30568-46-8Relevant articles and documents
Synthesis and pharmacological evaluation of 1-Alkyl-N-[(1R)-1-(4- fluorophenyl)-2-methylpropyl]piperidine-4-carboxamide derivatives as novel antihypertensive agents
Watanuki, Susumu,Matsuura, Keisuke,Tomura, Yuichi,Okada, Minoru,Okazaki, Toshio,Ohta, Mitsuaki,Tsukamoto, Shin-Ichi
, p. 1376 - 1385 (2012/01/05)
We synthesized and evaluated inhibitory activity against T-type Ca 2+ channels for a series of 1-alkyl-N- [(1R)-1-(4-fluorophenyl)-2- methylpropyl]piperidine-4-carboxamide derivatives. Structure-activity relationship studies have revealed that the isopropyl substituent at the benzylic position plays an important role in exerting potent inhibitory activity, and the absolute configuration of the benzylic position was found to be opposite that of mibefradil, which was first launched as a new class of T-type Ca2+ channel blocker. Oral administration of N- [(1R)-1-(4-fluorophenyl)-2-methylpropyl]-1-[2-(3-methoxyphenyl)ethyl] piperidine-4-carboxamide (17f) lowered blood pressure in spontaneously hypertensive rats without inducing reflex tachycardia, an adverse effect often caused by traditional L-type Ca2+ channel blockers.
One-pot synthesis of primary tert-alkylamines by the addition of organometallic reagents to nitriles mediated by Ti(Oi-Pr)4
Tomashenko, Olesya,Sokolov, Viktor,Tomashevskiy, Alexander,De Meijere, Armin
, p. 652 - 654 (2007/10/03)
A number of primary tert-alkylamines (18 examples, 25-72% yields) have been prepared according to a simple one-pot procedure by the addition of organometallic reagents such as Grignard reagents and organolithium compounds to nitriles in the presence of Ti(Oi-Pr)4. Georg Thieme Verlag Stuttgart.
Imidazole derivatives as therapeutic agents
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, (2008/06/13)
Compounds of the formula I STR1 and pharmaceutically acceptable salts thereof in which R1 represents hydrogen, halo, cyano, cyanoalkyl, alkyl, alkoxy, phenoxy, phenyl, alkoxycarbonyl, --NR13 R14, --N(R15)SO2 R16, halogenated alkoxy, halogenated alkyl, arylalkoxy, hydroxy, phenylalkyl, alkoxycarbonylvinyl, --S(O)n R7, alkoxycarbonylalkyl, carboxyalkyl, --CONR11 R12 carbamoylvinyl, --OSO2 R21, 4,5-dihydrothiazol-2-yl, 4,4-dimethyl-2-oxazolin-2-yl or --NR60 R61 ; or R1 represents a group of formula --(O)z --L3 G wherein z equals 0 or 1, L3 represents a C1-4 alkylene chain, G represents a group of formula a), b), c), or d): a) --NR22 R23 ; b) --S(O)m R26 ; c) CONR27 R28 ; d) --OR29 ; R2 and R3 independently represent hydrogen, halo, alkyl, alkoxy, --NR13 R14, halogenated alkoxy, halogenated alkyl, hydroxy, --S(O)n R7 or --NR60 R61 ; L1 represents e) a bond, or f) alkylene, cycloalkylene or cycloalkylidene; T represents a bond or O, S, SO, SO2, a carbonyl group, or 1,3-dioxolan-2-ylidene; L2 represents alkylene, cycloalkylene, or cycloalkylidene; R6 represents hydrogen or alkyl (optionally substituted by alkoxycarbonyl or hydroxy); Q represents a C1-9 alkylene chain (optionally substituted by alkyl or hydroxy); and Y represents an optionally substituted imidazole ring; which are antiinflammatory, antiallergic and immunodulant agents. Compositions containing these compounds and processes to make them are also disclosed.