1355174-84-3

Upstream product

• 89792-20-1 6-methyl-7H-pyrrolo[2,3-d]pyrimidine-2,4-diol 
• 1377432-79-5 tert-butyl 2-chloro-6-methyl-4-oxo-4H-pyrrolo[2,3-d]pyrimidine-7(4aH)-carboxylate 
• 22115-41-9 2-(bromomethyl)benzonitrile 
• 1355174-81-0 2-chloro-6-methyl-4,7-dihydro-4H-pyrrolo[2,3-d]pyrimidin-4-one 
• 1192711-71-9 2,4-dichloro-6-methyl-7H-pyrrolo[2,3-d]pyrimidine 

Downstream Products

• 1355173-69-1 2-((2-((R)-3-aminopiperidin-1-yl)-6-methyl-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-3-yl)methyl)benzonitrile 

Relevant academic research and scientific papers

Novel pyrrolopyrimidine analogues as potent dipeptidyl peptidase IV inhibitors based on pharmacokinetic property-driven optimization

We previously reported a highly potent DPP-IV inhibitor 6 with low in vivo efficacy. While trying to maintain consistent in vitro and in vivo biological activity, we initiated a pharmacokinetic property-driven optimization to improve the metabolic stability and permeability of inhibitor 6. A simple scaffold replacement of thienopyrimidine with pyrrolopyrimidine (21a) led to significantly improved metabolic stability (4% vs. 65% remaining). Further modification of the pyrrolopyrimidine scaffold to produce compound 21j resulted in much better oral bioavailability than 6. Importantly, compound 21j exhibits greater in vivo efficacy than does 6 and Alogliptin and is worthy of further development.