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Synthetic studies on pactamycin, a potent antitumor antibiotic†
Nobuyuki Matsumoto,Takashi Tsujimoto,Atsuo Nakazaki,Minoru Isobe,Toshio Nishikawa
RSC Advances Pub Date : 07/27/2012 00:00:00 , DOI:10.1039/C2RA21060F
Abstract

Two synthetic approaches to the functionalized cyclopentane core structure of pactamycin are described. The first approach employed the Pauson–Khand reaction of an enyne prepared from diacetone-D-glucose as a chiral starting material, providing a potentially useful tricyclic intermediate for pactamycin. The second approach involved an intramolecular 1,3-dipolar cycloaddition between the nitrone and acetylene functionalities of a precursor derived from an intermediate of the first approach. The expected isoxazoline cycloadduct was not detected, but instead an aziridine aldehyde was obtained, probably through ring contraction (Baldwin rearrangement) of the expected isoxazoline product. Further transformation provided a highly functionalized cyclopentane bearing an aniline at the C-3 position, but with different stereochemistry from that of pactamycin.

Graphical abstract: Synthetic studies on pactamycin, a potent antitumor antibiotic
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