84815-20-3Relevant academic research and scientific papers
Palladium-Catalyzed Reductive Carbonylation of (Hetero) Aryl Halides and Triflates Using Cobalt Carbonyl as CO Source
Dogga, Bhushanarao,Joseph, Jayan T.,Kumar, C. S. Ananda
supporting information, p. 309 - 313 (2020/12/23)
An efficient protocol for the reductive carbonylation of (hetero) aryl halides and triflates under CO gas-free conditions using Pd/Co2(CO)8 and triethylsilane has been developed. The mild reaction conditions, enhanced chemoselectivity and, easy access to heterocyclic and vinyl carboxaldehydes highlights its importance in organic synthesis.
Convenient method for the preparation of the 2-methyl thiophen-3-yl magnesium bromide lithium chloride complex and its application to the synthesis of 3-substituted 2-methylthiophenes
Kogami, Masakazu,Watanabe, Nobuhide
, p. 681 - 688 (2013/01/15)
Lithium chloride was found to accelerate formation of the Grignard reagent from inactive 3-bromo-2-methylthiophene (1) and commercial magnesium metal. Based on this finding, a convenient and potentially scalable preparation of ethyl 2-methylthiophene-3-ca
NOVEL INDOLE AND PYRROLOPYRIDINE AMIDES
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Page/Page column 56, (2012/09/11)
The present invention relates to indole and pyrrolopyridine amide derivatives of formula (I) wherein R1, R 2, R 3, U, V, W, X, Y, Z and ring A are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as orexin receptor antagonists.
Antiinflammation agents
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Page/Page column 33, (2010/02/06)
Compounds, compositions and methods that are useful in the treatment of inflammatory, immunoregulatory, metabolic, infectious and cell proliferative diseases or conditions are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in inflammation, metabolism, infection and cell proliferation. The subject compounds contain a fused heterobicyclic ring.
Fused pyridine derivatives
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Example 284, (2010/01/30)
The present provides a condensed pyridine compound (I) represented by the following formula: (wherein, R2represents ring A represents benzene ring, pyridine ring, thiophene ring or furan ring; and B represents its pharmaceutically acceptable salt or hydrates thereof, which is a clinically useful medicament having a serotonin antagonism, in particular, that for treating, ameliorating or preventing spastic paralysis or central muscle relaxants for ameliorating myotonia.
α2 adrenoceptor agonists as potential analgesic agents. 3. Imidazolylmethylthiophenes
Boyd,Rasmussen,Press,Raffa,Codd,Connelly,Li,Martinez,Lewis,Almond,Reitz
, p. 863 - 872 (2007/10/03)
A series of imidazolylmethylthiophenes has been prepared and evaluated as ligands for the α2 adrenoceptor. These compounds were tested in two animal models that are predictive of analgesic activity in humans. The 3-thienyl compounds were generally the most potent, particularly those with substitution in the 4-position. A subset of the most active compounds was further evaluated for adverse cardiovascular effects in the anesthetized rat model. In addition to excellent binding at the α2D adrenoceptor, the 4-bromo analogues 20e and 21e were very active in the rat abdominal irritant test (RAIT) with ED50 doses of 0.38 and 0.31 mg/kg, respectively. We constructed a pharmacophore model based on the biological activity of the present series, dexmedetomidine (1), and conformationally restrained analogues 3 and 4.
4-?(thien-3-yl)methyl!-imidazole analgesics
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, (2008/06/13)
Described herein are 4-?(thien-3-yl)methyl!-imidazoles of the formula: STR1 wherein R is hydrogen or methyl, and X is C1-4 alkyl, bromine or chlorine; or STR2 wherein Y is hydrogen, C1-4 alkyl, bromine or chlorine, and Z is C1-4
Lithiation of Heterocycles Directed by α-Amino Alkoxides
Comins, Daniel L.,Killpack, Michael O.
, p. 104 - 109 (2007/10/02)
The addition of heterocyclic aromatic aldehydes to certain lithium dialkylamides gave α-amino alkoxides that were ring-lithiated with butyllithium.Alkylation and hydrolysis provided ring-substituted heterocyclic aromatic aldehydes via a one-pot reaction.The metalation of α-amino alkoxides derived from thiophenecarboxaldehydes, furaldehydes, N-methylpyrrolecarboxaldehydes, and indolecarboxaldehydes was examined.The regioselectivity of the lithiation, was dependent on the heterocycle, the amine component of the α-amino alkoxide, and the metalation conditions.A novel N-methyl metalation of α-amino alkoxides derived from N-methylpyrrole-2-carboxaldehyde and N-methylindole-2-carboxaldehyde was achieved when N,N,N'-trimethylethylenediamine was used as the amine component for in situ formation of the α-amino alkoxides.The novel directed N-methyl lithiations are attributed to an intramolecular TMEDA-like assisted metalation.
