27514-07-4Relevant articles and documents
Unexpected resistance to base-catalyzed hydrolysis of nitrogen pyramidal amides based on the 7-azabicyclic[2.2.1]heptane scaffold
De Velasco, Diego Antonio Ocampo Gutiérrez,Su, Aoze,Zhai, Luhan,Kinoshita, Satowa,Otani, Yuko,Ohwada, Tomohiko
, (2018/09/26)
Non-planar amides are usually transitional structures, that are involved in amide bond rotation and inversion of the nitrogen atom, but some ground-minimum non-planar amides have been reported. Non-planar amides are generally sensitive to water or other n
7-Azabicyclo[2.2.1]heptane as a scaffold for the development of selective sigma-2 (σ2) receptor ligands
Banister, Samuel D.,Rendina, Louis M.,Kassiou, Michael
supporting information; experimental part, p. 4059 - 4063 (2012/07/03)
A series of N-substituted 7-azabicyclo[2.2.1]heptanes (12-17 and 22-25) and similarly substituted pyrrolidines (32-36 and 41-44) were synthesized as sterically-reduced, achiral analogs of adamantane- and trishomocubane-derived σ ligands. In vitro competition binding assays against σ receptors revealed that arylalkyl N-substituents conferred selectivity for the σ2 subtype, while alicyclic or polycarbocyclic substituents imparted high affinity for both subtypes. The σ2 binding and subtype selectivities of N-arylalkyl-7-azanorbornanes was generally greater than the analogously-substituted pyrrolidines, indicating that steric bulk and conformational restriction around the nitrogen atom are likely important for subtype discrimination.
PROCESSES FOR PRODUCING MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR
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Page/Page column 41, (2011/12/04)
The present invention relates to the process for producing modulators of cystic fibrosis transmembrane conductance regulator (CFTR).