- Design, synthesis and biological evaluation of substituted 2-amino-1,3-thiazine derivatives as antituberculosis and anti-cancer agents
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A series of substituted 2-amino-1,3-thiazines were synthesized as amides (9a–9i), carbamates (9j–9m), sulfonamides (9n–9o) and urea derivatives (9p–9q) by treating the compound 7 with acid chlorides (8a–8i), chloroformates (8j–8m), sulfonyl chlorides (8n–8o) and isocyanates (8p–8q) respectively. The synthesized compounds (9a–9q) were screened for antituberculosis activity against Mycobacterium tuberculosis H37Rv ATCC 27294 and the results show that some of these derivatives possess good activity against Mycobacterium tuberculosis H37Rv ATCC 27294. A few also display promising cytotoxic activity against human breast cancer MCF-7 and human esophageal cancer EC-9706 cell lines. Regarding both biological profiles 9b, 9m and 9h are the most active for anti-cancer, anti-TB activity.
- Nagendra Prasad, Tangella,Eeda, Koti Reddy,Gudise, Veera Babu,Basha, Shaik Firoj,Anwar, Shaik
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supporting information
p. 1277 - 1285
(2019/04/27)
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- Synthesis of β-haloketones by β-addition reactions of α,β-unsaturated ketones with BX3 (X = Br, Cl) as halide source
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A series of β-bromoketones and β-chloroketones were synthesized by the addition reactions of α,β-unsaturated ketones under BX 3 (X = Br, Cl) and ethylene glycol reaction system. The α,β-unsaturated ester also was successfully converted to its corresponding β-bromoester under the reaction condition. A series of β-bromoketones and β-chloroketones were synthesized by the addition reactions of α,β-unsaturated ketones under BX3 (X=Br, Cl) and ethylene glycol reaction system. Copyright
- Lee, Adam Shih-Yuan,Wang, Shu-Huei,Chang, Yu-Ting
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p. 364 - 368
(2014/05/06)
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- Rhodium(I)-catalyzed arylation of β-chloro ketones and related derivatives through domino dehydrochlorination/conjugate addition
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Highly efficient arylations of β-chloro ketones and their ester and amide derivatives were achieved by means of domino dehydrochlorination/Rh(I)- catalyzed conjugate addition. In situ generated vinyl ketones and their analogues were identified as the reaction intermediates. The present synthetic protocol provides a concise route to (chiral) β-aryl ketones, esters, and amides. Copyright
- Jiang, Quanbin,Guo, Tenglong,Wang, Qingfu,Wu, Ping,Yu, Zhengkun
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supporting information
p. 1874 - 1880
(2013/07/19)
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- Trifluoroacetic anhydride - Catalyzed conjugate addition of boronic acids to α,β-unsaturated ketones
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The conjugate addition of boronic acids to α,β-unsaturated ketones catalyzed by acylating reagents has been explored. The results show that trifluoroacetic anhydride catalyzes the addition of vinylboronic acids under experimentally simple and metal-free conditions for a variety of substrates with good yields.
- Roscales, Silvia,Rincón, ángela,Buxaderas, Eduardo,Csák?, Aurelio G.
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experimental part
p. 4721 - 4724
(2012/09/08)
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- Synthesis of β-Amino and β-Methoxy Ketones by Lewis Acids Promoted β-Substitution Reactions of βγ,-Unsaturated Ketones
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A reaction mixture of β,γ-unsaturated ketone and BF 3·OEt2 in CH3OH was stirred at room temperature and β-methoxy ketone was produced in high yield. The β-amino ketone was obtained as the major product from a reaction mixture of β,γ-unsaturated ketone, AlCl3 and Ts-NH2 in CH2Cl2 at room temperature. This Lewis acid promoted β-substitution reaction mechanism was proposed as that the process occurred via in situ isomerization of β,γ-unsaturated ketone to α,β-unsaturated ketone followed by the 1,4-addition reaction.
- Lee, Adam Shih-Yuan,Wang, Shu-Huei,Chang, Yu-Ting,Chu, Shu-Fang
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p. 2359 - 2363
(2007/10/03)
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