mardi 17 avril 2007

Synthesis of the camptothecin core

The post of today deals with the synthesis of the camptothecin core.

This synthesis described by Fortunak in 1996, has an intramolecular Diels-Alder [4+2] cycloaddition as key step between an unactivated alkyne and a imidate generated
in situ by action of Me3OBF4 on a N-arylamide.

This synthesis has been recently improved by Yao et al. using a mixture of Ph
3PO and Tf2O (2:1) instead of Me3OBF4, by this methodology a wide range of tetracyclic "camptothecin-like" molecules has been synthesized.

Organic Letters, ASAP, April 14, 2007

1 commentaire:

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