product,and each of them can be formed as the predominant product when using the catalyst of CH3COONa,Na2CO3 and p-TsOH,respectively.

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更新日期/Last Update: 2020-02-05