- Stereoselective total synthesis of almorexant
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A highly stereoselective synthesis of almorexant has been achieved using (R)-tert-butanesulfinamide as a chiral source. The chiral tetrahydroisoquinoline core was constructed through allylation of chiral N-sulfinyl imine followed by ring closure of the se
- Reddy, N. Siva Senkar,Reddy, B.V. Subba
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p. 3157 - 3159
(2014/05/20)
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- Enantioselective synthesis of almorexant via iridium-catalysed intramolecular allylic amidation
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An enantioselective synthesis of almorexant, a potent antagonist of human orexin receptors, is presented. The chiral tetrahydroisoquinoline core structure was prepared via iridium-catalysed asymmetric intramolecular allylic amidation. Further key catalytic steps of the synthesis include an oxidative Heck reaction at room temperature and a hydrazine-mediated organocatalysed reduction. The Royal Society of Chemistry 2013.
- Fa?anás-Mastral, Martín,Teichert, Johannes F.,Fernández-Salas, José Antonio,Heijnen, Dorus,Feringa, Ben L.
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p. 4521 - 4525
(2013/08/23)
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- PROCESS FOR THE PREPARATION OF AN ENANTIOMERIC TRISUBSTITUTED 3,4-DIHYDRO-ISOQUINOLINE DERIVATIVE
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The present invention relates to a process for the preparation of the compound of formula (7) which process comprises the hydrogenation of the compound of formula (4) using bis[chloro-1,5-cyclooctadiene-iridium], (S)-i-dicyclohexylphosphino-2-[(S)-α-(dime
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Page/Page column 7; 13; 14
(2010/12/29)
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- SOLID FORMS OF ( 2R) -2- { ( IS ) -6, 7 -DIMETHOXY- 1- [2- (4-TRIFLU0R0METHYL-PHENYL) -ETHYL] -3, 4-DIHYDR0-1H -ISOQUINOLIN-2-YL} -N-METHYL-2-PHENYL-ACETAMIDE HYDROCHLORIDE
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The invention relates to hydrated crystalline forms of (2R)-2-{(1 S)-6,7-dimethoxy-1 - [2-(4-thfluoromethyl-phenyl)-ethyl]-3,4-dihydro-1 H-isoquinolin-2-yl}-Λ/-methyl-2- phenyl-acetamide hydrochloride, to the amorphous form of this compound, and to further crystalline forms of this compound, to processes for the preparation thereof, pharmaceutical compositions containing said crystalline forms or said amorphous form, and their use as orexin receptor antagonists.
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Page/Page column 17-18
(2010/09/17)
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- TRISUBSTITUTED 3,4-DIHYDRO-1H-ISOQUINOLIN COMPOUND, PROCESS FOR ITS PREPARATION, AND ITS USE
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The present invention relates to the compound of formula 7*acetate (see below), a process for its preparation, and its use
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Page/Page column 13
(2010/02/17)
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- Tetrahydroisoquinoline Derivatives to Enhance Memory Function
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The invention relates to the use of tetrahydroisoquinoline derivatives for the preparation of a medicament to enhance, maintain and/or restore all stages and/or types of short-, middle- and/or long-term memory.
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- PROCESS FOR THE PREPARATION OF AN ENANTIOMERIC TRISUBSTITUTED 3,4-DIHYDRO-ISOQUINOLINE DERIVATIVE
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The present invention relates to a process for the preparation of the compound of formula (7) which process comprises the hydrogenation of the compound of formula (4) using bis[chloro-1,5-cyclooctadiene-iridium], (S)-i -dicyclohexylphosphino- 2-[(S)-α-(di
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Page/Page column 28
(2009/08/14)
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- TRISUBSTITUTED 3,4-DIHYDRO-1H-ISOQUINOLIN COMPOUND, PROCESS FOR ITS PREPARATION, AND ITS USE
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The present invention relates to the compound of formula (7*)acetate (see below), a process for its preparation, and its use.
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Page/Page column 28
(2009/08/14)
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- SUBSTITUTED 1,2,3,4-TETRAHYDROISOQUINOLINE DERIVATIVES
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The invention relates to novel 1,2,3,4-tetrahydroisoquinoline derivatives of formula (I) wherein R1, R2, R3 and X are as defined in the claims, and their use as active ingredients in the preparation of pharmaceutical compo
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Page/Page column 29
(2010/02/15)
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