245510-06-9Relevant articles and documents
Nucleophilic Substitutions of Alcohols in High Levels of Catalytic Efficiency
Stach, Tanja,Dr?ger, Julia,Huy, Peter H.
supporting information, p. 2980 - 2983 (2018/05/28)
A practical method for the nucleophilic substitution (SN) of alcohols furnishing alkyl chlorides, bromides, and iodides under stereochemical inversion in high catalytic efficacy is introduced. The fusion of diethylcyclopropenone as a simple Lewis base organocatalyst and benzoyl chloride as a reagent allows notable turnover numbers up to 100. Moreover, the use of plain acetyl chloride as a stoichiometric promotor in an invertive SN-type transformation is demonstrated for the first time. The operationally straightforward protocol exhibits high levels of stereoselectivity and scalability and tolerates a variety of functional groups.
ALKOXY COMPOUNDS FOR DISEASE TREATMENT
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Page/Page column 231, (2009/05/29)
The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.
NEW CHEMICAL COMPOUNDS
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Page/Page column 86-87, (2008/12/08)
The present invention provides compounds of formula (I) having muscarinic M3 receptor and β-adrenergic receptor modulating activity; processes for their preparation and their use in therapy; wherein A, R1, R2, R3 and Rsup
A practical synthesis of enantiopure 7-alkoxy-4-aryl- tetrahydroisoquinoline, a dual serotonin reuptake inhibitor/histamine H 3 antagonist
Deng, Xiaohu,Liang, Jimmy T.,Liu, Jing,McAllister, Heather,Schubert, Garsten,Mani, Neelakandha S.
, p. 1043 - 1050 (2012/12/30)
An efficient synthesis of compound 1 featuring a novel sequential Friedel-Crafts alkylation strategy to construct the 4-aryl- tetrahydroisoquinoline core structure has been developed. Resolution with (D/L)-di-p-toluoyl-tartaric acid is utilized to provide the enantiomerically pure material. Overall, the route is concise and amenable for large-scale synthesis.
Dual serotonin transporter/histamine H3 ligands: Optimization of the H3 pharmacophore
Keith, John M.,Gomez, Leslie A.,Letavic, Michael A.,Ly, Kiev S.,Jablonowski, Jill A.,Seierstad, Mark,Barbier, Ann J.,Wilson, Sandy J.,Boggs, Jamin D.,Fraser, Ian C.,Mazur, Curt,Lovenberg, Timothy W.,Carruthers, Nicholas I.
, p. 702 - 706 (2007/10/03)
A series of tetrahydroisoquinolines acting as dual histamine H3/serotonin transporter ligands is described. A highly regio-selective synthesis of the tetrahydroisoquinoline core involving acid mediated ring-closure of an acetophenone intermediate followed by reduction with NaCNBH3 was developed. In vitro and in vivo data are discussed.
Novel tetrahydroisoquinolines are histamine H3 antagonists and serotonin reuptake inhibitors
Letavic, Michael A.,Keith, John M.,Jablonowski, Jill A.,Stocking, Emily M.,Gomez, Leslie A.,Ly, Kiev S.,Miller, Jennifer M.,Barbier, Ann J.,Bonaventure, Pascal,Boggs, Jamin D.,Wilson, Sandy J.,Miller, Kirsten L.,Lord, Brian,McAllister, Heather M.,Tognarelli,Wu, Jiejun,Abad, Marta C.,Schubert, Carsten,Lovenberg, Timothy W.,Carruthers, Nicholas I.
, p. 1047 - 1051 (2007/10/03)
A series of novel 4-aryl-1,2,3,4-tetrahydroisoquinoline-based histamine H3 ligands that also have serotonin reuptake transporter inhibitor activity is described. The synthesis, in vitro biological data, and select pharmacokinetic data for these novel compounds are discussed.
TETRAHYDROISOQUINOLINE COMPOUNDS FOR TREATMENT OF CNS DISORDERS
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Page/Page column 53-54, (2010/11/08)
Certain tetrahydroisoquinoline compounds are histamine H3 receptor and serotonin transporter modulators useful in the treatment of histamine H3 receptor-and serotonin-mediated diseases.
MESO-SUBSTITUTED PORPHYRINS
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Page 29-30, (2010/02/07)
Meso-substituted porphyrins of general formula (I) suitable for the use as photosensitising agents, in particular in photodynamic therapy, are herein described.