Journal
TETRAHEDRON
Volume 62, Issue 11, Pages 2465-2470Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tet.2006.01.001
Keywords
camptothecin; topoisomerase 1; Sonogashira coupling; palladium; catalysis
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We studied copper-free Sonogashira reaction using 7-chloro camptothecins, and determined that rac-BINAP/Pd(OAc)(2) was an efficient catalyst for the coupling reaction. With this process, a number of 7-substituted camptothecins with a wide range of functional groups are potentially accessible. Besides, two drugs, SN-38 and BNP-1350, Could be prepared by this method. (c) 2006 Elsevier Ltd. All rights reserved.
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