1194565-98-4Relevant academic research and scientific papers
Magnesium meerwein-ponndorf-verley-oppenauer reaction. the origin of an impurity in PDA-641 batches
Wilk, Bogdan K.,Helom, Jean L.,Coughlin, Clifford W.
, p. 407 - 411 (1998)
An impurity in the initial scale-up batch of PDA-641 was identified and the pathway of its formation was established. The precursor of the impurity was formed by magnesium Meerwein-Ponndorf-Verley-Oppenauer reaction during the Grignard addition step. As a
New selective phosphodiesterase 4D inhibitors differently acting on long, short, and supershort isoforms
Bruno, Olga,Romussi, Alessia,Spallarossa, Andrea,Brullo, Chiara,Schenone, Silvia,Bondavalli, Francesco,Vanthuyne, Nicolas,Roussel, Christian
supporting information; scheme or table, p. 6546 - 6557 (2010/03/26)
The lack of selective inhibitors toward the long, short, or supershort phosphodiesterases (PDE4s) prevented researchers from carefully defining the connection between different enzyme isoforms, their brain localization, and their role in neurodegenerative diseases such as Alzheimer's disease (AD). In the search for new therapeutic agents for treating memory and learning disorders, we synthesized new rolipram related PDE4 inhibitors, which had some selectivity toward the long form PDE4D3. The first series was synthesized as racemate and then resolved by semipreparative HPLC on chiral supports. Herein we report the synthetic pathways to obtain compounds 1a-c, 2a-c, 3a-c, 4a-f, 5a,b, 6a,b, 7a,b, the chiral analytical study to resolve compounds 1a-c, 2a-c, 3a-c, the molecular docking study for compound 1c, and the biological results and some SAR considerations that provide some insights and hints for the structural requirements for PDE4D subtype selectivity and enzyme inhibition.
