A facile synthesis of bis-tacrine isosteres

An efficient synthesis of highly potent and selective acetylcholinesterase (AChE) inhibitors, bis-tacrines and their isosteres 2– 4, has been accomplished by bis-amination of 9-chloro-tetrahydroacridine ( 9a) and its analogs. The critical intermediates were concisely prepared in situ by heating the...

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Bibliographic Details
Published inTetrahedron letters Vol. 41; no. 11; pp. 1815 - 1818
Main Authors Hu, Ming-Kuan, Lu, Chih-Feng
Format Journal Article
LanguageEnglish
Published OXFORD Elsevier Ltd 11.03.2000
Elsevier
Subjects
Chemistry
Chemistry, Organic
Physical Sciences
Science & Technology
ALZHEIMERS-DISEASE
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Summary:An efficient synthesis of highly potent and selective acetylcholinesterase (AChE) inhibitors, bis-tacrines and their isosteres 2– 4, has been accomplished by bis-amination of 9-chloro-tetrahydroacridine ( 9a) and its analogs. The critical intermediates were concisely prepared in situ by heating the corresponding ortho-amino aromatic acids and cycloketones in the presence of phosphorus oxychloride.
ISSN:0040-4039
1873-3581
DOI:10.1016/S0040-4039(00)00036-8