Solid phase and combinatorial synthesis of benzodiazepine compounds on a solid support
AssigneeThe Regents of the University of California
InventorJonathan A. Ellman
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Abstract
Methods, compositions, and devices for synthesis of therapeutically useful compounds. The invention provides a rapid approach for combinatorial synthesis and screening of libraries of derivatives of therapeutically important classes of compounds such as benzodiazepines, prostaglandins and .beta.-turn mimetics. In order to expediently synthesize a combinatorial library of derivatives based upon these core structures, general methodology for the solid phase synthesis of these derivatives is also provided. This disclosure thus also describes an important extension of solid phase synthesis methods to nonpolymeric organic compounds.
Claims18
A method of making a plurality of benzodiazepines on a substrate comprising the steps of:
- coupling substituted amino benzophenones to a substrate, said substituted amino benzophenones comprising protecting groups;
- removing said protecting groups from said amino benzophenones to form amino benzophenones having amino active sites;
- coupling a plurality of amino acid derivatives to said amino active sites;
- and
- cyclizing molecules resulting from the step of coupling said plurality of amino acid derivatives, whereby a plurality of benzodiazepines are formed on said substrate.
Dependencies are inferred from the claim text.