4.4 Article

One-step synthesis of 2-arylbenzothiazole ('BTA') and -benzoxazole precursors for in vivo imaging of β-amyloid plaques

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TETRAHEDRON LETTERS
卷 46, 期 8, 页码 1349-1351

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2004.12.111

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2-arylbenzothiazole; BTA; 2-arylbenzoxazole; amyloid plaques; palladium; direct coupling

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We report the simple and efficient synthesis of 2-arylbenzothiazoles ('BTA') and 2-arylbenzoxazoles by direct coupling of benzothiazoles or benzoxazoles with aryl bromides. This method permits direct one-step access to precursors of radiolabeled BTA-1 and BTA-2 and their 6-rnethoxy analogues, used for in vivo imaging of beta-amyloid plaques with positron emission tomography (PET). (C) 2004 Elsevier Ltd. All rights reserved.

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