Synthesis of a Novel Pentagastrin??Drug Conjugate for a Targeted Tumor Therapy

…, O Panknin, F Major, B Krewer

Index: Tietze, Lutz F.; Panknin, Olaf; Major, Felix; Krewer, Birgit Chemistry - A European Journal, 2008 , vol. 14, # 9 p. 2811 - 2818

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Citation Number: 13

Abstract

Abstract The synthesis of the novel pentagastrin seco-CBI conjugate 3, which is based on the highly cytotoxic antitumor antibiotic (+)-duocarmycin SA (1), is reported. A key step in the synthesis is the palladium-catalyzed carbonylation of aryl bromide 7 to give the benzyl ester 16, which is transformed into the new seco-CBI derivative 21 bearing a carboxylic acid ester moiety. Subsequent transformation of 21 into an activated ester followed by the ...