- “On water” nano-Cu2O-catalyzed CO-free one-pot multicomponent cascade cyanation-annulation-aminolysis reaction toward phthalimides
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An efficient nano-Cu2O-catalyzed cascade multicomponent reaction of 2-halobenzoic acids and trimethylsilyl cyanide with diverse amines was developed using water as a solvent, affording versatileN-substituted phthalimide derivatives in moderate to excellent yields. This novel strategy features carbon monoxide gas-free, environmentally benign, one-pot multistep transformation, commercially available reagents, a cheap catalyst without any additives, wide functional group tolerance, and operational convenience.
- Wen, Xiaowei,Liu, Xiaojuan,Yang, Zhiqi,Xie, Menglan,Liu, Yuxi,Long, Lipeng,Chen, Zhengwang
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supporting information
p. 1738 - 1743
(2021/03/14)
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- ANTIMICROBIAL COMPOUNDS AND METHODS
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The invention is directed to compounds that are active as antibacterial agents. The invention compounds are active against gram-positive and gram-negative bacteria and can be used to treat infections caused by gram-positive and gram-negative bacteria. Also disclosed are processes and intermediates for making the compounds.
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Paragraph 00704
(2020/07/31)
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- Application of maleimide compound as chitin synthase inhibitor
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The invention discloses an application of a maleimide compound as shown in a formula I. In the formula I, R0 is phenyl, benzyl, phenethyl, phenylpropyl, p-fluorophenyl, p-chlorophenyl, p-bromophenyl,p-methoxyphenyl, p-methylphenyl or p-hydroxyphenyl, R1 is hydrogen, methyl, phenyl or chlorine; and R2 is hydrogen, methyl, phenyl or chlorine. The provided maleimide compound has a good inhibition effect on chitin synthase.
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Paragraph 0024-0027; 0044-0047
(2020/07/12)
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- Anti-leishmanial and cytotoxic activities of a series of maleimides: Synthesis, biological evaluation and structure-activity relationship
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In the present study, 45 maleimides have been synthesized and evaluated for anti-leishmanial activities against L. donovani in vitro and cytotoxicity toward THP1 cells. All compounds exhibited obvious anti-leishmanial activities. Among the tested compounds, there were 10 maleimides with superior anti-leishmanial activities to standard drug amphotericin B, and 32 maleimides with superior anti-leishmanial activities to standard drug pentamidine, especially compounds 16 (IC50 50 50 > 10 μg/mL). The anti-leishmanial activities of 16 and 42 were 10 times better than that of amphotericin B. The structure and activity relationship (SAR) studies revealed that 3,4-non-substituted maleimides displayed the strongest anti-leishmanial activities compared to those for 3-methyl-maleimides and 3,4-dichloro-maleimides. 3,4-dichloro-maleimides were the least cytotoxic compared to 3-methyl-maleimides and 3,4-non-substituted maleimides. The results show that several of the reported compounds are promising leads for potential anti-leishmanial drug development.
- Fan, Yongxian,Lu, Yuele,Chen, Xiaolong,Tekwani, Babu,Li, Xing-Cong,Shen, Yinchu
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- First total synthesis of 5-hydroxy-3-methyl-4-propylsulfanyl-5 h -furan-2-one: A cancer chemopreventive agent
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The first total synthesis of 5-hydroxy-3-methyl-4-propylsulfanyl-5H-furan- 2-one, a newly discovered natural product with anticancer property is described by two different routes. A sequence involving an incorporation of a methyl group via a Gilman reagent and a chemoselective reduction of a cyclic anhydride functionality are the key steps. The methods proposed start from easily available starting materials and allow ready preparation of the final compound in good overall yield. Georg Thieme Verlag Stuttgart · New York.
- Borikar, Sanjay P.,Paul, Vincent,Puranik, Vedavati G.,Sathe, Vilas T.,Lagunas-Rivera, Selene,Ordonez, Mario
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experimental part
p. 1595 - 1598
(2011/06/24)
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- Highly Enantioselective diels-alder reactions of maleimides catalyzed by activated chiral oxazaborolidines
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[Chemical equation presented] Diels-Alder reactions of various combinations of maleimides and 1,3-dienes with cationic oxazaborolidines as catalysts have been shown to be highly efficient and enantioselective.
- Mukherjee, Santanu,Corey
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supporting information; experimental part
p. 632 - 635
(2010/06/17)
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- Efficient asymmetric hydrogenation of the C-C double bond of 2-methyl- and 2,3-dimethyl-N-phenylalkylmaleimides by Aspergillus fumigatus
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Eight N-phenylalkylmaleimides (four 2-methyl-N-phenylalkylmaleimides and four 2,3-dimethyl-N-phenylalkylmaleimides with an alkyl chain (CH2)n (n = 1-4) between the imide N and the benzene ring) were subjected to biotransformation usi
- Sortino, Maximiliano,Zacchino, Susana Alicia
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experimental part
p. 535 - 539
(2010/08/20)
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- Rhodium-catalyzed asymmetric construction of quaternary carbon stereocenters: Ligand-dependent regiocontrol in the 1,4-addition to substituted maleimides
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A rhodium-catalyzed asymmetric 1,4-addition of arylboronic acids to substituted maleimides has been described. The regioselectivity in this reaction is controlled by the choice of ligand (dienes or bisphosphines), and 1,4-adducts with a quaternary stereoc
- Shintani, Ryo,Duan, Wei-Liang,Hayashi, Tamio
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p. 5628 - 5629
(2007/10/03)
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- Asymmetric hydrogenation of the C-C double bond of 1- and 1,2-methylated maleimides with cultured suspension cells of Marchantia polymorpha
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Suspension cultured cells of Marchantia polymorpha have the potential to hydrogenate the C-C double bonds of 2-methyl- and 2,3-dimethylmaleimide derivatives to give enantiomerically pure (2R)-2-methyl- and (2R,3R)-2,3-dimethylsuccinimide derivatives, resp
- Hegazy, Mohamed-Elamir F.,Shishido, Kozo,Hirata, Toshifumi
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p. 1859 - 1862
(2007/10/03)
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- Synthesis of N-substituted -alkoxy-3-aryl-4-methyl-2,5-dihydro-2-pyrrolones
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5-Alkoxy-1-aralkyl-3-aryl-4-methyl-2,5-dihydro-2-pyrrolones and the corresponding alkylthio derivatives were synthesized for the first time through the intermediate formation of unsymmetrical maleimides. The possibility of wide variation of the substituen
- Nikitin,Andryukhova
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p. 561 - 569
(2007/10/03)
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- Product diversity in cyclisations of maleamic acids: The imide-isoimide dichotomy
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Cyclisation of maleamic acids with acetic anhydride in dimethylacetamide (DMA) at ca. 75°C, with or without added cobalt naphthenate, gives predominantly maleimides when the parent maleic anhydride is unsubstituted. However, when the maleic anhydride has
- Corrie, John E. T.,Moore, Madeleine H.,Wilson, Giles D.
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p. 777 - 781
(2007/10/03)
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- The Synthesis of 5-Ylidenepyrrol-2(5H)-ones from Maleimides and from Pyrrol-2-(5H)-ones
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A series of maleimides 5 have been prepared by reaction of the appropriate maleic anhydrides with either ammonium acetate or methylammonium acetate in boiling acetic acid.The maleimides underwent Wittig-type reactions with stabilised phosphoranes, under m
- Gill, G. Bryon,James, Gwyn D.,Oates, Karen V.,Pattenden, Gerald
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p. 2567 - 2580
(2007/10/02)
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- Synthesis of 5-Iminopyrrol-2-one Derivatives from 1,3-Oxazines. Ring Transformations via Attack on the 2- or 6-Position of 1,3-Oxazines
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Reaction of the 2H-1,3-oxazine-2,4(3H)-dione derivatives (1) with potassium cyanide resulted in a ring contraction to give the corresponding 5-imino-1,5-dihydro-2H-pyrrol-2-ones (2), together with the 3-acetyl-4-amino-1H-pyrrole-2,5-diones (3) or the (E)-
- Yogo, Motoi,Hirota, Kosaku,Maki, Yoshifumi
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p. 2097 - 2102
(2007/10/02)
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