- Method for preparing chiral nitrogen-phosphorus ligand L-8 containing pyridocyclopentane
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The invention discloses a method for preparing chiral nitrogen-phosphorus ligand L-8 containing pyridocyclopentane, and belongs to the technical field of medical intermediate chiral ligands. The chiral nitrogen-phosphorus L-8 ligand is prepared from cyclopentanone through the steps of addition, cyclization, chlorination, asymmetric boronation, oxidation, coupling, esterification and the like in sequence, large-scale preparation is relatively easy to achieve through the route, and the defect that in a traditional route, the yield is low in the first step of ring closing reaction and chiral alcohol preparation is overcome, and by selecting a proper chiral ligand, and combining with butyl lithium, asymmetric synthesis of chiral alcohol is realized, and a chiral separation column mode adoptedin literature is avoided.
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- Method for synthesizing chiral nitrogen-phosphorus ligand L-8 containing pyridocycloheptane
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The invention discloses a method for synthesizing a chiral nitrogen-phosphorus ligand L-8 containing pyridocycloheptane, and belongs to the technical field of medical intermediate chiral ligands. Thechiral nitrogen-phosphorus L-8 ligand is prepared from cyclopentanone through the steps of addition, cyclization, chlorination, asymmetric boronation, oxidation, coupling, esterification and the likein sequence, large-scale preparation is relatively easy to achieve through the route, and the defect that in a traditional route, the yield is low in the first step of ring closing reaction and chiralalcohol preparation, and by selecting a proper chiral ligand, and combining with butyl lithium, asymmetric synthesis of chiral alcohol is realized, and a chiral separation column mode adopted in literature is avoided.
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- SUBSTITUTED L,2-DIHYDRO-3H-PYRAZOLO[3,4-D]PYRIMIDIN-3-ONES
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Compounds of Formula (I) are provided herein. Such compounds, as well as pharmaceutically acceptable salts and compositions thereof, are useful for treating diseases or conditions, including conditions characterized by excessive cellular proliferation, such as breast cancer.
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Paragraph 0156
(2019/10/01)
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- GHRELIN O-ACYLTRANSFERASE INHIBITORS
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This invention relates to novel compounds according to Formula (I) which are inhibitors of ghrelin O-acyltransferase (GOAT), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment
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Page/Page column 64; 65
(2019/08/26)
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- Ligand-Enabled β-C–H Arylation of α-Amino Acids Without Installing Exogenous Directing Groups
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Herein we report acid-directed β-C(sp3)-H arylation of α-amino acids enabled by pyridine-type ligands. This reaction does not require the installation of an exogenous directing group, is scalable, and enables the preparation of Fmoc-protected unnatural amino acids in three steps. The pyridine-type ligands are crucial for the development of this new C(sp3)-H arylation.
- Chen, Gang,Zhuang, Zhe,Li, Gen-Cheng,Saint-Denis, Tyler G.,Hsiao, Yi,Joe, Candice L.,Yu, Jin-Quan
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p. 1506 - 1509
(2017/02/05)
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- ANTI-FIBROTIC PYRIDINONES
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This application relates to polycyclic compounds with a pyridinone or pyridinone derivative core including, substituted pyridinones, 5,6- and 6,6- bicyclic heterocycles and substituted pyridine-thiones. This application also discloses methods of preparing these polycyclic compounds, pharmaceutical compositions and medicaments comprising said compounds and methods to treat, prevent or diagnose diseases, disorders or conditions associated with fibrosis.
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Paragraph 0339
(2015/11/02)
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- ANTI-FIBROTIC PYRIDINONES
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Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.
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Paragraph 0586; 0589
(2014/04/17)
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- Design and synthesis of orally-active and selective azaindane 5HT2c agonist for the treatment of obesity
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Based on our original pyrazine hit, CP-0809101, novel conformationally-restricted 5HT2c receptor agonists with 2-piperazin-azaindane scaffold were designed. Synthesis and structure-activity relationship (SAR) studies are described with emphasis on optimization of the selectivity against 5HT2a and 5HT2b receptors with excellent 2c potency. Orally-active and selective compounds were identified with dose-responsive in vivo efficacy in our pre-clinical food intake model.
- Liu, Kevin K.-C.,Cornelius, Peter,Patterson, Terrell A.,Zeng, Yuan,Santucci, Stephanie,Tomlinson, Elizabeth,Gibbons, Colleen,Maurer, Tristan S.,Marala, Ravi,Brown, Janice,Kong, Jimmy X.,Lee, Eunsun,Werner, Wendy,Wenzel, Zane,Vage, Chandra
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scheme or table
p. 266 - 271
(2010/04/24)
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- Construction of 5,6-ring-fused 2-pyridones: An effective annulation tactic achieved in water
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An efficient protocol to annulate the 5,6-fused 2-pyridone ring system, exploiting a tandem condensation of propiol-amide and cyclic -keto methyl esters in water, followed by acid- or base-promoted intramolecular ring closure and decarboxylation, has been
- Smith III, Amos B.,Atasoylu, Onur,Beshoreb, Douglas C.
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experimental part
p. 2643 - 2646
(2010/01/16)
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- 4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: In vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains
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In a program to optimize the anti-HIV activity of the 4-benzyl and 4-benzoyl-3-dimethylaminopyridinones 9 and 10, lead compounds in a new class of highly potent non-nucleoside type inhibitors of HIV-1 reverse transcriptase, modification of the alkyl substitutents at the C-5 and C-6 positions on the pyridinone ring and of the substitutents on the C-3 amino group has been studied. Of the 17 new 5/6-modified analogues prepared, compounds 31b and 32b substituted at C-5 by an extended nonpolar chain containing an ether function and a C-6 methyl group and compound 35 bearing a C-5 ethyl/C-6 hydroxymethyl substituent pattern were selected on the basis of their in vitro activity against wild-type HIV and the three principle mutant strains, K103N, Y181C, and Y188L. When tested further, it was shown that these molecules, and in particular compound 35, are globally more active than 9, 10, and efavirenz against an additional eight single [L100I, K101E, V106A, E138K, V179E, G190A/S, and F227C] and four double HIV mutant strains [L100I + K103N, K101E + K103N, K103N + Y181C, and F227L + V106A], which are clinically relevant. Concerning modulation of the N-3 substituent, 36 new analogues were prepared. Of these, the N-methyl-N-(2-methoxyethyl)-substituted compounds 40, 42, and 62, as well as the doubly modified compounds 77a and 77b, were selected from the initial screen and were subsequently shown to be active at sub-micromolar concentrations (IC50's) against all the other mutant strains except K103N + Y181C and F227L + V106A. Two possible, but distinct, modes of binding of these analogues in RT were suggested from molecular modeling studies. The preferred mode of binding for compound 62, corresponding to the predicted "orientation 1", was revealed in the X-ray crystal structure of the compound 62-RT complex.
- Benjahad, Abdellah,Croisy, Martine,Monneret, Claude,Bisagni, Emile,Mabire, Dominique,Coupa, Sophie,Poncelet, Alain,Csoka, Imre,Guillemont, Jér?me,Meyer, Christophe,Andries, Koen,Pauwels, Rudi,De Béthune, Marie-Pierre,Himmel, Daniel M.,Das, Kalyan,Arnold, Eddy,Chi, Hung Nguyen,Grierson, David S.
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p. 1948 - 1964
(2007/10/03)
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- A Simplified Route to a Key Intermediate in the Synthesis of the Chinese Nootropic Agent Huperzine A
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An efficient one-pot, three-component process for the preparation of 2-pyridones from a carbonyl compound, ammonia, and methyl propiolate has been found which provides ready access to a key intermediate in the synthesis of huperzine A.
- Kozikowski, Alan P.,Reddy, E. Rajarathnam,Miller, Chris P.
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p. 195 - 197
(2007/10/02)
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- Reactions de cyclisation de pentynyl-2 pyrimidones-4
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Acetylenic amidines HCC-(CH2)n-C(=NH)NH2 give, by condensation with β-ketoesters, pyrimidones substituted on carbon 2 by an acetylenic chain.Two types of evolution are observed when compounds are heated without any catalyst.The minor route is a cyclization by attack on a triple bond by the amidic nitrogen atom.The main reaction is a cycloaddition involving the non activated triple bond and an azadienic system, leading to non isolated tricyclic intermediates which retrocyclize to stable bicyclic compounds.
- Rougeot, Etienne,Moskowitz, Henri,Miocque, Marcel
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p. 1407 - 1409
(2007/10/02)
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