- A Borrowing Hydrogen Approach to the Synthesis of RS-67,333
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A new strategy using the borrowing hydrogen methodology to access the 5-HT4R agonist RS-67,333 is presented. Especially, this selective and highly potent ligand of 5-HT4 receptor was obtained quickly and efficiently by catalytic alkylation of a ketone with various alcohols in the presence of a catalytic amount of (Cp?IrCl2)2.
- Carbonnel, Elodie,Alix, Florent,Gembus, Vincent
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p. 2057 - 2062
(2017/04/26)
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- 1-PHENYLALKANONE 5-HT4 RECEPTOR LIGANDS
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The present invention relates to novel 5-HT 4 receptor ligands which are 1-(5-halo-4-aminophenyl) (C 2-6)alkan-1-one derivatives in which the 5-halo-4-aminophenyl group is substituted at its 2-position with (C 1-4)alkyloxy or phenyl(C 1-4)alkyloxy and optionally substituted at its 3-position with (C 1-4)alkyloxy or substituted at its 2-and 3-positions together with methylenedioxy or ethylenedioxy and the highest numbered carbon of the (C 2-6)alkan-1-one is substituted with di(C 1-4)alkylamino, morpholin-1-yl or pyrrolidin-1-yl or optionally substituted piperidin-1-yl, piperidin-4-yl, azacyclohept-1-yl, azabicyclo[2.2.1]hept-3-yl, azabicylo[2.2.2]oct-3-yl or azabicylo[3.2. 2] non-3-yl; and the pharmaceutically acceptable salts, individual isomers and mixtures of isomers and methods of using and making such derivatives.
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