- Novel synthesis method for ortho-alkane superseded pyridine
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The invention relates to a novel synthesis method for ortho-alkane superseded pyridine. According to the method, ortho halogenated pyridine serves as raw materials, the ortho halogenated pyridine and corresponding alcohol react to obtain the ortho-alkane superseded pyridine under the action of sodium hydroxide. The reaction has universality for the ortho halogenated pyridine, and the method is simple and practical. Influence of consumption of the sodium hydroxide on mono-substitution and di-substitution in the reaction is inspected, alkoxy mono-substitution products and alkoxy di-substitution production are acquired, and a novel simply-operated, economical and favorable process for synthesis ortho-alkane superseded pyridine is provided.
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Paragraph 0018; 0019; 0020; 0021
(2017/07/19)
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- A new synthesis of pyridinyl trifluoromethanesulfonates via one-pot diazotization of aminopyridines in the presence of trifluoromethanesulfonic acid
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The first method for the direct one-pot transformation of aminopyridines into pyridinyl trifluoromethanesulfonates is developed. The procedure involves diazotization of aminopyridines with sodium nitrite in a DMSO paste in the presence of trifluoromethanesulfonic acid.
- Krasnokutskaya, Elena A.,Kassanova, Assiya Zh.,Estaeva, Makpal T.,Filimonov, Victor D.
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p. 3771 - 3773
(2014/07/07)
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- PYRROLIDINONE DERIVATIVES AS GPR119 MODULATORS FOR THE TREATMENT OF DIABETES, OBESITY, DYSLIPIDEMIA AND RELATED DISORDERS
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The present invention relates to pyrrolidinone derivatives of formula (I). The pyrrolidinone derivatives of formula (I) are GPR119 modulators and useful for the prevention and/or treatment of diabetes, obesity, dyslipidemia and related disorders. The invention furthermore relates to the use of pyrrolidinone derivatives as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
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Page/Page column 45; 67
(2014/05/07)
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- Inverse electron demand diels-alder reactions of 1,2,3-triazines: Pronounced substituent effects on reactivity and cycloaddition scope
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A systematic study of the inverse electron demand Diels-Alder reactions of 1,2,3-triazines is disclosed, including an examination of the impact of a C5 substituent. Such substituents were found to exhibit a remarkable impact on the cycloaddition reactivity of the 1,2,3-triazine without altering, and perhaps even enhancing, the intrinsic cycloaddition regioselectivity. The study revealed not only that the reactivity may be predictably modulated by a C5 substituent (R = CO2Me > Ph > H) but also that the impact is of a magnitude to convert 1,2,3-triazine (1) and its modest cycloaddition scope into a heterocyclic azadiene system with a reaction scope that portends extensive synthetic utility, expanding the range of participating dienophiles. Significantly, the studies define a now powerful additional heterocyclic azadiene, complementary to the isomeric 1,2,4-triazines and 1,3,5-triazines, capable of dependable participation in inverse electron demand Diels-Alder reactions, extending the number of complementary heterocyclic ring systems accessible with implementation of the methodology.
- Anderson, Erin D.,Boger, Dale L.
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supporting information; experimental part
p. 12285 - 12292
(2011/09/16)
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- PHOSPHATIDYLINOSITOL 3 KINASE INHIBITORS
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Provided are compounds according to Formula (I), or stereoisomer, prodrug, polymorph, or pharmaceutically acceptable salt forms thereof, wherein X, Y, R1, R6 , R7, and R8 are as defined, which compounds are effective inhibitors of PI3-kinase and/or other medically and clinically relevant kinases. Also provided are pharmaceutical compositions and methods of using the compounds and compositions as PB -kinase and kinase inhibitors. More particularly, the compounds of the invention provide treatments and therapeutics for human diseases regulated by, or associated with, the activity of, PI3-kinases and/or protein kinases, or mutant or variant forms thereof.
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Page/Page column 127
(2010/01/12)
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- Pyridyl piperazines for the treatment of CNS disorders
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This invention is directed to compounds of Formula I and to pharmaceutical compositions comprising the compound of Formula I. where the dashed line represents an optional double bond; and where n is 1 or 2, and Ar1, Ar2, . . . and Z
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Page/Page column 15
(2010/02/15)
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- PYRIDIL-LACTAMS AND THEIR USE 5 -HTl RECEPTORS LIGAN
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The present invention relates to novel pyridyl-lactams, compounds of the formula (I), wherein R1 is a group of the formula G1, G2, G3 or G4 depicted below, and R3, Y, R6, R7, R8, R13, a, n and m are as defined herein, their pharmaceutically acceptable salts, pharmaceutical compositions, their preparation and intermediates therefrom, and their use in treating or preventing depression, anxiety, obsessive compulsive disorder (OCD) and other disorders for which a 5-HT1B antagonist is indicated.
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Page/Page column 36
(2010/11/24)
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- Alpha V integrin receptor antagonists
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The present invention relates to novel imidazolidinone derivatives thereof, their synthesis, and their use as αv integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors αvβ3 and/or
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