- Development of an enantioselective, kilogram-scale, rhodium-catalysed 1,4-addition
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A rhodium-catalysed 1,4-addition of an arylboron species to an α,β-unsaturated ester was the key chirality-inducing step in the synthesis of an API. We describe herein the development of this chemistry, including optimization of reagent charges, reaction
- Brock, Sally,Hose, David R.J.,Moseley, Jonathan D.,Parker, Alexandra J.,Patel, Ian,Williams, Andrew J.
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p. 496 - 502
(2013/01/03)
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- Chemical Compound
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The present invention relates to 4-[3-(1,1-difluoroethyl)-5-methyl-4H-1,2,4-triazol-4-yl]-1-{(1R,3R)-3-(3,5-difluorophenyl)-1-methyl-3-[1-(methylsulfonyl)piperidin-4-yl]propyl}piperidine (I): or a pharmaceutically acceptable salt thereof, as well as processes for the preparation of this compound and its use in the treatment of CCR5 disease states.
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Page/Page column 9
(2008/12/06)
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- Chemical Compound
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The present invention relates to 4-{(1R,3R)-1-(3,5-difluorophenyl)-3-[4-(3-ethyl-5-isopropyl-4H-1,2,4-triazol-4-yl)piperidin-1-yl]butyl}-1-(methylsulfonyl)piperidine (I): or a pharmaceutically acceptable salt thereof, as well as to processes for preparing
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Page/Page column 9
(2008/12/06)
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- PROCESS FOR PREPARING BETA- (FLUOROPHENYL) -PROPANOATE ESTER DERIVATIVES
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A process for preparing a compound of formula (I) comprising reacting a compound of formula (II) with a fluorinated boron species of formula (III) in the presence of: an alcohol; a rhodium (I) pre-catalyst species; a suitable ligand that binds to the rhodium (I) pre-catalyst species to form a catalyst complex; a base; and, a suitable solvent; the process being carried out at a temperature in the range 40 to 110oC. The compounds of formula (I) are useful in the preparation of pharmaceutically active compounds.
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Page/Page column 13-14
(2008/06/13)
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- PIPERIDINE OR 8-AZA-BICYCLO[3.2.1]OCT-3-YL DERIVATIVES USEFUL AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
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Compounds of formula (I): wherein R1, R2, R3, R4, A and n are as defined; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activit
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- PIPERIDINE DERIVATIVES AS CCR5 RECEPTOR MODULATORS
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Compounds of formula (I) wherein R1, R2, R3, A and n are as defined; and X is S(O)2 NR4R5 or NR6S(O)2R7; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).
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- NOVEL PIPERIDINE DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR CCR5
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Compounds of formula (I) wherein R1, R2, R3, R4, A, X, m and n are as defined; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).
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