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.
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
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.
