19715-80-1Relevant academic research and scientific papers
Amidation reaction of carboxylic acid with formamide derivative using SO3?pyridine
Kawano, Shota,Saito, Kodai,Yamada, Tohru
supporting information, p. 584 - 586 (2018/04/12)
The amidation reaction of carboxylic acid derivatives was developed using sulfur trioxide pyridine complex (SO3?py) as a commercially available and easily handled oxidant. This method could be applied to the reaction of various aromatic and aliphatic carboxylic acids, including optically active ones, with formamide derivatives to afford the corresponding amides in good to high yields.
SULFONAMIDE DERIVATIVE AND PREPARATION METHOD AND USE THEREOF
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Paragraph 0119; 0120, (2018/11/21)
The present invention discloses a compound shown in formula I or a stereoisomer, pharmaceutically acceptable salt, crystal form, solvate or isotopologue thereof. The compound of the present invention shows excellent inhibition activity against histone dea
Catalytic Enantioselective α-Fluorination of 2-Acyl Imidazoles via Iridium Complexes
Xu, Guo-Qiang,Liang, Hui,Fang, Jie,Jia, Zhi-Long,Chen, Jian-Qiang,Xu, Peng-Fei
supporting information, p. 3355 - 3358 (2016/12/09)
The first highly enantioselective α-fluorination of 2-acyl imidazoles utilizing iridium catalysis has been accomplished. This transformation features mild conditions and a remarkably broad substrate scope, providing an efficient and highly enantioselective approach to obtain a wide range of fluorine-containing 2-acyl imidazoles which are found in a variety of bioactive compounds and prodrugs. A large scale synthesis has also been tested to demonstrate the potential utility of this fluorination method.
A chemoselective Reformatsky-Negishi approach to α-haloaryl esters
Wong, Brian,Linghu, Xin,Crawford, James J.,Drobnick, Joy,Lee, Wendy,Zhang, Haiming
, p. 1508 - 1515 (2014/02/14)
A practical synthesis of α-haloaryl esters has been achieved via a chemoselective Negishi coupling of poly-halogenated aromatics and Reformatsky reagents in the presence of catalytic Pd(dba)2 and Xantphos. This chemistry tolerates a variety of aryl halides and was successfully applied to the synthesis of Ibuprofen. The α-haloaryl ester products, exemplified by ethyl 2-(4-bromo-2-chlorophenyl)acetate (3a), can be further functionalized via palladium or copper catalysis to afford an array of α-aryl esters.
COMPOUNDS WHICH POTENTIATE AMPA RECEPTOR AND USES THEREOF IN MEDICINE
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Page/Page column 86, (2008/06/13)
Compounds of formula (I) and salts and solvates are provided: formula (I). Processes for preparation, pharmaceutical compositions, and uses thereof as a medicament, for example in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.
Palladium-catalyzed conversion of benzylic and allylic halides into α-aryl and β,γ-unsaturated tertiary amides by the use of a carbamoylsilane
Cunico, Robert F.,Pandey, Rajesh K.
, p. 9048 - 9050 (2007/10/03)
Treatment of allylic and benzylic halides with N,N- dimethylcarbamoyl(trimethyl)silane in the presence of tetrakis- (triphenylphosphine)palladium(0) affords tertiary amides, which arise from the replacement of the halogen by the N,N-dimethylcarbamoyl group.
NEW BICYCLIC ANGIOTENSIN II AGONISTS
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Page 37, (2010/02/07)
There is provided compounds of formula (I), wherein R1a, R1b, n, Y1, Y2, Y3, Y4, Z1, Z2, R2 and R3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful as selective agonists of the AT2 receptor, and thus, in particular, in the treatment of inter alia gastrointestinal conditions, such as dyspepsia, IBS and MOF, and cardiovascular disorders.
N9 -cyclopentyl-substituted adenine derivatives having adenosine-2 receptor stimulating activity
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, (2008/06/13)
The compound of the formula I STR1 wherein R, R 3 and R 5 independently represent hydrogen or hydroxy provided that at least one of R, R 3 and R 5 represents hydroxy; R 1 represents hydrogen, lower alkyl, C 3 -C 7 -alkenyl, hydroxy-lower alkyl, optionally substituted cycloalkyl or optionally substituted cycloalkyl-lower alkyl, bicycloalkyl, bicycloalkyl-lower alkyl, adamantyl, tetrahydropyranyl, tetrahydrothiopyranyl, tetrahydropyranyl-lower alkyl, tetrahydrothiopyranyl-lower alkyl, adamantyl-lower alkyl, aryl-hydroxy-lower alkyl, aryl, aryl-lower alkyl, aryl-C 3 -C 6 -cycloalkyl, 9-fluorenyl, 9-fluorenyl-lower alkyl or cycloalkenyl-lower alkyl; or R 1 represents a bicyclic benzo-fused 5 or 6-membered saturated cyabocyclic radical or a benzo-fused 5 or 6-membered saturated heterocyclic radical containing a heteroatom selected from oxygen and sulfur directly attached to the fused benzene ring, any said bicyclic radicals being optionally substituted on the benzo portion by lower alkyl, lower alkoxy or halogen, or R 1 represents any said bicyclic radical substituted-lower alkyl; R 2 represents hydrogen, halogen, --S--R 1 '', --NR b --R 1 '', or --NH--R 1 '' in each of which R 1 '' has meaning as defined for R 1 provided that R 1 '' in --SR 1 '' does not represent hydrogen; R b represents lower alkyl; R 4 represents hydroxymethyl provided that R 2 does not represent either hydrogen or --NHR 1 '' in which R 1 '' represents either hydrogen or lower alkyl; or R 4 represents lower alkoxymethyl or lower alkylthiomethyl; or R 4 represents --CONHR 6 in which R 6 represents lower alkyl; aryl-lower alkyl, C 3 -C 6 -cycloalkyl or hydroxy-lower alkyl; pharmaceutically acceptable ester derivatives thereof in which free hydroxy groups are esterified in form of a pharmaceutically acceptable ester; and pharmaceutically acceptable salts thereof; methods for their preparation; and their use as adenosine receptor agonists are disclosed.
2-Phenyl-2-(1-hydroxycycloalkyl)ethylamine derivatives: Synthesis and antidepressant activity
Yardley,Morris Husbands,Stack,Butch,Bicksler,Moyer,Muth,Andree,Fletcher III,James,Sielecki
, p. 2899 - 2905 (2007/10/02)
A series of 2-phenyl-2-(1-hydroxycycloalkyl)ethylamine derivatives was examined for the ability to inhibit both rat brain imipramine receptor binding and the synaptosomal uptake of norepinephrine (NE) and serotonin (5-HT). Neurotransmitter uptake inhibition was highest for a subset of 2-phenyl-2-(1-hydroxycyclohexyl)dimethylethylamines in which the aryl ring has a halogen or methoxy substituent at the 3- and/or 4-positions. Potential antidepressant activity in this subset was assayed in three rodent models - the antagonism of reserpine-induced hypothermia, the antagonism of histamine-induced ACTH release, and the ability to reduce noradrenergic responsiveness in the rat pineal gland. An acute effect seen in the rat pineal gland with several analogues, including 1-[1-(3,4-dichlorophenyl)-2-(dimethylamino)ethyl]cyclohexanol (23) and 1-[2-(dimethylamino)-1-(4-methoxyphenyl)ethyl]cyclohexanol (4), was taken as a possible correlate of a rapid onset of antidepressant activity. Compound 4 (venlafaxine) is presently undergoing clinical evaluation.
