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Synthetic technology transfer of Larotaxel

Synthetic technology transfer of Larotaxel
English name:Larotaxel
Chinese name:莱龙泰素
Chemical name:4,10-beta-diacetoxy-2-alpha-benzoy-loxy-5-beta, 20-epoxy-1,13-alpha-dihydroxy-9-oxo
-19-nor-cyclopropa[g]tax-11-ene,13-esterwith(2R,3S)-N-tert-bu-toxycarbonyl-3-phenylisoserine, dihydrate
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Larotaxel, undergoing the phase Ⅲ evaluation of France’s sanofi-aventis, is a newly taxanes derivatives. The clinical results show that its effectiveness higher than taxol, and have an effect to breast cancer, which is taxol drug resistance.
Larotaxel is a kind of microtubule inhibitor, can reduce the expression of P glycoprotein. preclinical studies have shown that Larotaxel have an effect to tumor cells which are drug resisitance taxol and docetaxel. The curative effect of treatment of APC and 5 - FU patients have no difference, security is similar to drug taxol.
Strating from 10-DAB, through the acetylation selectively to prepare baccatin, cyclization, coupling of sadi-chain,deprotection to get the qualified raw material.


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