14490-45-0Relevant academic research and scientific papers
POLYCYCLIC AMINES AS OPIOID RECEPTOR MODULATORS
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, (2018/10/11)
The present invention provides a genus of polycyclic amines that are useful as opioid receptor modulators. The compounds of the invention are useful in both therapeutic and diagnostic methods, including for treating pain, neurological disorders, cardiac disorders, bowel disorders, drug and alcohol addiction, drug overdose, urinary disorders, respiratory disorders, sexual dysfunction, psoriasis, graft rejection or cancer.
Palladium on Carbon-Catalyzed Chemoselective Oxygen Oxidation of Aromatic Acetals
Yasukawa, Naoki,Asai, Shota,Kato, Maho,Monguchi, Yasunari,Sajiki, Hironao,Sawama, Yoshinari
, p. 5604 - 5607 (2016/11/17)
The development of an unprecedented chemoselective transformation has contributed to forming a novel synthetic process for target molecules. Chemoselective oxidation of aromatic acetals has been accomplished using a reusable palladium on carbon catalyst under atmospheric oxygen conditions to form ester derivatives with tolerance of aliphatic acetals and ketals.
Reductive carbonylation of aryl halides employing a two-chamber reactor: A protocol for the synthesis of aryl aldehydes including 13C- and D-isotope labeling
Korsager, Signe,Taaning, Rolf H.,Lindhardt, Anders T.,Skrydstrup, Troels
, p. 6112 - 6120 (2013/07/26)
A protocol has been developed for conducting the palladium-catalyzed reductive carbonylation of aryl iodides and bromides using 9-methylfluorene-9- carbonyl chloride (COgen) as a source of externally delivered carbon monoxide in a sealed two-chamber system (COware), and potassium formate as the in situ hydride source. The method is tolerant to a wide number of functional groups positioned on the aromatic ring, and it can be exploited for the isotope labeling of the aldehyde group. Hence, reductive carbonylations run with 13COgen provide a facile access to 13C-labeled aromatic aldehydes, whereas with DCO2K, the aldehyde is specifically labeled with deuterium. Two examples of double isotopic labeling are also demonstrated. Finally, the method was applied to the specific carbon-13 labeling of the β-amyloid binding compound, florbetaben.
Palladium-catalysed direct regioselective synthesis of cyclic ketals from electron-rich olefins and aryl bromides in ionic liquids
Hyder, Zeynab,Mo, Jun,Xiao, Jianliang
, p. 1699 - 1704 (2007/10/03)
The Heck reaction comprises one of the most important carbon-carbon coupling reactions in organic synthesis. The popularity of the reaction is attributable to the broad availability of aryl halides and to the tolerance of the reaction for a wide variety o
Direct synthesis of protected arylacetaldehydes by tetrakis(phosphane)- palladium-catalyzed arylation of ethyleneglycol vinyl ether
Kondolff, Isabelle,Doucet, Henri,Santelli, Maurice
, p. 765 - 774 (2007/10/03)
A range of aryl bromides undergo Heck reaction with ethylene glycol vinyl ether, in the presence of [PdCl(C3H5)]2/ cis,cis,cis-1,2,3,4-tetrakis[(diphenylphosphanyl)methyl]cyclopentane as catalyst, to give regioselectively protected arylacetaldehydes in good yields. The β-arylation products were obtained in with 93-100 % selectivity with electron-poor aryl bromides or heteroaryl bromides. Furthermore, this catalyst can be used at low loading, even for reactions with sterically hindered aryl bromides. The aryl vinyl ether intermediates undergo subsequent ketalisation to give the corresponding 2-benzyl-1,3-dioxolane derivatives. Wiley-VCH Verlag GmbH & Co. KGaA, 2006.
Direct synthesis of protected arylacetaldehydes by palladium- tetraphosphine-catalyzed arylation of ethyleneglycol vinylether
Kondolff, Isabelle,Doucet, Henri,Santelli, Maurice
, p. 1561 - 1564 (2007/10/03)
Through the use of [PdCl(C3H5)]2/cis,cis, cis-1,2,3,4-tetrakis(diphenylphosphinomethyl) cyclopentane as a catalyst, a range of aryl bromides undergo Heck reaction with ethyleneglycol vinylether to give regioselectively protected arylacetaldehydes in good yields. The β-arylation products were obtained in the range 93-98% selectivity with electron-poor aryl bromides. Furthermore, this catalyst can be used at low loading, even for reactions of sterically hindered aryl bromides. The arylvinyl ethers intermediates undergo subsequent ketalization to give the corresponding 2-benzyl-1,3-dioxolane derivatives.
Convergence of absorption and fluorescence in cross-conjugated oligomers consisting of chalcone building blocks
Meier, Herbert,Aust, Harald,Ickenroth, Dirk,Kolshorn, Heinz
, p. 529 - 535 (2007/10/03)
The absorption and fluorescence spectra of two series of chalcone oligomers (1a-d) and (2a-d) are reported. Due to small or vanishing orbital coefficients (HMO calculation) within the cross-conjugated systems, the bathochromic shifts caused by the extensi
Synthesis of novel oximes of 2-aryl-6-methoxy-3,4-dihydronaphthalene and their evaluation as inhibitors of 17α-hydroxylase-C17,20-lyase (P450 17)
Zhuang, Yan,Hartmann, Rolf W.
, p. 36 - 40 (2007/10/03)
The synthesis and biological evaluation of oximes of 2-aryl-6-methoxy-3,4-dihydronaphthalene (7a, 7b, 14a, 14b) as nonsteroidal inhibitors of 17α-hydroxylase-C17,20-lyase (P450 17, CYP 17) is described. The target compounds were synthesized and identified
Ester derivatives and pharmaceutical compositions containing them
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, (2008/06/13)
The invention concerns ester derivatives of the formula I wherein Ar is phenyl, naphthyl, indenyl, indanyl, a 10-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from
OXIME DERIVATIVES
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, (2008/06/13)
The invention concerns oxime derivatives of the formula I wherein R4 includes hydrogen, carboxy, carbamoyl, amino, cyano, trifluoromethyl, (1-4C)alkylamino, di(1-4C)alkylamino and (1-4C)alkyl; RS includes hydrogen, (1-4C)alkyl, (3-4C)alkeny1,(3-4C)alkynyl, (2-5C)alkanoyl, halogeno-(2-4-C)alkyl and hydroxy-(2-4C)alky1;Arl is phenylene or a hetercaryl diradical; Al is a direct link to XI, or Al is (1-4C)alkylene; XI is oxy, thio, sulphinyl or sulphonyl; Ar2 is phenylene or a heteroaryl diradical; RI is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkyny1; and R2 and R3 together form a group of the formula -A2. X2-A3- which together with the carbon atom to which A2 and A3 are attached define a ring having 5 or 6 ring atoms, wherein each of A2 and A3 is (1-3C)alkylene and X2 is oxy, thio, sulphinyl, sulphonyl or imino; or a pharmaceutically-acceptable sah thereof; processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.
