ISSN:
1573-501X
Keywords:
benzodiazepine
;
combinatorial chemistry
;
intramolecular cyclization
;
polymer-bound precursor
;
scaffold
;
solid-phase synthesis
Source:
Springer Online Journal Archives 1860-2000
Topics:
Chemistry and Pharmacology
Notes:
Abstract An efficient method for solid-phase constructionof tetrahydro-1,4-benzodiazepin-2-one scaffold is described.Polymer-bound 4-(bromomethyl)-3-nitrobenzoic acid was reactedwith α-amino acid methyl esters, followed by nitro groupreduction and hydrolysis. Subsequent intramolecular cyclizationand alkylation at N(4) afforded the structurally diverse productsin high yields and excellent purities.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1023/A:1016282115183
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