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| 特比萘芬的合成 | |
| 引用本文： | 特比萘芬的合成[J]. 中国药科大学学报, 2001, (1): 10-11. |
| 作者姓名： | 田丽娟 韩英 孟正木 夏超 张久红 |
| 作者单位： | 1. 中国药科大学天然药物化学教研室， 南京 210038 2. 江苏省药物研究所， 南京 210009 3. 南京中医药大学， 南京 210002 |
| 基金项目： | 江苏省自然科学基金资助项目(BK97115) |
| 摘 要： | 目的：研究抗真菌药特比萘芬的合成路线及工艺。方法：以频哪酮为起始原料，经氯代，脱所化氢，格氏反应得6，6－二甲基－1－庚烯－4－炔－3－醇（5），溴代后与N－甲基－1－萘甲胺反应得标题化合物。结果：合成了目标化合物，其结构经IR，^1HNMR,MS，元素分析得以确正。结论：合成路线及工艺较适用于工业化生产。 |
| 关 键 词： | 角鲨烯环氧化酶抑制剂 特比萘芬 格氏反应 合成 抗真菌药 |
| 文章编号： | 1000-5048(2001)01-0010-03 |
| 修稿时间： | 2000-10-12 |
Synthesis of Terbinafine |
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| Synthesis of Terbinafine[J]. Journal of China Pharmaceutical University, 2001, (1): 10-11. | |
| Authors: | TIAN Li Juan HAN Ying MENG Zheng Mu XIA Chao ZHANG Jiu Hong |
| Affiliation: | TIAN Li Juan,HAN Ying 1,MENG Zheng Mu,XIA Chao 1,ZHANG Jiu Hong 2 Department of Phytochemistry,China Pharmaceutical University,Nanjing 210038, 1Jingsu Institute of Materia Medica,Nanjing 210009, 2Nanjing University of Traditiona |
| Abstract: | AIM:Bio-active constituents were expected to be obtained fromAnnona glabra Linn. METHODS: It is extracted with 95% alcohol, distributed by different solvents, isolated via column chromatography on silica gel and purified by crystallization et al. RESULTS: Six compounds were isolated from Annona glabra Linn. Among them, five compounds were kaurane diterpenoids and one compound was alkaloid. On the basis of the preperties and spectral analysis, their structures were identified as terpeneⅠ(-)-kaur-16-en-19-oic acid、terpeneⅡ16α-hydro-19-acetoxy-ent-kauran-17-oic acid、terpeneⅢ(-)-kauran-19-al-17-oic acid、terpene Ⅳent-19-carbomethoxykauran-17-oic acid、terpeneⅤ 19-hydroxy-16α-(-)-kauran-17-oic acid and alkaloid oxoglaucine. CONCLUSION: Among them, ent-19-carbomethoxykauran-17-oic acid、19-hydroxy-16α-(-)-kauran-17-oic acid and oxoglaucine were isolated from this plant for the first time. |
| Keywords: | Annona glabra% kaurane diterpenoid alkaloid chemical constituent |
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