- SUBSTITUTED PYRIDINYL-PYRIMIDINES AND THEIR USE AS MEDICAMENTS
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The invention relates to new substituted pyridinyl-pyrimidines of formula 1 wherein ring A is a five-membered saturated or unsaturated carbocyclic ring which optionally comprises one, two or three heteroatoms each independently from each other selected from the group N, S and O, wherein R1, R2, R4, R3, R5 and R6 are defined as in claim 1 and wherein ring A is further optionally substituted by one or two further substituents and the pharmaceutically acceptable salts, diastereomers, enantiomers, racemates, hydrates and solvates of the aforementioned compounds.
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Paragraph 0322; 0325-0326
(2013/03/26)
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- SUBSTITUTED PYRIDINYL-PYRIMIDINES AND THEIR USE AS MEDICAMENTS
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The invention relates to new substituted pyridinyl-pyrimidines of formula 1 wherein ring A is a five-membered saturated or unsaturated carbocyclic ring which optionally comprises one, two or three heteroatoms each independently from each other selected from the group N, S and O, wherein R1, R2, R4, R3, R5 and R6 are defined as in claim 1 and wherein ring A is further optionally substituted by one or two further substituents and the pharmaceutically acceptable salts, diastereomers, enantiomers, racemates, hydrates and solvates of the aforementioned compounds.
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Page/Page column 108; 109
(2012/08/08)
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- 4,4′-Disubstituted L-prolines as highly enantioselective catalysts for direct aldol reactions
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A new series of 4,4′-disubstituted prolines (1a-h) has been developed and tested as organocatalysts in the direct catalytic asymmetric aldol reaction of several aliphatic ketones with aldehydes. Catalyst 1g affords the best enantioselectivities for this transformation. The reaction was carried out in DMF using a catalyst loading of 10 mol% at -10°C to give the aldol products in up to 97% ee for acetone. In the cases of cyclohexanone and cyclopentanone, the corresponding anti-products were obtained in 94% ee.
- Gu, Liuqun,Yu, Menglong,Wu, Xiaoyu,Zhang, Yazhu,Zhao, Gang
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p. 2223 - 2228
(2007/10/03)
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- Synthesis and utility of the 3,3-dimethyl-5-substituted-2-pyrrolidinone 'Quat' chiral auxiliary
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The synthesis and utility of the 3,3-dimethyl-5-substituted-2-pyrrolidinone 'Quat' chiral auxiliary in stereoselective enolate reactions of attached N-acyl side chains combined with the mild and non-racemising conditions required for the ultimate removal of the chiral side chain is described.
- Davies, Stephen G.,Dixon, Darren J.,Doisneau, Gilles J.-M.,Prodger, Jeremy C.,Sanganee, Hitesh J.
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p. 647 - 658
(2007/10/03)
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- Synthesis of 5-substituted-3,3-dimethyl-2-pyrrolidinones: "Quat" chiral auxiliaries
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The synthesis of a series of chiral auxiliaries, 5-substituted-3,3-dimethyl-2-pyrrolidinones, "quats", from L-glutamic acid is described. Efficient regeneration of the chiral auxiliaries from their N-pivaloyl derivatives is readily achieved with LiOH in THF-water at 20°C.
- Davies, Stephen G.,Doisneau, Gilles J. -M.,Prodger, Jeremy C.,Sanganee, Hitesh J.
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p. 2369 - 2372
(2007/10/02)
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