Synthesis of four novel natural product inspired scaffolds for drug discovery

…, G Nikolakopoulos, P de Almeida Leone…

Index: Jenkins, Ian D.; Lacrampe, Fabienne; Ripper, Justin; Alcaraz, Lilian; Van Le, Phuc; Nikolakopoulos, George; De Leone, Priscila Almeida; White, Rodney H.; Quinn, Ronald J. Journal of Organic Chemistry, 2009 , vol. 74, # 3 p. 1304 - 1313

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Citation Number: 22

Abstract

Inspired by the novel spiro structures of a number of bioactive natural products such as the histrionicotoxins, a series of novel spiro scaffolds have been designed and robust syntheses developed. The scaffolds are ready-to-use building blocks and can be easily prepared on a 5− 20 g scale. They contain two amino groups (one Boc-protected) and have been designed for ease of conversion to a lead generation library, using either amide formation or ...