Biased Multicomponent Reactions to Develop Novel Bromodomain Inhibitors

Biased Multicomponent Reactions to Develop Novel Bromodomain Inhibitors

BET bromodomain inhibition has contributed new insights into gene regulation and emerged as a promising therapeutic strategy in cancer. Structural analogy of early methyl-triazolo BET inhibitors has prompted a need for structurally dissimilar ligands as probes of bromodomain function. Using fluorous-tagged multicomponent reactions, we developed a focused chemical library of bromodomain inhibito...

Multicomponent Reactions

Multicomponent reactions

Chemistry as a central science is facing a steadily increasing demand for new chemical entities (NCE). Innovative solutions, in all kinds of disciplines that depend on chemistry, require new molecules with specific properties, and their societal consequences are fundamental and pioneering. However, NCE not only demand a realistic structural space but also their feasibility poses challenges to s...

Synthesis of Phosphorus Derivatives via Multicomponent Reactions

Stable derivatives of oxaphosphaphenanthrenes were prepared using multicomponent reactions of 3-bromo-2-naphthol, dialkyl acetylenedicarboxylate and trimethyl or triphenyl phosphite under microwave conditions with good yields. 

Multicomponent reactions II

The concept of multicomponent reactions (MCR) [1] has been around in organic chemistry since the very early days. Indeed, the first example known in literature, the Strecker synthesis of α-aminonitriles [2], has been developed into an industrial process for the production of methionine in an annual scale of several hundreds of thousand tons per year. In addition, a lot of syntheses of heterocyc...