100911-29-3Relevant academic research and scientific papers
THIAZOLE DERIVATIVE
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Page/Page column 67-68, (2012/12/14)
Provided is a compound having an agonist action on GPR52, which is useful as a prophylactic or therapeutic drug for mental diseases such as schizophrenia and the like, and the like. A compound represented by the formula (I): wherein each symbol is as defi
Discovery of an orally efficaceous 4-phenoxypyrrolidine-based BACE-1 inhibitor
Iserloh,Pan,Stamford,Kennedy,Zhang,Zhang,Parker,McHugh,Favreau,Strickland,Voigt
, p. 418 - 422 (2008/09/18)
Based on a lead compound identified from the patent literature, we developed patentably novel BACE-1 inhibitors by introducing a cyclic amine scaffold as embodied by 1a and 1b. Extensive SAR studies assessed a variety of isophthalamide replacements including substituted pyrrolidinones and ultimately led to the identification of 11. Due to its favorable overall profile, 11 has been extensively profiled in various in vivo settings.
A chemoenzymatic approach to the synthesis of enantiomerically pure aza analogues of paraconic acid methyl ester and both enantiomers of methyl β-proline
Felluga, Fulvia,Pitacco, Giuliana,Prodan, Massimo,Pricl, Sabrina,Visintin, Marco,Valentin, Ennio
, p. 3241 - 3249 (2007/10/03)
Enantiopure methyl esters of 1-alkyl-5-oxo-3-pyrrolidinecarboxylic acids were obtained by enzymatic resolution of the corresponding chiral racemic mixtures. A particularly favourable interaction, also supported by molecular mechanics calculations, was observed between the 1-benzyl derivative and α-chymotrypsin, for which the enantiomeric ratio, E, exceeded 200. The absolute configurations of the lactams were determined by means of CD spectroscopy. From the resulting enantiomerically pure (99% e.e.) (S)-(+)-1-benzyl-3-pyrrolidinecarboxylic acid and methyl (R)-(-)-1-benzyl-3-pyrrolidinecarboxylate, the methyl esters of (+) and (-)-β-proline were synthesised in 99% e.e. and 18 and 22% overall yield, respectively.
