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PREPARATION OF TAXOL AND DOCETAXEL THROUGH PRIMARY AMINES

机译:通过主胺制备他克索和十六烷

摘要

The invention relates to a process for converting Taxol A, B and C to Taxol primary amine which can then be easily and efficiently converted to Taxol A or docetaxel, thereby significantly increasing the yield of these products from biomass. The method includes the removal of the amide from the side-chain with Schwartz's reagent to form an imine, followed by the hydrolysis of the imine to the primary amine. The primary amine can then be converted to Taxol A or docetaxel. New Taxol imine compounds and primary amine salts have been formed by this process.
机译:本发明涉及将紫杉醇A,B和C转化为紫杉醇伯胺的方法,然后可以容易且有效地将其转化为紫杉醇A或多西他赛,从而显着提高这些产物从生物质中的产率。该方法包括用Schwartz试剂从侧链上除去酰胺以形成亚胺,然后将亚胺水解为伯胺。然后可以将伯胺转化为紫杉醇A或多西他赛。通过这种方法已经形成了新的紫杉醇亚胺化合物和伯胺盐。

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