Three renieramycin-type antitumor alkaloids, (鈭?-jorunnamycins A (1) and C (2) and (鈭?-jorumycin (3), have been synthesized by a new convergent approach, which features a highly regio- and stereoselective Pictet鈥揝pengler cyclization to couple the isoquinoline and the trisubstituted phenylalaninol partners. This synthetic strategy opens an economical access to these important antitumor alkaloids with high yields: (鈭?-jorunnamycin A, as a common precursor to other renieramycin-type alkaloids and their analogues, is obtained with 18.1% overall yield from l-tyrosine.
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