21782-59-2Relevant articles and documents
Scandium(III) Triflate-Catalyzed anti-Markovnikov Hydrothiolation of Functionalized Olefins
Kuciski, Krzysztof,Pawluc, Piotr,Hreczycho, Grzegorz
supporting information, p. 3936 - 3942 (2016/01/25)
Scandium(III) triflate promoted highly selective addition of thiols to functionalized olefins under mild conditions. The addition follows anti-Markovnikov regioselectivities, which are unusual for Lewis acids-catalyzed hydrothiolation. This reaction marks broad functional groups tolerance, which opens a beneficial synthetic route to functionalized and biologically active thio-compounds. This method is broadly applicable and offers a simple work-up in the green manner.
BENZOIC ACID COMPOUNDS AND USE THEREOF AS MEDICAMENTS
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, (2008/06/13)
Benzoic acid compounds of the formula STR1 wherein each symbol is as defined in the specification, optical isomers thereof and pharmaceutically acceptable salts thereof; pharmaceutical composition comprising this compound and pharmaceutically acceptable additive; and serotonin 4 receptor agonists, gastrointestinal prokinetic agents and therapeutic agents for various gastrointestinal diseases, which comprise this compound as active ingredient. The compounds of the present invention have high and selective affinity for serotonin 4 receptor, and show agonistic effects thereon. Accordingly, they are useful medications for the prophylaxis and treatment of various gastrointestinal diseases, central nervous disorders, cardiac function disorders, urinary diseases, and the like, as well as useful anti-nociceptors for analgesic use which increase threshold of pain.
Synthesis of potent non-imidazole histamine H3-receptor antagonists
Ganellin, C. Robin,Leurquin, Fabien,Piripitsi, Antonia,Arrang, Jean-Michel,Garbarg, Monique,Ligneau, Xavier,Schunack, Walter,Schwartz, Jean-Charles
, p. 395 - 404 (2007/10/03)
Histamine has been converted into a non-imidazole H3-receptor histamine antagonist by addition of a 4-phenylbutyl group at the N(α)-position followed by removal of the imidazole ring. The resulting compound, N-ethyl- N-(4-phenylbutyl)amine, remarkably has a Ki = 1.3 μM as an H3 antagonist. Using this as a lead compound, a novel series of homologous O and S isosteric tertiary amines was synthesised and structure-activity studies furnished N- (5-phenoxypentyl)pyrrolidine (Ki = 0.18 ± 0.10 μM, for [3H]histamine release from rat cerebral cortex synaptosomes) which, more importantly, was active in vivo. Substitution of NO2 into the para position of the phenoxy group gave N-(5-p-nitrophenoxypentyl)pyrrolidine, UCL 1972 (Ki= 39 ± 11 nM), ED50 = 1.1 ± 0.6 mg/kg per os in mice on brain tele-methylhistamine levels.