641-70-3Relevant academic research and scientific papers
Solvent-free synthesis of new chalcone derivatives from 3-nitro phthalic acid and evaluation of their biological activities
Ahamed, Luma S.,Ali, Rana Abid,Ahmed, Rana S.
, p. 2963 - 2968 (2021/05/28)
Synthesis of 2-(4-Acetyl-phenyl)-4-nitro-isoindole-1, 3-dione chalcones were performed by fusion of 3-nitro phthalic anhydride with p-aminoacetophenone. Then the later was grinded with different aromatic aldehydes in the presence of sodium hydroxide to produce new chalcones derivatives A3-10 without using any solvent formation of new Narylphthailimide chalcones were confirmed by FT-IR,1HNMR, 13CNMR spectroscopy and all final compounds were tested for their antifungal and antibacterial activity some of them showed more biological activity than the standard drugs.
ANTIVIRAL 1,3-DI-OXO-INDENE COMPOUNDS
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Paragraph 0239-0240, (2021/10/22)
This disclosure provides compounds of Formula (I) as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and methods to use these compounds, salts and compositions for treating viral infections.
ANTIVIRAL 1,3-DI-OXO-INDENE COMPOUNDS
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Paragraph 0264, (2021/10/22)
The invention provides compounds of Formula (I): as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and methods to use these compounds, salts and compositions for treating viral infections.
Synthesis process for continuously preparing pomalidomide by using microchannel reactors
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Paragraph 0052-0054, (2020/03/06)
The invention discloses a synthesis process for continuously preparing pomalidomide by using microchannel reactors. The synthesis process comprises the following steps tha (1) 3-nitrophthalic acid isdissolved in acetic anhydride, and a reaction is performed to obtain 3-nitrophthalic anhydride; (2) 3-nitrophthalic anhydride is dissolved in formic acid to prepare a homogeneous solution A; (3) 3-aminopiperidine-2,6-dione is dissolved in ammonium formate and formic acid to prepare a homogeneous solution B; (4) palladium on carbon and methanol are prepared into suspension C; (5) the homogeneous solution A and the homogeneous solution B are simultaneously pumped into a microstructured mixer I in a microchannel reaction device separately, and after mixing, the mixture is introduced into a microstructured reactor I; (6) the suspension C and an effluent from the microstructured reactor I are simultaneously pumped into a microstructured mixer II in the microchannel reaction device separately while the step (5) is carried out, and after mixing, the mixture is introduced into a microstructured reactor II; and (7) an effluent from the microstructured reactor II is collected to obtain pomalidomide.
Preparation method of 3-nitrophthalic anhydride
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Paragraph 0013-0015, (2019/04/10)
The invention relates to a preparation method of 3-nitrophthalic anhydride. The method includes the following steps: placing 3-nitrophthalic acid in a reaction solvent, adding a catalyst, and heatingfor reaction; and removing the reaction solvent and the catalyst from an obtained substance under negative pressure to obtain the 3-nitrophthalic anhydride. In the preparation method, the 3-nitrophthalic acid raw material can be easily obtained, the 3-nitrophthalic anhydride is synthesized by direct catalytic dehydration in one step, and the preparation method has the advantages of simple process,low cost, high yield and no by-products.
Synthesis and chemiluminescent properties of amino-acylated luminol derivatives bearing phosphonium cations
Pantelia, Anna,Daskalaki, Ira,Consuelo Cuquerella,Rotas, Georgios,Miranda, Miguel A.,Vougioukalakis, Georgios C.
, (2019/11/11)
The monitoring of reactive oxygen species in living cells provides valuable information on cell function and performance. Lately, the development of chemiluminescence-based reactive oxygen species monitoring has gained increased attention due to the advantages posed by chemiluminescence, including its rapid measurement and high sensitivity. In this respect, specific organelle-targeting trackers with strong chemiluminescence performance are of high importance. We herein report the synthesis and chemiluminescence properties of eight novel phosphonium-functionalized amino-acylated luminol and isoluminol derivatives, designed as mitochondriotropic chemiluminescence reactive oxygen species trackers. Three different phosphonium cationic moieties were employed (phenyl, p-tolyl, and cyclohexyl), as well as two alkanoyl chains (hexanoyl and undecanoyl) as bridges/linkers. Synthesis is accomplished via the acylation of the corresponding phthalimides, as phthalhydrazide precursors, followed by hydrazinolysis. This method was chosen because the direct acylation of (iso)luminol was discouraging. The new derivatives’ chemiluminescence was evaluated and compared with that of the parent molecules. A relatively poor chemiluminescence performance was observed for all derivatives, with the isoluminol-based ones being the poorest. This result is mainly attributed to the low yield of the fluorescence species formation during the chemiluminescence oxidation reaction.
Preparation method of 3-nitrophthalic anhydride
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Paragraph 0021; 0023; 0024; 0026; 0028; 0030; 0033, (2018/11/22)
Belonging to the field of fine chemical industry, the invention discloses a preparation method of 3-nitrophthalic anhydride. The method provided by the invention adopts 3-nitrophthalic acid as the starting raw material, carries out Vilsmeier reaction with acyl chloride under the action of a catalyst to obtain 3-nitrophthalic anhydride. The invention screens different acyl chlorides, different solvents and different amide reaction conditions, at the same time avoids use of dangerous and national precursor controlled chemicals in the compound preparation process, and makes the preparation process unrestricted. In the preparation process, the organic solvent can be recycled, the production cost is reduced, at the same time the post-treatment is economical and simple, and the product has highyield and purity.
Discovery of Wogonin-based PROTACs against CDK9 and capable of achieving antitumor activity
Bian, Jinlei,Ren, Jie,Li, Yongren,Wang, Jubo,Xu, Xi,Feng, Yifan,Tang, Hui,Wang, Yajing,Li, Zhiyu
supporting information, p. 373 - 381 (2018/10/08)
Wogonin is a natural product isolated from the Scutellaria baicalensis and has been proved to be a potent and selective inhibitor of CDK9. Using this scaffold, we designed and synthesized a series of proteolysis targeting chimeras (PROTACs) targeting CDK9 by recruiting ubiquitin E3 ligase cereblon (CRBN). For constructing diverse Wogonin-based PROTACs, a “click chemistry” approach was employed for the synthesis of CDK9-targeting PROTACs. The results of western blotting assays showed that compounds containing triazole group in the linker could selectively downregulate the intracellular CDK9 level. Among these compounds, 11c could selectively degrade CDK9 in a concentration-dependent manner. In addition, the application of the proteasome inhibitor MG132 and CRBN siRNA silencing confirmed that 11c could promote the proteasome-dependent and CRBN-dependent degradation. Consistent with the degradation of the CDK9 protein, 11c selectively inhibits proliferation of CDK9-overexpressed cancer cells. Thus, our Wogonin-based PROTAC would be an efficient probe that induces the degradation of CDK9.
A 3 - phthalic acid synthetic method (by machine translation)
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Paragraph 0015; 0021; 0022, (2018/10/19)
The invention discloses a 3 - phthalic acid synthetic method, the raw material 3 - nitrophthalic acid is dissolved by acetyl chloride solvent dehydration is carried out, after the dehydration by the fluorination potassium [...], then adding thionyl chloride to remove the by-product generated in the process of fluoro, purification to obtain the target compound 3 - phthalic acid. The invention relates to 3 - nitrophthalic acid as the synthetic 3 - phthalic acid raw material, the raw material is cheap, simple process, high yield; by adjusting the PH of the method, the product from the sulfolane solvent in very good separation out, solves the high boiling point of the solvent is not easily evaporated difficult; using acetyl chloride as dehydration solvent, not only replacing the drug control acetic anhydride, but also reduces the acetic anhydride in the dehydration process of the acetic acid by-product, mild reaction conditions after processing is simple and convenient. (by machine translation)
