101046-32-6Relevant articles and documents
Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 2: Development of a [3.3.0]-based series and other piperidine bioisosteres
Sheffler, Douglas J.,Nedelovych, Michael T.,Williams, Richard,Turner, Stephen C.,Duerk, Brittany B.,Robbins, Megan R.,Jadhav, Sataya B.,Niswender, Colleen M.,Jones, Carrie K.,Conn, P. Jeffrey,Daniels, R. Nathan,Lindsley, Craig W.
, p. 1062 - 1066 (2014/03/21)
This Letter describes the development and SAR of a novel series of GlyT1 inhibitors derived from a scaffold hopping approach, in lieu of an HTS campaign, which provided intellectual property position. Members within this new [3.3.0]-based series displayed excellent GlyT1 potency, selectivity, free fraction, and modest CNS penetration. Moreover, enantioselective GlyT1 inhibition was observed, within this novel series and a number of other piperidine bioisosteric cores.
Prostanoids and related compounds. V. Synthesis of 6-aza-5-oxo-2,3,4-trinor-1,5-inter-m-phenylene prostacyclin derivatives
Miyajima,Takemoto,Achiwa
, p. 3175 - 3179 (2007/10/02)
6-Aza-5-oxo-2,3,4-trinor-1,5-inter-m-phenylene prostacyclin derivatives were synthesized by use of 1,3-dipolar cycloaddition as a key step.
Trifluoroacetic Acid-Catalyzed 1,3-Cycloaddition of the Simplest Iminium Ylide Leading to 3- or 3,4-Substituted Pyrrolidines and 2,5-Dihydropyrroles
Terao, Yoshiyasu,Kotaki, Hiromi,Imai, Nobuyuki,Achiwa, Kazuo
, p. 2762 - 2766 (2007/10/02)
The 1,3-dipolar cycloaddition of an intermediary iminium ylide formed from N-benzyl-N-(methoxymethyl)trimethylsilylmethylamine to conjugated olefinic and acetylenic dipolarophiles in the presence of a catalytic amount of trifluoroacetic acid has been found to give 3- or 3,4-substituted pyrrolidines and 2,5-dihydropyrroles.