- OXAZOLE OREXIN RECEPTOR ANTAGONISTS
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The present invention is directed to oxazole compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the oxazole compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
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Page/Page column 69; 70
(2015/02/25)
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- OXAZOLE OREXIN RECEPTOR ANTAGONISTS
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The present invention is directed to oxazole compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the oxazole compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
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Page/Page column 80; 81
(2015/02/25)
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- Enantioselective synthesis of anti-β-hydroxy-α-amido esters by asymmetric transfer hydrogenation in emulsions
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Herein, we present two methods for an asymmetric transfer hydrogenation through the dynamic kinetic resolution of α-amido-β-ketoesters. These procedures yield the corresponding anti-β-hydroxy-α-amido esters in good yields and with good diastereo- and enantioselectivities. First, the scope of the reduction of α-amido-β-ketoesters by using triethylammonium formate azeotrope is examined. Then, an emulsion technology with sodium formate is explored, which allows for broader substrate scope, faster reaction times, and lower catalyst loading. Furthermore, these reactions are operationally simple and can be set up in air.
- Seashore-Ludlow, Brinton,Villo, Piret,Somfai, Peter
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supporting information; experimental part
p. 7219 - 7223
(2012/07/13)
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- PROCESS FOR PRODUCING OPTICALLY ACTIVE β-HYDROXY-α-AMINOCARBOXYLIC ACID DERIVATIVE
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[PROBLEMS] To provide a process for efficiently producing the anti isomer of an optically active β-hydroxy-α-aminocarboxylic acid derivative useful as an intermediate for medicines/agricultural chemicals. [MEANS FOR SOLVING PROBLEMS] The process, which is for producing an optically active β-hydroxy-α-aminocarboxylic acid derivative represented by the formula (2) or (3) [Chemical formula 3] (wherein R1 means (un)substituted C1-20 alkyl or an (un)substituted C4-12 aromatic group and R2 means (un)substituted C1-20 alkyl or an (un)substituted C4-12 aromatic group), comprises hydrogenating an α-aminoacylacetic ester compound represented by the formula (1): [Chemical formula 1] [wherein R1 and R2 have the same meanings as defined above] in the presence of an acid through a catalytic asymmetric hydrogenation reaction employing as a catalyst a rhodium complex having as a ligand an optically active compound represented by the formula (4), (4'), or (5): [Chemical formula 2] the process being characterized in that the hydrogenation is conducted in the presence of an acetic acid salt.
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Page/Page column 23-24
(2008/06/13)
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- PROCESS FOR PRODUCTION OF OPTICALLY ACTIVE BETA-HYDROXY- ALPHA-AMINOCARBOXYLIC ACID DERIVATIVES
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There is provided a process for efficiently producing an anti form of an optically active β-hydroxy-α-aminocarboxylic acid derivative that is useful as an intermediate for pharmaceuticals and agrochemicals. The process for producing optically active β-hydroxy-α-aminocarboxylic acid derivative of formula (2) or (3) wherein R1 is substituted or unsubstituted C1-20 alkyl group, or substituted or unsubstituted C4-12 aromatic group, R2 is substituted or unsubstituted C1-20 alkyl group, or substituted or unsubstituted C4-12 aromatic group, characterized by comprising subjecting an α-aminoacyl acetic acid ester compound of formula (1) wherein R1 and R2 have the same meaning as the above, to hydrogenation by catalytic asymmmetric hydrogenation in the presence of an acid.
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Page/Page column 20-21
(2010/11/08)
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- Dynamic kinetic resolution catalyzed by Ir axially chiral phosphine catalyst: Asymmetric synthesis of anti aromatic β-hydroxy-α-amino acid esters
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The anti selective hydrogenation of α-amino-β-keto esters via dynamic kinetic resolution was achieved for the first time by using the iridium-MeOBIPHEP catalyst in asymmetric synthesis of anti aromatic β-hydroxy-α-amino acid esters with excellent diastereo- and enantioslectivities. Acetic acid as a solvent and sodium acetate as an additive affected dramatically the yield and the enantioselectivity, respectively. The product anti aromatic β-hydroxy-α-amino acid esters are useful for synthesis of pharmaceuticals and natural products. Copyright
- Makino, Kazuishi,Hiroki, Yasuhiro,Hamada, Yasumasa
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p. 5784 - 5785
(2007/10/03)
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- Nonionic superbase-promoted synthesis of oxazoles and pyrroles: Facile synthesis of porphyrins and α-C-acyl amino acid esters
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The reaction of acyl chlorides or acid anhydrides with isocyanoacetates in the presence of the superior strong nonionic base P(MeNCH2CH2)3N (1) gave oxazoles in 98-99% yield. Treatment of the oxazoles with HCl-MeOH gave α-
- Tang,Verkade
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p. 7793 - 7802
(2007/10/02)
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- An efficient synthesis and acylation of α-amino-β-keto-esters: Versatile intermediates in the synthesis of peptide mimetics
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A flexible and high yield synthesis of α-amino-β-keto esters has been developed via acylation of the ketimine derivatives of α-amino esters. These α-amino-β-keto-esters were acylated with chiral amino acid derivatives in 36-95% yields.
- Singh, Jasbir,Gordon, Thomas D.,Earley, William G.,Morgan, Barry A.
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p. 211 - 214
(2007/10/02)
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