COMPOUND DIVERSIFICATION USING LATE STAGE FUNCTIONALIZATION

摘要

The present invention relates to methods for generating limited chemical diversity for biologically relevant lead molecules by late state functionalization, separation, and post-functionalization modification. The methods optionally include one or more screening steps. Traditional drug development has relied on the synthesis of individual compounds or the generation of large chemical libraries, but these methods have generally been fairly inefficient in obtaining drug products.

主权项

1. A method for generating a compound library comprising the following steps:
a) functionalizing a compound using a C—H functionalization chemistry to form a mixture of compounds; and b) performing one or more post-functionalization modification chemistries on the mixture of compounds.