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A Concise Synthesis of the DNA-Intercalating and Antimalarial Alkaloid Cryptolepine and Its Fluorescence Behaviour in Solvents of Different Polarities

✍ Scribed by Tapan Kumar Lai; Asima Chatterjee; Julie Banerji; Deboleena Sarkar; Nitin Chattopadhyay


Publisher
John Wiley and Sons
Year
2008
Tongue
German
Weight
202 KB
Volume
91
Category
Article
ISSN
0018-019X

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✦ Synopsis


Abstract

A microwave‐induced rapid and facile synthesis of the DNA‐intercalating and antimalarial drug cryptolepine is described. The key step in this synthesis involves the aqueous‐phase base‐catalyzed condensation of isatin and 1‐acetyl‐1__H__‐indol‐3‐yl acetate which has been simplified and expedited by dielectric heating, employing an ordinary domestic microwave oven. The method transforms the synthesis of an important drug molecule from a prohibitively lengthy process to a matter of a few minutes with a much improved yield. Dual absorption and fluorescence is observed from the molecular system in solvents of different polarity thus providing valuable insight into its binding modes toward protein or DNA.