Taxol and its analogue side chain synthesizing method
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A synthetic method and analogue technology, applied in the field of synthesis of paclitaxel and its analogue side chains, can solve the problems that threaten the long-term persistence and regional distribution of Taxus plants
Inactive Publication Date: 2005-12-21
成都科杰高新技术发展有限公司
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With the current extraction and separation methods, such a large supply will undoubtedly threaten the long-term persistence and regional distribution o
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Abstract
This invention has disclosed a kind of synthetic method to paclitaxol and side chain of its analogue. This invention using low-cost alpha- glycolic acid as raw material, the asymmetry addition reaction induced by chirality tertiary butyl sulfinamide as committed step, prepares paclitaxol and polyene paclitaxol side chain. The chemical product quotiety of key reaction is high, protecting group is easy to control and operate, synthesis process is short.
Description
technical field [0001] The invention relates to a method for synthesizing the side chains of paclitaxel and its analogs, in particular to a new method for synthesizing the side chains of paclitaxel and its analogs based on chiral tert-butyl sulfenamide niffervine. Background technique [0002] Paclitaxel, a diterpenoid compound with unique anticancer activity, was first extracted from the bark of Pacific yew (Taxus.brevifolia) by American chemists Wall and Wani in 1967. The drug entered Phase III clinical trials in 1990 and was approved by the US FDA at the end of 1992 for the treatment of ovarian and breast cancers that are ineffective against conventional chemotherapy. In 1995, my country Peking Union Medical College and Haikou Pharmaceutical Factory respectively obtained the approval number of Class II new drugs, becoming the second country in the world to produce paclitaxel and its injection. Due to its unique anticancer mechanism and broad-spectrum and efficient antica...
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