- Reactions of 1,2,4-Triazin-5(2H)-ones with Phenols and Aromatic Amines
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1,2,4-Triazin-5(2H)-ones 1 react as well with phenols, resorinol and its dimethyl ethers, as with dimethyland diethylaniline, yielding 6-aryl-1,6-didydro-1,2,4-triazin-5(2H)-ones 2, 4-8, 12-15. Oxidation of the 1,6-dihydroadducts 2a,b gives the correspond
- Chupakbin, Oleg N.,Rusinov, Vladimir L.,Beresnev, Dmitri G.,Neunhoeffer
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Read Online
- Ruthenium-Catalyzed Asymmetric Allylic Alkylation of Isatins
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A new ruthenium-based catalytic system for branched-selective asymmetric allylic alkylation is disclosed and applied to the synthesis of chiral isatin derivatives. The catalyst, which is generated in situ from commercially available CpRu(MeCN)3PF6 and a BINOL-derived phosphoramidite, is both highly active (TON up to 180) and insensitive to air and moisture. Additionally, the N-alkylated isatins accessible using this methodology are versatile building blocks that are readily transformed into chiral analogs of achiral drug molecules.
- Kalnmals, Christopher A.,Parkin, Sean,Ramakrishnan, Divya,Ryan, Michael C.,Smaha, Rebecca W.,Trost, Barry M.
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supporting information
(2020/04/02)
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- COMPOUNDS FOR TREATMENT OF GLIOBLASTOMA
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The present invention relates to compounds and methods for the treatment of glioblastoma, as well as to a pharmaceutical composition comprising said compounds. More specifically the invention relates to substituted quinoline derivatives having the formula (I), (II) or (III), and a pharmaceutical composition comprising said compounds for the treatment of cancer. (Formulae (I), (II), (III))
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Paragraph 00358-00359
(2018/09/08)
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- Double Carbonylation Using Glyoxal (HCOCOH): A Practical Copper-Promoted Synthesis of Isatins from Primary and Secondary Anilines
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A novel double carbonylation process has been demonstrated with easily available HCOCOH (glyoxal) as the double carbonylation reagent. Simple CuCl2?2H2O (copper(II) chloride dihydrate) was used as the oxidant for this transformation. Under optimized reaction conditions, various primary and secondary anilines were double-carbonylated to afford their corresponding isatins (26 examples, up to 80% yields). (Figure presented.).
- Kuan, Suzie Hui Chin,Sun, Wei,Wang, Lu,Xia, Chungu,Tay, Meng Guan,Liu, Chao
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supporting information
p. 3484 - 3489
(2017/09/06)
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- Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties
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We have screened molecules for inhibition of MetAP2 as a novel approach toward antiangiogenesis and anticancer therapy using affinity selection/mass spectrometry (ASMS) employing MetAP2 loaded with Mn2+ as the active site metal. After a series
- Kawai, Megumi,BaMaung, Nwe Y.,Fidanze, Steve D.,Erickson, Scott A.,Tedrow, Jason S.,Sanders, William J.,Vasudevan, Anil,Park, Chang,Hutchins, Charles,Comess, Kenneth M.,Kalvin, Douglas,Wang, Jieyi,Zhang, Qian,Lou, Pingping,Tucker-Garcia, Lora,Bouska, Jennifer,Bell, Randy L.,Lesniewski, Richard,Henkin, Jack,Sheppard, George S.
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p. 3574 - 3577
(2007/10/03)
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- Sulfonamides having antiangiogenic and anticancer activity
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Compounds having methionine aminopeptidase-2 inhibitory (MetAP2) are described. Also described are pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, methods of inhibiting angiogenesis, and methods of treating cancer.
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- Sulfonamides having antiangiogenic and anticancer activity
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Compounds having methionine aminopeptidase-2 inhibitory (MetAP2) are described. Also described are pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, methods of inhibiting angiogenesis, and methods of treating cancer.
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- Sulfonamides having antiangiogenic and anticancer activity
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Compounds having methionine aminopeptidase-2 inhibitory (MetAP2) are described. Also described are pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, methods of inhibiting angiogenesis, and methods of treating
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