Method for docetaxel synthesis

作者: Nicholas J. Sisti , Charles S. Swindell

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摘要: A method of producing docetaxel comprises the esterification C7, C10 di-CBZ 10-deacetyl baccatin III and an N-CBZ C2'-protected 3-phenyl isoserine side chain wherein C2' is protected by a hydrogenatable benyl-type protecting group. The carbobenzyloxy groups are then replaced with hydrogen group at C3' nitrogen site t-butoxycarbonyl. Finally, resulting compound deprotected replacing benzyl-type to produce docetaxel. preferably employs excess, such as six equivalents, for each equivalent III. Benzyloxymethyl preferred C2'.

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