| 正交实验设计优化光敏剂紫红素-18的合成工艺 |
| 投稿时间：2010-06-17 修订日期：2010-11-01 点此下载全文 |
| 引用本文：王曜,姚建忠,缪震元,盛春泉,张万年.正交实验设计优化光敏剂紫红素-18的合成工艺[J].药学实践杂志,2011,29(2):114~116 |
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| 基金项目:国家自然科学基金(30371737)和上海市重点学科建设基金(B906)资助项目. |
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| 中文摘要:目的 优化光敏剂紫红素-18 (1)的合成工艺。 方法 以脱镁叶绿酸a(2)为原料,经空气氧化及碱开环制得化合物1;选择影响其合成产率的反应时间(A)、氢氧化钾溶液浓度(B)、反应溶剂(C)和化合物2与氢氧化钾的质量投料比(D)为考察因素,每个因素各取三个水平,采用L9(34)正交试验法优化目标物1的最佳合成工艺。 结果 合成目标物1的最优反应条件为B1C2A2D2,反应工艺收率从34.4%提高到45.6%。 结论 新工艺提高了收率、缩短了反应时间、消除了毒性溶剂,适合工业化生产。 |
| 中文关键词:药物化学 工艺改进 紫红素-18 正交设计 光敏剂 |
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| Optimization of the synthesis of photosensitizer purpurin-18 by orthogonal design |
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| Abstract:Objective To optimize the synthesis of photosensitizer purpurin-18(1). Methods Target compound 1 was synthesized through air oxidation and simultaneously ring cleavage of pheophorbide a (2) in presence of alkali. Four main factors influencing synthetic yield of 1 such as reaction time (A), concentration of potassium hydroxide (B), solvent (C) and weight ratio of material 2 to potassium hydroxide (D),which was chosed three levels respectively,were evaluated by the orthogonal experimental design of L9 (34). Results The optimization term of the synthesis of target compound 1 was B1C2A2D2. The yield of 1 was raised from 34.4% to 45.6%. Conclusion The yield was raised. The reaction time was shortened and the toxic solvent was removed. The procedure was suitable for industrial production. |
| keywords:medicinal chemistry process improvement purpurin-18 orthogonal design photosensitizer |
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