Syntheses and biological activities of dihydro-5,6-dehydrokawain derivatives.
Syntheses and biological activities of dihydro-5,6-dehydrokawain derivatives.
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二氢-5,6-脱氢川椒素衍生物的合成及其生物活性。
DOI：
10.1271/bbb.60.1643
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发表时间：
1996
期刊：
影响因子：
--
通讯作者：
S. Toyama
中科院分区：
文献类型：
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作者：
S. Tawata;S. Taira;N. Kobamoto;M. Ishihara;S. Toyama
研究了二氢-5,6-脱氢kawain衍生物的合成及其对植物病原真菌和白蚁的生物活性。采用不经层析的简单方法从Alpinia speciosa K. SCHUM叶片中分离出二氢-5,6-脱氢kawain。所得白色结晶化合物经仪器分析鉴定为二氢-5,6-脱氢氢化氢(1)。以二氢-5,6-脱氢钾为水解原料，制备了4-羟基-6-（2-苯乙基）- 2h -吡喃-2-酮(3)。通过与磷剂反应，合成了3个二氢-5,6-脱氢kawain衍生物。在所合成的化合物中，二甲基[6-（2-苯乙基）-2-氧- 2h -吡喃-4-基]硫代酸酯(4)在100 ppm下对罗氏皮质菌的抑菌活性最强，达91%。
The syntheses and biological activities of dihydro-5,6-dehydrokawain derivatives against plant pathogenic fungi and termites were investigated. Dihydro-5,6-dehydrokawain was isolated by a simple method without chromatography from the leaves of Alpinia speciosa K. SCHUM. The white crystalline compound obtained was identified as dihydro-5,6-dehydrokawain (1) by instrumental analyses. 4-Hydroxy-6-(2-phenylethyl)-2H-pyran-2-one (3) was prepared by hydrolyzing dihydro-5,6-dehydrokawain. Three dihydro-5,6-dehydrokawain derivatives were synthesized by reacting 3 with phosphoric agents. Among the synthesized compounds, dimethyl [6-(2-phenylethyl)-2-oxo-2H-pyran-4-yl]phosphorothionate (4) had the strongest antifungal activity of 91% at 100 ppm against Corticium rolfsii.