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Synthesis of ascomycin and FK 506 derivatives with modified effector domain

✍ Scribed by Peter Nussbaumer; Maximilian A. Grassberger; Gerhard Schulz

Publisher: Elsevier Science
Year: 1999
Tongue: French
Weight: 205 KB
Volume: 40
Category: Article
ISSN: 0040-4039
DOI: 10.1016/s0040-4039(99)00629-2

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✦ Synopsis

Oxidation of the 22-hydrazone of ascomycin using manganese dioxide generates in situ the reactive 22-diazo intermediate, which decomposes to give ascomycin analogues with modified effector region. In dichloromethane several products are obtained, whereas in methanol a cyclopropane derivative is generated as the main product starting from the hydrazone of both ascomycin and FK 506.

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