4.4 Article

Studies toward the total synthesis of RP-66453

Journal

TETRAHEDRON LETTERS
Volume 43, Issue 14, Pages 2577-2580

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0040-4039(02)00307-6

Keywords

neurotensine receptor antagonist; RP 66453; macrocycle; biaryl; biaryl ether; intramolecular SNAr reaction

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Synthesis of a bicyclic A-B-O-C ring system of RP-66453, an neurotensine receptor antagonist, with an endo aryl-aryl and an endo aryl-aryl ether bond is described. An alternative synthetic strategy starting from the construction of functionalized B-O-C cycloisodityrosine unit is also detailed. (C) 2002 Elsevier Science Ltd. All rights reserved.

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