148775-22-8Relevant academic research and scientific papers
The design and synthesis of novel NK1/NK2 dual antagonists
Reichard, Gregory A.,Ball, Zachary T.,Aslanian, Robert,Anthes, John C.,Shih, Neng-Yang,Piwinski, John J.
, p. 2329 - 2332 (2000)
Functional probing of the backbone of the Sanofi NK2 antagonist SR 48968 has resulted in the discovery of two new classes of NK1/NK2 dual antagonists: the diamine class and the oxime class. The addition of the amino or the oxime functional group results in the reversal of the stereochemical preference of the NK2 receptor. (C) 2000 Elsevier Science Ltd.
Hydroamination versus Allylic Amination in Iridium-Catalyzed Reactions of Allylic Acetates with Amines: 1,3-Aminoalcohols via Ester-Directed Regioselectivity
Kim, Seung Wook,Wurm, Thomas,Brito, Gilmar A.,Jung, Woo-Ok,Zbieg, Jason R.,Stivala, Craig E.,Krische, Michael J.
supporting information, p. 9087 - 9090 (2018/08/03)
In the presence of a neutral dppf-modified iridium catalyst and Cs2CO3, linear allylic acetates react with primary amines to form products of hydroamination with complete 1,3-regioselectivity. The collective data, including deuterium labeling studies, corroborate a catalytic mechanism involving rapid, reversible acetate-directed aminoiridation with inner-sphere/outer-sphere crossover followed by turnover-limiting proto-demetalation mediated by amine.
Dialkylzinc-mediated allylic polyfluoroarylation reaction
Kurauchi, Daisuke,Hirano, Keiichi,Kato, Hisano,Saito, Tatsuo,Miyamoto, Kazunori,Uchiyama, Masanobu
supporting information, p. 5849 - 5857 (2015/08/03)
Abstract We present an allylic polyfluoroarylation reaction with broad substrate scope and excellent functional group tolerance, using organozinc reagents under mild conditions. A catalytic amount of triphenylphosphine oxide efficiently promotes iodine-zinc exchange reaction between polyfluoroaryl iodide and dimethylzinc, and the resulting phosphine oxide-activated polyfluoroarylzinc undergoes substitution reaction with allylic halides to afford the corresponding polyfluoroarylated products.
Organocatalytic asymmetric cyanation of isatin derived N-Boc ketoimines
Liu, Yun-Lin,Zhou, Jian
supporting information, p. 4421 - 4423 (2013/06/05)
We report the first catalytic asymmetric cyanation of N-Boc ketoimines, which enables highly enantioselective synthesis of oxindole based α-amino nitriles. An unprecedented tandem aza-Wittig/Strecker reaction is also developed, emerging as a promising strategy for the catalytic asymmetric cyanation of ketoimines formed in situ from achiral ketones.
USE OF SPIRO [ IMIDAZOLIDINE-4, 3'-INDOLE] 2, 2', 5' (1H) TRIONES FOR TREATMENT OF CONDITIONS ASSOCIATED WITH VANILLOID RECEPTOR 1
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Page/Page column 18; 24, (2008/06/13)
The present invention relates to a new use of spiro-hydantoin derivatives of formula (I), or salts, solvates or solvated salts thereof, as well as to new compounds, a process for their preparation and new intermediates used in the preparation thereof, pha
NEW COMPOUNDS I
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Page/Page column 28, (2008/06/13)
The present invention relates to new compounds of formula (I), wherein R1 to R9 and X are as defined as in formula I, or salts, solvates or solvated salts thereof, processes for their preparation and to new intermediates used in the
SUBSTITUTED ARYLALKYLAMINES AS NEUROKININ ANTAGONISTS
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, (2008/06/13)
Aralkylamine derivatives of formula (I) and their salts are new: A1 = CH2R6, OR6, NR6R7, SOeR13, (CR6R7)qOR6, (CR6R7)qNR6R7 or (CR6R7)qSOeR13; q = 1-6; A2 = H; or A1+A2 = O, CR6R7, NOR6 or S; Q = R5-phenyl, R5-naphthyl, SR6, NR6R7, OR6 or R5-heteroaryl; T
Synthesis, modelling, and μ-opioid receptor affinity of N-3(9)-arylpropenyl-N-9(3)-propionyl-3,9-diazabicyclo[3.3.1]nonanes
Pinna,Murineddu,Curzu,Villa,Vianello,Borea,Gessi,Toma,Colombo,Cignarella
, p. 553 - 562 (2007/10/03)
A series of N-3-arylpropenyl-N-9-propionyl-3,9-diazabicyclo[3.3.1]nonanes (1a-g) and of reverted N-3-propionyl-N-9-arylpropenyl isomers (2a-g), as homologues of the previously reported analgesic 3,8-diazabicyclo[3.2.1]octanes (I-II), were synthesized and evaluated for the binding affinity towards opioid receptor subtypes μ, δ and κ. Compounds 1a-g and 2a-g exhibited a strong selective μ-affinity with Ki values in the nanomolar range, which favourably compared with those of I and II. In addition, contrary to the trend observed for DBO-I, II, the μ-affinity of series 2 is markedly higher than that of the isomeric series 1. This aspect was discussed on the basis of the conformational studies performed on DBN which allowed hypotheses on the mode of interaction of these compounds with the μ receptor.
SUBSTITUTED OXIMES, HYDRAZONES AND OLEFINS AS NEUROKININ ANTAGONISTS
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, (2008/06/13)
Compound represented by the structural formula STR1 or a pharmaceutically acceptable salt thereof, wherein: a is 0, 1, 2 or3; b, d and e are independently 0, 1 or 2;R is H, C 1-6 alkyl,--OH or C 2-C 6 hydroxyalkyl;A is an optionally su
