A number of novel 7- O -noscapine glycoconjugates have been synthesized starting from noscapine, an alkaloid found in the opium plant, via two successive steps. The first step is a selective 7- O -demethylation of noscapine and the next is a subsequent propargylation which affords 7- O -propargyl noscapine ( 3 ) in good yield. The structure was confirmed by extensive spectroscopic data including single crystal X-ray data. The 1,3-dipolar cycloaddition of the developed noscapine derivative 3 with glycosyl azides 6a–m was investigated to give the triazole-linked second-generation noscapine analogs in their glycoconjugate forms ( 8a–m ) to augment the therapeutic efficacy of noscapine.
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