- Solvent-controlled two-step one-pot syntheses of α-X (X = Br or Cl) enamino ketones/esters and 3-(2,5-dioxopyrrolidin-1-yl)acrylate by using terminal carbonyl alkynes
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A new two-step one-pot aminobromination/chlorination of carbonyl alkynes has been achievedviaa Michael addition of aliphatic secondary amines and subsequent β-bromination/chlorination of the obtained enamines to afford various α-X (X = Br or Cl) enamino ketones/esters in moderate to good yields. A solvent-controllable protocol has been developed to produce versatile 3-(2,5-dioxopyrrolidin-1-yl)acrylates in moderate yields by using toluene as the solvent and chain alkyl propiolates as alkynyl substrates.
- Chen, Xiao Yun,Yuan, Shuxia,Chen, Yan,Sun, Chenyang,Tang, Yaonan,Chen, Guang,Zhu, Baocheng,Chen, Kaiwei,Zheng, Shaojun,Cheng, Xiaofang
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supporting information
p. 7914 - 7919
(2021/09/28)
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- Green H 2 O-Promoted Solvent-Free Synthesis of Enaminocarbonyl Compounds with High Stereoselectivity from Electron-Deficient Terminal Alkynes
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A green H 2 O-promoted solvent-free hydroamination of electron-deficient terminal alkynes with amines has been developed. All secondary amines, including aliphatic and aromatic amines, gave the corresponding (E)-enamines in good to excellent yi
- Chen, Guang,Chen, Xiao Yun,Cheng, Xiaofang,Tang, Yaonan,Yuan, Shuxia,Zhang, Luming,Zhu, Baocheng
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supporting information
p. 878 - 882
(2020/05/28)
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- Ir-catalyzed chemoselective reduction of β-amido esters: A versatile approach to β-enamino esters
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The conversion of β-amido esters to β-enamino esters is an indispensable step for some synthetic approaches to alkaloids and related medicines. Known methods for such transformation are not only stepwise, but also proceed with low atom-efficiency. Herein, we report a direct and versatile approach that features the Ir-catalyzed chemoselective reduction of β-amido esters with 1,1,3,3-tetramethyldisiloxane (TMDS). In addition, a lack of some signals was observed in the 13C NMR spectra of some alicyclic β-enamino esters. This revealed a longstanding existing but being ignored phenomenon in the literature.
- Yang, Zhi-Ping,Lu, Guang-Sheng,Ye, Jian-Liang,Huang, Pei-Qiang
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p. 1624 - 1631
(2019/01/04)
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- PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS
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Compounds of Formula (I), Formula (II), Formula (III), Formula (IV), Formula (V), Formula (VI), Formula (VII), Formula (VIII), and methods of use as lnterleukin-1 Receptor Associated Kinase (IRAK4) inhibitors are described herein.
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Page/Page column 131
(2019/01/10)
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- A field-based disparity analysis of new 1,2,5-oxadiazole derivatives endowed with antiproliferative activity
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A series of 1,2,5-oxadiazoles were synthesized as new potential antiproliferative agents. The in vitro cytotoxic activity evaluation of title compounds through MTT assay revealed that some of them showed significant activity against the HCT-116 cancer cell line. The field-based disparity analysis provided indications about the electrostatic, hydrophobic, and shape features underlying the cytotoxicity, suggesting that increasing the negative electrostatic field on the heterocyclic core of the structure has positive effects on the activity. The structure–activity relationships (SAR) around a particular compound can be explained allowing for a structural rationale for the differences in activity. The SAR provided by this series of compounds can be exploited to carry out further lead optimization.
- Porta, Federica,Gelain, Arianna,Barlocco, Daniela,Ferri, Nicola,Marchianò, Silvia,Cappello, Valentina,Basile, Livia,Guccione, Salvatore,Meneghetti, Fiorella,Villa, Stefania
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p. 820 - 839
(2017/10/03)
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- Discovery of potent and selective pyrazolopyrimidine Janus kinase 2 inhibitors
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The discovery of somatic Jak2 mutations in patients with chronic myeloproliferative neoplasms has led to significant interest in discovering selective Jak2 inhibitors for use in treating these disorders. A high-throughput screening effort identified the p
- Hanan, Emily J.,Van Abbema, Anne,Barrett, Kathy,Blair, Wade S.,Blaney, Jeff,Chang, Christine,Eigenbrot, Charles,Flynn, Sean,Gibbons, Paul,Hurley, Christopher A.,Kenny, Jane R.,Kulagowski, Janusz,Lee, Leslie,Magnuson, Steven R.,Morris, Claire,Murray, Jeremy,Pastor, Richard M.,Rawson, Tom,Siu, Michael,Ultsch, Mark,Zhou, Aihe,Sampath, Deepak,Lyssikatos, Joseph P.
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p. 10090 - 10107
(2013/01/16)
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- A facile approach to substituted acrylates by regioselective and stereoselective addition of thiols and amines to an alkynyl ester in water
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Water-promoted hydrothiolation and hydroamination of ethyl propiolate leading to highly regioselective and stereoselective formation of thioacrylates and β-enamino esters in excellent yields, by a simple, efficient, and environmentally friendly reaction p
- Randive, Nitin A.,Kumar, Varun,Nair, Vipin A.
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experimental part
p. 1329 - 1332
(2011/09/20)
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- 3-Aryl-4-isothiazolecarboxylic acid and 3-aryl-4-isoxazolecarboxylic acid derivatives and their use as herbicides
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Carboxylic acid derivatives having the formula STR1 have been found to be effective herbicides. They are especially effective when applied as a pre-emergent herbicide.
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- 3-Aryl-4-isoxazolecarboxylic acids as plant growth regulants
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3-Aryl-4-isothiazolecarboxylic acids as well as 3-aryl-4-isoxazolecarboxylic acids have been found to be effective plant growth regulants especially when applied to soybean plants.
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