当前位置: X-MOL 学术J. Asian Nat. Prod. Res. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Synthesis of pogostone by one-step.
Journal of Asian Natural Products Research ( IF 1.3 ) Pub Date : 2016-05-31 , DOI: 10.1080/10286020.2016.1184253
Han-Bin Chen 1, 2 , Jiang-Tao Zhou 2, 3 , Yu-Hong Liu 2, 3 , Zhen-Biao Zhang 2, 3 , Ya-Xian Zhan 2, 3 , Zi-Ren Su 2, 3 , Hui-Fang Zeng 1, 2
Affiliation  

Pogostone, isolated from Pogostemon cablin, has many biological activities such as potential antibacterial, anticandida, and antifungal. Traditional extraction leads to low output of PO about 17.6 mg/kg from Herba Pogostemonis. The previous literature had reported a synthetic study and the yield had reached 4.48% with strictly controlled reaction conditions. The two methods above cannot meet the large demand of PO; we report a new synthesis method. 4-hydroxy-6-methyl-2-pyrone (1) was added in toluene, with the existence of acylation catalyst 4-dimethylaminopyridine (DMAP), 4-methylvaleric acid (2), and condensing agent dicyclohexylcarbodiimide (DCC), PO was synthesized after the combination of 3-carbon of (1) with 1-OH of (2) in the acylation reaction. The purity had reached 98%, determined by HPLC. The structure was confirmed by spectroscopic methods including infrared, electron ionization mass spectrometry, and nuclear magnetic resonance spectroscopy. PO was totally synthesized in one step including cyclization, with total yield of 27.2%.



中文翻译:

一步法合成Pogostone。

Pogostone,与Pogostemon cablin隔离具有许多生物活性,例如潜在的抗菌,防霉和抗真菌作用。传统的提取方法会导致草药草的PO产量低,约为17.6 mg / kg。先前的文献报道了一项合成研究,在严格控制的反应条件下,收率达到4.48%。以上两种方法不能满足PO的大量需求。我们报告了一种新的合成方法。将4-羟基-6-甲基-2-吡喃酮(1)加入甲苯中,同时存在酰化催化剂4-二甲基氨基吡啶(DMAP),4-甲基戊酸(2)和缩合剂二环己基碳二亚胺(DCC),PO为(1)的3个碳原子与(2)的1 -OH酰基化反应后合成。通过HPLC测定纯度达到98%。通过分光光度法(包括红外,电子电离质谱和核磁共振波谱。PO包括环化在内的一步全过程合成,总收率为27.2%。

更新日期:2016-05-31
down
wechat
bug