10-去乙酰基-7-表紫杉醇转化为紫杉醇的研究(英文)An efficient conversion method of 10-deacetyl-7-epi-taxol into taxol
匡云艳,须媚,陈芬儿
摘要(Abstract):
目的将天然紫杉烷类物质10 -去乙酰基- 7 -表紫杉醇高效地转化为抗癌药物紫杉醇。方法首先将10 -去乙酰基 7 -表紫杉醇中的2′OH选择性保护、7 -OH乙酰化、去保护3步一锅反应获得7- 表紫杉醇,再在DBU的催化下差向异构化为紫杉醇。结果本方法以10 -去乙酰基 7 -表紫杉醇为起始原料,以4 0 %的总收率制备得到紫杉醇。结论建立了一条将天然紫杉烷类物质以较高的化学选择性以及良好的收率转化为紫杉醇的途径。
关键词(KeyWords): 药物化学;化学合成;紫杉醇;10-去乙酰基-7-表紫杉醇;7-表紫杉醇
基金项目(Foundation):
作者(Author): 匡云艳,须媚,陈芬儿
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