1228587-66-3

Upstream product

• 91271-78-2 (3-(pyrrolidin-1-ylmethyl)phenyl)methanamine 
• 1228587-58-3 ethyl 2-(3-(pyrrolidin-1-ylmethyl)benzylamino)acetate 
• 1228587-56-1 ethyl 2-((6-amino-2-(methylthio)-5-nitropyrimidin-4-yl)(3-(pyrrolidin-1-ylmethyl)benzyl)amino)acetate 
• 51359-78-5 4-(bromomethyl)benzaldehyde 
• 17201-43-3 4-cyanobenzyl bromide 
• 650628-72-1 4-[(pyrrolidin-1-yl)methyl]-benzaldehyde 

Downstream Products

• 1228586-25-1 C₂₂H₂₈N₆O₃ 
• 1228585-41-8 4-amino-2-n-butoxy-8-[4’-(pyrrolidin-1“-ylmethyl)-benzyl]-5,6,7,8-tetrahydropteridin-6-one 

Relevant academic research and scientific papers

METHODS OF PREPARING TOLL-LIKE RECEPTOR MODULATORS

The present invention provides methods of preparing 4-amino-2-biitoxy-8-(3- (pyrrolidin-1-ylmethyl)benzyl)-7,8-dihydropteridin-6(5H)-one and related compounds.

Identification and optimization of pteridinone toll-like receptor 7 (TLR7) agonists for the oral treatment of viral hepatitis

Pteridinone-based Toll-like receptor 7 (TLR7) agonists were identified as potent and selective alternatives to the previously reported adenine-based agonists, leading to the discovery of GS-9620. Analogues were optimized for the immunomodulatory activity and selectivity versus other TLRs, based on differential induction of key cytokines including interferon α (IFN-α) and tumor necrosis factor α (TNF-α). In addition, physicochemical properties were adjusted to achieve desirable in vivo pharmacokinetic and pharmacodynamic properties. GS-9620 is currently in clinical evaluation for the treatment of chronic hepatitis B (HBV) infection.

MODULATORS OF TOLL-LIKE RECEPTORS

Provided are modulators of TLRs of Formula II: pharmaceutically acceptable salts thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.