【作者】 邵宜；

【导师】 吕秀阳；

【作者基本信息】 浙江大学 ， 制药工程， 2011， 硕士

【摘要】 长春花(Catharanthus roseus (L.) G. Don)是夹竹桃科长春花属一种重要的药用植物。长春花中含有很多有价值的吲哚类生物碱,其中长春碱(Vinblastine, VLB)、长春新碱(Vincristine, VCR)是临床广泛应用的抗肿瘤药物,长春质碱(Catharanthine, CTR)和文多林(Vindoline, VDL)是长春碱类药物半合成的重要原料。本文以提高长春花资源利用率为目的,开展了长春碱类生物碱的提取,分离和半合成研究,建立了长春花综合利用的一个新模式。1、建立了一个适合工业生产的长春花提取方法,在提取同时得到长春碱,长春质碱和文多林。较佳提取提取工艺为四倍80%乙醇提取,提取三次。2、通过pH梯度萃取将长春总碱分为双吲哚碱和单吲哚碱两部分,并通过层析分离纯化得到长春碱,长春质碱和文多林。3、通过重铬酸与长春碱反应一步生成长春新碱,并通过层析分离得到99%长春新碱。4、通过长春质碱和文多林耦合生成脱水长春碱,并通过溴化、缩环反应得到长春瑞滨,再通过一系列层析分离得到99%的长春瑞滨。更多还原

【Abstract】 Catharanthus roseus (L.) G. Don is one of the important medicinal plants of Catharanthus in Apocynaceae.Many important indole alkaloids were found in Catha-ranthus roseus,in which Vinblastine(VLB) and Vincristine(VCR) were widely used for anti-cancers in clinic,and Catharanthine(CTR) and Vindoline(VDL) were important materials for semi-synthesis of Catharanthus alkaloids.In this article,In order to im-provethe utilization of Catharanthus roseus’s.the process of extraction,isolation and semi-synthesis of VLB were studied,and a mode for comprehensive utilization of Ca-tharanthus roseus was established.1. Establish a extraction method for Catharanthus roseus in industry,to obtain VLB Catharanthine(CTR) and Vindoline(VDL).The extraction method use four times 80% ethanol-water(v/v) and extraction three times.2. Vinblastine were separated into mono-indole alkaloids and dimeric-indole al-kaloids by pH gradient extraction method, and VLB Catharanthine(CTR) and Vindo-line(VDL) were obtained by chromatography method.3. Synthesize Dichromic acid with VLB to obtain Vincristine(VCR) by one-step reaction, and the 99% purity of Vincristine(VCR) was obtained by chromatography method..4. Couple Catharanthine(CTR) with Vindoline(VDL)’s to obtain Anhydrovinblas-tine(AVLB), then go through bromination and Ring-Closure Reaction-, further go through chromatography separation, then 99% purity of Vinorelbine(VNR) was ob-tained.更多还原