Solid phase and combinatorial synthesis of compounds on a solid support

Abstract

Abstract Methods, compositions and devices for synthesizing combinatorial libraries of various useful compounds, such as benzodiazepines, prostaglandins, β-turn mimetics and glycerol derived drugs is described. Methodologies for solid phase synthesis of these derivatives is provided. With respect to benzodiazepines, a plurality of regions on the substrate (226a and 226b), which are provided with linker molecules (220) having active sites (222) protected by groups P (224). The linkers are deprotected and coupled to substituted aminobenzophenone molecules A and B, which are then deprotected and coupled to (f-moc) protected aminoacyl moieties C and D. Subsequently, C and D are deprotected and the molecules cyclized to yield a plurality of benzodiazepine compounds on the substrate, useful for receptor screening.

Inventors

• 👤 Jonathan A. Ellman
• 👤 Alex A. Virgilio

Bibliographic Details