335206-60-5Relevant academic research and scientific papers
Preparation system and preparation method of benzo quinazolinone derivative
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Paragraph 0039; 0063; 0064, (2017/11/04)
The invention discloses a preparation system and preparation method of a benzo quinazolinone derivative and belongs to the technical field of organic synthesis. The preparation system of the benzo quinazolinone derivative comprises a reactor, an ultrasonic-assisted reaction device, an ice-water bath cooling device, a suction filtration device, a washing device and a vacuum drying device, wherein the ultrasonic-assisted reaction device, the ice-water bath cooling device, the suction filtration device, the washing device and the vacuum drying device are sequentially arranged. Aromatic aldehyde, alpha-tetralone and urea or thiourea are taken as reaction raw materials and are catalyzed under the catalytic action of an acidic ionic liquid catalyst and under the ultrasonic-assisted action to prepare the benzo quinazolinone derivative. By adopting the technical scheme, the catalyst is relatively small in dosage and loss, and can be recycled for multiple times, the preparation system is high in raw material utilization rate and short in reaction time and a product is simple and convenient to purify.
Synthesis of fused thiazolo[3,2-a]pyrimidinones: N-aryl-2-chloroacetamides as doubly electrophilic building blocks
Janardhan, Banothu,Srinivas, Basavoju,Rajitha, Bavantula,Peter A., Crooks
, p. 224 - 226 (2014/01/06)
2-Chloro-N-phenylacetamide and N-(benzo[d]thiazol-2-yl)-2-chloroacetamide are doubly electrophilic building blocks for the formation of ring annulated thiazolo[3,2-a]pyrimidinone products. This synthetic route involves formation of the title compound in acceptable product yields by the elimination of the by-product, aniline/2-aminobenzothiazole. Analytical and spectral studies, as well as single crystal X-ray data on the representative compound 6c confirmed the structure of all the reaction products.
Indolylmethylene benzo[h]thiazolo[2,3-b]quinazolinones: Synthesis, characterization and evaluation of anticancer and antimicrobial activities
Gali, Rajitha,Banothu, Janardhan,Porika, Mahendar,Velpula, Ravibabu,Hnamte, Sairengpuii,Bavantula, Rajitha,Abbagani, Sadanandam,Busi, Siddhardha
, p. 4239 - 4242 (2014/09/17)
A series of novel 10-((1H-indol-3-yl)methylene)-7-aryl-7,10-dihydro-5H- benzo[h]thiazolo[2,3-b]quinazolin-9(6H)-ones (8a-t) have been synthesized in good yields by the reaction of benzo[h]quinazoline-2(1H)-thiones (4a-f) with 2-chloro-N-phenylacetamide (5) followed by Knoevenagel condensation with various indole-3-carbaldehydes (7a-d) under conventional method. All the synthesized compounds were characterized by spectral studies and screened for their in vitro anticancer and antimicrobial activities. Compound 8c has exhibited excellent activity against MCF-7 (breast cancer cell line) than the standard drug Doxorubicin. Compound 8d against both the cancer cell lines, 8q against MCF-7 and 8c, 8h against HepG2 have also shown good activity. Remaining compounds have shown moderate activity against both the cell lines. Antimicrobial activity revealed that, the compound 8q and 8t against Staphylococcus aureus and 8i, 8k, 8l, 8q & 8t against Klebsiella pneumoniae have shown equipotent activity on comparing with the standard drug Streptomycin. Remaining compounds have shown significant antibacterial and comparable antifungal activities against all the tested microorganisms.
Design, synthesis, and interaction study of quinazoline-2(1 H)-thione derivatives as novel potential Bcl-xL inhibitors
Feng, Yu,Ding, Xiao,Chen, Tao,Chen, Lili,Liu, Fang,Jia, Xu,Luo, Xiaomin,Shen, Xu,Chen, Kaixian,Jiang, Hualiang,Wang, Hui,Liu, Hong,Liu, Dongxiang
experimental part, p. 3465 - 3479 (2010/09/05)
Development of inhibitors to antagonize the activities of antiapoptotic Bcl-2 family proteins is of particular interest in cancer chemotherapy. We discovered a quinazoline-2(1H)-thione derivative (DCBL55) as a new Bcl-x L, Bcl-2, and Mcl-1 inhi
