221654-69-9Relevant articles and documents
Synthesis of 1-[(1R)-1-(6-fluoro-1,3-benzothiazol-2-yl)ethyl]-3-substituted phenyl ureas and their inhibition activity to acetylcholinesterase and butyrylcholinesterase
Pejchal, Vladimir,Stepankova, Sarka,Drabina, Pavel
experimental part, p. 57 - 62 (2011/03/21)
A series of novel 1-[(1R)-1-(6-fluoro-1,3-benzothiazol-2-yl)ethyl]-3- substituted phenyl ureas were synthesized by the condensation of (1R)-1-(6-fluoro-1,3-benzothiazol-2-yl)ethanamine with substituted phenyl isocyanates under mild conditions. Their structures were confirmed 1H, 13C, and 19F NMR spectra, and elemental analyses. The optical activities were confirmed by optical rotation measurements. The inhibition activity of 1-[(1R)-1-(6-fluoro-1,3-benzothiazol-2- yl)ethyl]-3-substituted phenyl ureas to acetylcholinesterase (ACHE) and butyrylcholinesterase (BCHE) was also tested. Preliminary bioassay indicated that the target ureas displayed excellent acetylcholinesterase and butyrylcholinesterase inhibition activity.
Process for producing substituted alkylamines or salts thereof
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, (2008/06/13)
The present invention provides a process for producing a substituted alkylamine represented by formula (3): or a salt thereof, which process comprises reacting a 2-aminothiophenol derivative metal salt represented by formula (1): with an amino acid-N-carboxy anhydride represented by formula (2): and then subjecting the reaction product to cyclization under an acidic condition. A substituted alkylamine typified by 1-(2-benzothioazolyl)akylamine, or a salt thereof can be produced from a 2-aminothiophenol derivative industrially at a high handleability and a high yield, and even when the intended substituted alkylamine is an optically active compound, the intended product can be produced without reducing the optical purity of the optically active raw material.
