- Ni-Catalyzed Reductive Arylcyanation of Alkenes
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We disclose a Ni-catalyzed reductive arylcyanation of alkene using environmentally benign and nontoxic organo cyanating reagent N-cyano-N-phenyl-p-toluenesulfonamide. This reaction provides a new method for the rapid synthesis of cyano-substituted oxindoles and isoquinoline-1,3-diones and features high functional group tolerance. In addition, an enantioselective version was developed for the construction of enantiomerically enriched 3-cyanomethyl oxindole. This method has also been applied to the synthesis of natural alkaloids (+)-esermethole and (+)-physostigmine.
- Li, Hengxu,Chen, Jiachang,Dong, Jueqi,Kong, Wangqing
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supporting information
p. 6466 - 6470
(2021/08/23)
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- Axial chiral biphenyl ring-chain isomeric compound, and preparation method and application thereof
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The invention belongs to the technical field of chiral compound recognition and purity determination, and particularly relates to an axial chiral biphenyl ring-chain isomeric compound, and a preparation method and an application thereof. The axial chiral
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Paragraph 0083-0087
(2020/02/10)
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- COMPOUNDS AND USES THEREOF
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The present invention features compounds useful in the treatment of neurological disorders. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders.
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Paragraph 1331
(2019/11/11)
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- Chemoselective Synthesis of Aryl Ketones from Amides and Grignard Reagents via C(O)-N Bond Cleavage under Catalyst-Free Conditions
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Conversion of a wide range of N-Boc amides to aryl ketones was achieved with Grignard reagents via chemoselective C(O)-N bond cleavage. The reactions proceeded under catalyst-free conditions with different aryl, alkyl, and alkynyl Grignard reagents. α-Ketoamide was successfully converted to aryl diketones, while α,β-unsaturated amide underwent 1,4-addition followed by C(O)-N bond cleavage to provide diaryl propiophenones. N-Boc amides displayed higher reactivity than Weinreb amides with Grignard reagents. A broad substrate scope, excellent yields, and quick conversion are important features of this methodology.
- Sureshbabu, Popuri,Azeez, Sadaf,Muniyappan, Nalluchamy,Sabiah, Shahulhameed,Kandasamy, Jeyakumar
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p. 11823 - 11838
(2019/10/02)
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- Nickel-catalyzed regioselective C-H halogenation of electron-deficient arenes
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A straightforward Ni(ii)-catalyzed general strategy was developed for the ortho-halogenation of electron-deficient arenes with easily available halogenating reagents N-halosuccinimides (NXS; X = Br, Cl and I). The transformation was highly regioselective and a wide substrate scope and functional group tolerance were observed. This discovery could be of great significance for the selective halogenation of amides, benzoic esters and other substances with guiding groups. Mechanistic investigations were also described.
- Li, Ze-Lin,Wu, Peng-Yu,Cai, Chun
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supporting information
p. 3462 - 3468
(2019/02/25)
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- Cell-Active Small Molecule Inhibitors of the DNA-Damage Repair Enzyme Poly(ADP-ribose) Glycohydrolase (PARG): Discovery and Optimization of Orally Bioavailable Quinazolinedione Sulfonamides
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DNA damage repair enzymes are promising targets in the development of new therapeutic agents for a wide range of cancers and potentially other diseases. The enzyme poly(ADP-ribose) glycohydrolase (PARG) plays a pivotal role in the regulation of DNA repair mechanisms; however, the lack of potent drug-like inhibitors for use in cellular and in vivo models has limited the investigation of its potential as a novel therapeutic target. Using the crystal structure of human PARG in complex with the weakly active and cytotoxic anthraquinone 8a, novel quinazolinedione sulfonamides PARG inhibitors have been identified by means of structure-based virtual screening and library design. 1-Oxetan-3-ylmethyl derivatives 33d and 35d were selected for preliminary investigations in vivo. X-ray crystal structures help rationalize the observed structure-activity relationships of these novel inhibitors.
- Waszkowycz, Bohdan,Smith, Kate M.,McGonagle, Alison E.,Jordan, Allan M.,Acton, Ben,Fairweather, Emma E.,Griffiths, Louise A.,Hamilton, Niall M.,Hamilton, Nicola S.,Hitchin, James R.,Hutton, Colin P.,James, Dominic I.,Jones, Clifford D.,Jones, Stuart,Mould, Daniel P.,Small, Helen F.,Stowell, Alexandra I. J.,Tucker, Julie A.,Waddell, Ian D.,Ogilvie, Donald J.
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supporting information
p. 10767 - 10792
(2019/01/04)
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- 2,4-DIOXO-QUINAZOLINE-6-SULFONAMIDE DERIVATIVES AS INHIBITORS OF PARG
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The present invention relates to compounds of formula I that function as inhibitors of PARG (Poly ADP-ribose glycohydrolase) enzyme activity wherein R1a, R1b, R1c, R1d, R1e, W, X1, X2, X3, X4, X5, X6, X7, c are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which PARG activity is implicated.
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Page/Page column 99; 179; 180
(2016/07/05)
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- Palladium-catalyzed C-C coupling of aryl halides with isocyanides: An alternative method for the stereoselective synthesis of (3E)-(Imino)isoindolin- 1-ones and (3E)-(imino)thiaisoindoline 1,1-dioxides
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A palladium-catalyzed, one-pot cyclization reaction to construct (3E)-(imino)isoindolin-1-ones and (3E)-(imino)thiaisoindoline 1,1-dioxides by introducing ortho-reactive functional groups on aryl halides is reported. Under optimal conditions, the cyclization reaction afforded the corresponding products in good to excellent yields (up to 93%) with high stereoselectivity. Notably, this transformation successfully extends its application for the synthesis of phenanthridines and dibenzooxazepines. This new synthetic protocol not only extends the application platform for palladium-catalyzed C-C coupling of aryl halides with isocyanides, but also opens atom-economic and step-economic synthetic routes for nitrogen-containing heterocyclic compounds with wide functional group compatibility. Copyright
- Liu, Bifu,Li, Yibiao,Jiang, Huanfeng,Yin, Meizhou,Huang, Huawen
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p. 2288 - 2300
(2012/11/07)
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- Rhodium(iii)-catalyzed oxidative carbonylation of benzamides with carbon monoxide
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An efficient strategy for the oxidative carbonylation of aromatic amides via C-H/N-H activation to form phthalimides using an Rh(iii) catalyst has been developed. The reaction shows a preference for C-H bonds of electron-rich aromatic amides and tolerates a variety of functional groups. The Royal Society of Chemistry 2011.
- Du, Ya,Hyster, Todd K.,Rovis, Tomislav
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p. 12074 - 12076
(2011/12/14)
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- AROMATIC HETEROANNULATION VIA ORTHO LITHIATION-CYCLIZATION OF N-ACYL-2-BROMOBENZAMIDES
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N-acyl-2-bromobenzamides participate in metal-halogen exchange with n-BuLi to form N-acyl-2-lithiobenzamides, which undergo cyclization to afford 3-alkylidenephtalimides.
- Hendi, Mukta S.,Natalie, Kenneth J. Jr.,Hendi, Shivakumar B.,Campbell, James A.,Greenwood, Thomas D.,Wolfe, James F.
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p. 275 - 278
(2007/10/02)
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- TRANSANNULAR BOND FORMATION BETWEEN THE ANTIMONY AND THE NITROGEN ATOMS IN DIBENZAZASTIBOCINE SYSTEM. FORMATION OF X-Sb-X AND X-Sb-N(1+) HYPERVALENT BOND
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6-Methyl-5,6,7,12-tetrahydro-12-p-tolyldibenzazastibocine (1) was prepared by means of one-pot reaction of di(o-bromobenzyl)methylamine (2), butyllithium, and antimony trichloride, followed by p-tolyllithium in 23percent yield.Halogenation of 1
- Ohkata, Katsuo,Ohnishi, Masako,Akiba, Kin-ya
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p. 5401 - 5404
(2007/10/02)
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