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

被引:150
作者
Alagille, D
Baldwin, RM
Tamagnan, GD
机构
[1] Yale Univ, New Haven, CT 06510 USA
[2] VA CT, HCS, Dept Psychiat, New Haven, CT 06510 USA
[3] Inst Neurodegenerat Disorders, New Haven, CT 06510 USA
基金
美国国家卫生研究院;
关键词
2-arylbenzothiazole; BTA; 2-arylbenzoxazole; amyloid plaques; palladium; direct coupling;
D O I
10.1016/j.tetlet.2004.12.111
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
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.
引用
收藏
页码:1349 / 1351
页数:3
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