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200517.fm Page 134 Friday, March 18, 2005 2:52 PM
2005
Pyrazole derivatives
R 0180
Preparation and Acylation of Highly Functionalized Copper Derivatives of
Leading to Polyfunctional 3-Acylindazoles. — The regioselective
17- 121 3-Iodoindazoles
acylation of indazole derivatives is smoothly achieved by iodine—copper exchange
reaction of 3-iodoindazole (I) with LiCu(neophyl)2 reagent, followed by acylation with
acid chlorides. A wide range of acid chlorides (II) can be used, including aliphatic,
aromatic as well as α,β-unsaturated acid chlorides. Additionally, the presence of
diverse functional groups is tolerated in the heterocyclic cuprate. — (YANG, X.;
KNOCHEL*, P.; Synlett 2004, 13, 2303-2306; Fachbereich Chem.,
Ludwig-Maximilians-Univ., D-81377 Muenchen, Germany; Eng.) — Mischke
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