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Synthesis of Novel Taxol Analogues with Heterocylclic Amino Moieties

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The synthesis of novel taxol analogues with an amiRe moiety at the 7- and 10-positions to examine the BBB penetration was described. The analogues were synthesized from 2'- 0- (tert-butyldim-ethylsilyl)taxol and 2'-0- (text- butyldimethylsilyl)-7-0- (triethylsilyl)-10-deacetyltaxol, the key intermediates, in 2 steps via the esterification with heterocyclic amino acids and the subsequent desilylation reaction.

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