40624-07-5Relevant articles and documents
N-[2-(1-azabicyclo[3.3.0]octan-5-YL)ethyl]-2-nitroaniline, a potent muscarinic agonist
Suzuki,Oka,Maeda,Furusawa,Mitani,Kataoka
, p. 1218 - 1220 (1997)
The muscarine receptor agonist SK-946, an aniline derivative with a characteristic bicyclo amine, was found. We describe a new synthetic method for 1-azabicyclo[3.3.0]octane and describe the biological activity of SK- 946.
A double-ring propyl alkone improved process for synthesizing (by machine translation)
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Paragraph 0037-0039, (2017/03/28)
The invention discloses a double-ring improved process for synthesizing propyl alkone. First of all, the reaction is an inert organic solvent in the presence of and solid sodium alcoholate, γ? Butyrolactone dehydration condensation between the molecules occurs, produce intermediate; then to the adding concentrated hydrochloric acid in the reaction system, generating a decarboxylation reaction, 1,7? Dichloroborane? 4? Heptanone crude; finally, in action ShiShimonoseki ahead into a double-ring n-propyl ketone. The invention has the advantage of using an inert organic solvent and solid sodium alcoholate, does not need the recovery carries on mellowly is greatly improved controllability and reaction, reduction reaction by-product, the product yield is higher than the conventional technical 15-20%, the production cost is reduced, reducing the environmental pressure, product quality is improved. (by machine translation)
Synthesis and nicotinic receptor activity of chemical space analogues of N -(3 R)-1-azabicyclo[2.2.2]oct-3-yl-4-chlorobenzamide (PNU-282,987) and 1,4-diazabicyclo[3.2.2]nonane-4-carboxylic acid 4-bromophenyl ester (SSR180711)
Bréthous, Lise,Garcia-Delgado, Noemi,Schwartz, Julian,Bertrand, Sonia,Bertrand, Daniel,Reymond, Jean-Louis
supporting information; experimental part, p. 4605 - 4618 (2012/07/28)
The Chemical Universe Generated Databases up to 11 atoms of CNOF (GDB-11) and up to 13 atoms of CNOClS (GDB-13) were used to enumerate analogues of the diamine part of two known α7 nicotinic receptor agonists and construct libraries of virtual analogues of these drugs. The libraries were scored using structure-based (docking to the nicotine binding site of the acetylcholine binding protein 1uw6.pdb) or ligand-based (similarity to the parent drugs) methods, and the top-scoring virtual ligands were inspected for easily accessible synthetic targets. In total, 21 diamines were prepared and acylated with aromatic carboxylic or oxycarbonic acids to produce 85 analogues of the parent drugs. The compounds were profiled by electrophysiology in Xenopus oocytes expressing human nicotinic acetylcholine receptor (nAChR) subtypes α7, α3β2, α4β2, α3β4, or α4β4. Characterization of selected compounds revealed eight inhibitors of the α7 nicotinic receptor and three positive allosteric modulators of the α3β2 nAChR.