90242-55-0Relevant academic research and scientific papers
Bicyclic-Fused Heteroaryl or Aryl Compounds
-
Paragraph 0754, (2015/10/28)
Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
IMIDAZOLIDINE CARBOXAMIDE DERIVATIVES AS P2X7 MODULATORS
-
Page/Page column 37, (2008/12/04)
The present invention relates to a compound of Formula (I) or a pharmaceutically acceptable salt thereof: The compounds or salts modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor (P2X7 receptor antagonists). The invention also provides the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment or prevention of disorders / diseases mediated by the P2X7 receptor, for example pain, inflammation or a neurodegenerative disease, in particular pain such as inflammatory pain, neuropathic pain or visceral pain.
Stereospecific Amination by Dynamic Kinetic Resolution Utilizing 2-Oxoimidazolidine-4-carboxylate as a Novel Chiral Auxiliary
Kubota, Hitoshi,Kubo, Akira,Takahashi, Masami,Shimizu, Ryo,Da-te, Tadamasa,et al.
, p. 6776 - 6784 (2007/10/03)
A novel type of stereospecific amination by dynamic kinetic resolution using (4S)-2-oxoimidazolidine-4-carboxylate (1) as a chiral auxiliary was developed. A reaction of a diastereomeric mixture of (4S)-3--2-oxoimidazolidine-4-carboxylates 4 with an amine in the presence of a base in HMPA predominantly afforded (4S)-3--2-oxoimidazolidine-4-carboxylates (S,R)-7 in good yields.The reaction proceeded by stereospecific SN2 type amination incorporated with rapid interconversion between the substrates (S,S)-4 and (S,R)-4.Mechanistic study suggested that the unique stereoselectivity was induced through the interaction between an amine and the ester group of (S,S)-4 in the transition state.The chiral auxiliary was easily removed with alkoxide anion to afford the α-amino acid synthon in good yields.
