- A New Efficient Access to Cyclic Imines
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Cyclic imines can be conveniently prepared from ω-azidoketones by an intramolecular 'aza-Wittig' reaction.
- Lambert, Pierre H.,Vaultier, Michel,Carrie, Robert
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Read Online
- Iron-Catalyzed Ring Expansion of Cyclobutanols for the Synthesis of 1-Pyrrolines by Using MsONH3OTf
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The synthesis of 1-pyrrolines from cyclobutanol derivatives and an aminating reagent (MsONH3OTf) has been developed. This one-pot procedure achieves C–N bond/C═N bond formation via ring expansion. A series of 1-pyrroline derivatives are synthes
- Zhuang, Daijiao,Gatera, Tharcisse,An, Zhenyu,Yan, Rulong
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supporting information
p. 771 - 775
(2022/01/20)
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- INDOLO HEPTAMYL OXIME ANALOGUE AS PARP INHIBITOR
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Disclosed is a type of indolo heptamyl oxime compounds as a PARP inhibitor. Specifically disclosed are a compound as represented by formula (II) and a pharmaceutically acceptable salt thereof.
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- PYRROLOPYRIMIDINE COMPOUNDS USED AS TLR7 AGONIST
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The present invention relates to a pyrrolopyrimidine compound as TLR7 agonist, and particularly relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, a preparation process thereof, a pharmaceutical composition containing such compounds and use thereof for manufacturing a medicament against viral infection.
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Paragraph 0103
(2017/07/29)
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- Pyrrolo pyrimidine ring compound, its use and pharmaceutical composition (by machine translation)
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The invention relates to an as TLR7 agonist of the pyrrolo pyrimidine compounds, specifically on a compound of formula (I) compound or its pharmaceutically acceptable salt, preparation method thereof, containing the compounds of the pharmaceutical composition, and its use for the preparation of antiviral drug use. Formula (I) (by machine translation)
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Page/Page column 53
(2017/07/31)
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- ETHYL N-BOC PIPERIDINYL PYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS
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Provided are compounds of Formula I as JAK inhibitors, which are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
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Page/Page column 49
(2016/05/24)
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- CYCLOALKYL NITRILE PYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS
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Compounds of formula I are provided, which are JAK inhibitors and are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
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Page/Page column 156
(2014/10/03)
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- ACYCLIC CYANOETHYLPYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS
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The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
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Page/Page column 86
(2014/10/03)
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- GEMINALLY SUBSTITUTED CYANOETHYLPYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS
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The instant invention provides compounds of Formula (I) which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
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Page/Page column 124
(2014/10/03)
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- The reaction of cyclic imines with the Ruppert-Prakash reagent. Facile approach to α-trifluoromethylated nornicotine, anabazine, and homoanabazine
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We have demonstrated that the Ruppert-Prakash reagent is able to react with a number of cyclic imines under acidic condition to afford the corresponding α-trifluoromethyl derivatives of nitrogen heterocycles. 5-7-Membered cyclic imines bearing various alkyl, aryl or heterocyclic group were successfully involved in this transformation. Novel trifluoromethylated analogues of nicotine, anabasine, and homoanabasine alkaloids were synthesized.
- Shevchenko, Nikolay E.,Vlasov, Katja,Nenajdenko, Valentine G.,R?schenthaler, Gerd-Volker
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scheme or table
p. 69 - 74
(2011/02/27)
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- Highly effective asymmetric hydrogenation of cyclic N -alkyl imines with chiral cationic Ru-MsDPEN catalysts
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A range of cyclic N-alkyl imines were efficiently hydrogenated by using a chiral cationic Ru(η6-cymene)(MsDPEN)(BArF) complex (MsDPEN = N-(methanesulfonyl)-1,2-diphenylethylenediamine) in high yields and up to 98% ee. A one-pot synthesis of chiral 2-phenylpyrrolidine via reductive amination was also developed.
- Chen, Fei,Ding, Ziyuan,Qin, Jie,Wang, Tianli,He, Yanmei,Fan, Qing-Hua
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supporting information; experimental part
p. 4348 - 4351
(2011/10/13)
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- METHODS OF USING DIHYDROPYRIDOPHTHALAZINONE INHIBITORS OF POLY (ADP-RIBOSE)POLYMERASE (PARP)
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Provided herein are methods of treating cancer comprising administering a topoisomerase inhibitor, temozolomide, or a platin in combination with a Compound of Formula (I) or Formula (II), where the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein.
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Page/Page column 196
(2011/11/01)
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- Iridium-catalyzed enantioselective hydrogenation of cyclic imines
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A catalytic complex made from [Ir(COD)Cl]2 [di-μ-chloro- bis(1,5-cyclooctadiene)diiridium(I)] precursor and (S,S)-f-Binaphane ((R,R)-1,1′-bis{(R)-4,5-dihydro-3H-dinaphtho[1,2-c:2′,1′-e] phosphepino}ferrocene) ligand effectively catalyzed the en
- Chang, Mingxin,Li, Wei,Hou, Guohua,Zhang, Xumu
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supporting information; experimental part
p. 3121 - 3125
(2011/02/22)
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- DIHYDROPYRIDOPHTHALAZINONE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP)
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A compound having the structure set forth in Formula (I) and Formula (II): wherein the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.
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Page/Page column 99
(2010/03/02)
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- THIAZOLYL-DIHYDRO-INDAZOLES
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The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a
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Page/Page column 41; 42
(2009/10/22)
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- ANTI-VIRAL COMPOUNDS
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Disclosed are compounds, stereoisomers, tautomers, pharmaceutically acceptable salts, or prodrugs thereof of having Formula (I), their preparation, use, and compositions thereof for treating an infection mediated at least in part by a virus in the Flavivi
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Page/Page column 49
(2008/12/06)
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- HEXAHYDRO-PYRROLO-ISOQUINOLINE COMPOUNDS
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Certain hexahydro-pyrrolo-isoquinoline compounds are histamine H3 receptor and serotonin transporter modulators useful in the treatment of histamine H3 receptor- and serotonin-mediated diseases.
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Page/Page column 60
(2010/11/25)
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- An efficient one-pot synthesis of pyrrolines and tetrahydropyridines from their chloro-precursors via in situ aza-Wittig reaction
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A simple and efficient method for synthesizing pyrrolines and tetrahydropyridines via an intramolecular aza-Wittig reaction has been achieved by microwave irradiation of the corresponding chloro-alkane derivatives in the presence of tertiary phosphite and sodium azide. The in situ formation of the alkyl azides makes this a facile and safe method for aza-Wittig reactions.
- Singh, Pradeep N.D.,Klima, Rodney F.,Muthukrishnan, Sivaramakrishnan,Murthy, Rajesh S.,Sankaranarayanan, Jagadis,Stahlecker, Heidi M.,Patel, Bhavika,Gudmundsdóttir, Anna D.
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p. 4213 - 4217
(2007/10/03)
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- Hammett correlation of nornicotine analogues in the aqueous aldol reaction: Implications for green organocatalysis
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(Chemical Equation Presented) A series of meta- and para-substituted 2-arylpyrrolidines were synthesized and examined for their ability to catalyze an aqueous aldol reaction under buffered conditions. Kinetic analysis of arylpyrrolidine-catalyzed reactions displayed a linear Hammett correlation with ρ = 1.14 (R2 = 0.996), indicating that the reaction is accelerated by electron-withdrawing aryl rings. These results show promise for the development of a synthetically viable aqueous organocatalyst.
- Rogers, Claude J.,Dickerson, Tobin J.,Brogan, Andrew P.,Janda, Kim D.
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p. 3705 - 3708
(2007/10/03)
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- Easy one-pot access to substituted 2-phenylpyrrolines from 2-pyrrolidinone
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An easy access to 2-aryl pyrrolidines is the reduction, stereospecific or not, of the corresponding 2-aryl-pyrroline (5-aryl-3,4-dihydro-2H-pyrrole). Preparation of the latter has been carried out from 2-pyrrolidinone using an easy one-pot two-step method
- Coindet, Cécile,Comel, Alain,Kirsch, Gilbert
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p. 6101 - 6104
(2007/10/03)
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- La reaction d'ω-azidocetones avec la triphenylphosphine: une voie d'acces generale aux imines cycliques
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The ω-azidoketones RC(=O)-CH(R')-(CH2)n-CH(R'')-N3 react with triphenylphosphine in anhydrous media to give 5, 6 and 7 membered cyclic imines via an intramolecular aza-Wittig reaction with good yields.A general synthesis of ω-haloketones which are the precursors of the azidoketones was also devised.
- Vaultier, M.,Lambert, P. H.,Carrie, R.
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- PHOTOCYCLOADDITIONS OF ELECTRON POOR OLEFINS TO 2-ARYL-1-PYRROLINIUM SALTS
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Photocycloadditions of the electron poor olefins, acrylonitrile and methyl acrylate to a series of para-substituted 2-phenyl-1-pyrrolinium perchlorates have been explored as part of studies designed to test new synthetic methods.
- Mariano, Patrick S.,Leone-Bay, Andrea
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p. 4581 - 4584
(2007/10/02)
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