150007-96-8Relevant articles and documents
An improved synthesis of butyl 4-[(4-amino-5-chloro-2-methoxybenzoyl)amino]-1-piperidineacetate (AU-224)
Sakaguchi, Jun,Higashi, Taijiro,Azuma, Takahiro,Suzuki, Tomio,Iwasaki, Nobuhiko,Kondo, Noriyuki,Nagata, Osamu,Kato, Hideo,Hanaoka, Miyoji
, p. 788 - 790 (2001)
A new and facile route for the synthesis of the novel gastrointestinal prokinetic butyl 4-[(4-amino-5-chloro-2-methoxybenzoyl)amino]-1-piperidineacetate (1b), which exhibited potent gastro- and colon-prokinetic activities by oral administration without significant side effects, was established. The key intermediate, butyl 4-amino-1-piperidineacetate (16), was prepared from commercially available 4-amino-1-benzylpiperidine (2) in a high yield with four steps. Compound 1b was prepared by condensation of commercially available 4-amino-5-choloro-2-methoxybenzoic acid (7) with 16 in 84% yield. This improved synthetic route was appropriate for large-scale synthesis of 1b.
Improved synthesis and application of [11C]benzyl iodide in positron emission tomography radiotracer production
Peko?ak, Aleksandra,Filp, Ulrike,Rotteveel, Lonneke,Poot, Alex J.,Windhorst, Albert D.
, p. 342 - 348 (2015/08/03)
Positron emission tomography has increased the demand for new carbon-11 radiolabeled tracers and building blocks. A promising radiolabeling synthon is [11C]benzyl iodide ([11C]BnI), because the benzyl group is a widely present functi
Synthesis and pharmacology of isoquinuclidine derivatives as 5-HT3 ligands
Iriepa, Isabel,Villasante, Francisco J.,Galvez, Enrique,Labeaga, Luis,Innerarity, Ana,Orjales, Aurelio
, p. 189 - 192 (2007/10/03)
A series of 4-amino-5-chloro-2-methoxybenzoates and benzamides containing the 5- and 6-isoquinuclidinyl system was synthesised and evaluated for binding to 5-HT3, 5-HT4 and D2 receptors. In general, the isoquinuclidine derivatives at the 5-position have shown to be more potent as 5-HT3 ligands but they also possess 5-HT4 and D2 properties. However, the results show that the derivatives at the 6-position afforded the most promising compounds in terms of both receptor affinity and selectivity.