21770-49-0Relevant academic research and scientific papers
Preparation method of 1,4-dioxane compounds
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Paragraph 0034-0038, (2021/07/24)
The invention provides a preparation method of 1,4-dioxane compounds, belonging to the technical field of synthesis of organic medicines. The preparation method comprises the following steps: a compound A is used as a starting raw material and is subjected to two-step chemical reaction to obtain a compound C; and the compound C, catechol and other raw materials are subjected to a cyclization reaction to construct a series of the 1,4-dioxane compounds which are novel single compounds. According to the invention, the 1,4-dioxane compounds are obtained through separation and purification of a total synthesis method for the first time, and the preparation method has the advantages of being clear in component, high in purity and the like, and has important significance in research of preparation of novel drugs through subsequent structural modification and transformation of the 1,4-dioxane compounds.
Synthesis and biological evaluation of a series of benzoxazole/ benzothiazole-containing 2,3-dihydrobenzo[b][1,4]dioxine derivatives as potential antidepressants
Wang, Songlin,Chen, Yin,Zhao, Song,Xu, Xiangqing,Liu, Xin,Liu, Bi-Feng,Zhang, Guisen
supporting information, p. 1766 - 1770 (2014/04/17)
A series of benzoxazole/benzothiazole-2,3-dihydrobenzo[b][1,4]dioxine derivatives (5a-5d and 8a-8j) was synthesized. Compounds were evaluated for binding affinities at the 5-HT1A and 5-HT2A receptors. Antidepressant activities of the compounds were screened using the forced swimming test (FST) and the tail suspension test (TST). The results indicated that the compounds exhibited high affinities for the 5-HT1A and 5-HT2A receptors and showed a marked antidepressant-like activity. Compound 8g exhibited high affinities for the 5-HT1A (Ki = 17 nM) and 5-HT2A (Ki = 0.71 nM) receptors; it also produced a decrease of the immobility time and exhibited potent antidepressant-like effects in the FST and TST in mice.
