Synthesis of Antitumor Bicyclic Hexapeptide RA-VII Analogues Possessing an Aromatic Amino Acid at Residue 2

RA-III acetate was treated with Lawesson’s reagent to afford [Tyr-3-Ψ­(CS-NH)-Ala-4]­RA-III acetate. Treatment of this product with Hg­(OAc)2/Li2CO3 and then methanol gave an oxazole intermediate. Acid-catalyzed arylation of the methylene carbon atom on the oxazole ring and subsequent partial hydrol...

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