118-29-6Relevant articles and documents
Synthesis, α-glucosidase inhibition and molecular docking studies of novel thiazolidine-2,4-dione or rhodanine derivatives
Wang, Guang-Cheng,Peng, Ya-Ping,Xie, Zhen-Zhen,Wang, Jing,Chen, Ming
, p. 1477 - 1484 (2017)
A series of novel thiazolidine-2,4-dione or rhodanine derivatives (5a-5k, 6a-6k) were synthesized and evaluated for their α-glucosidase inhibitory activity. The majority of compounds exhibited potent inhibitory activity in the range of 5.44 ± 0.13 to 50.45 ± 0.39 μM, when compared to the standard drug acarbose (IC50 = 817.38 ± 6.27 μM). Among the compounds in the series, compounds 5k, 6a, 6b, 6e, 6h and 6k showed potent inhibitory potential with IC50 values of 20.95 ± 0.21, 16.11 ± 0.19, 7.72 ± 0.16, 7.91 ± 0.17, 6.59 ± 0.15 and 5.44 ± 0.13 μM, respectively. Compound 6k (IC50 = 5.44 ± 0.13 μM), containing chloro and rhodanine groups at the 2- and 4-positions of the phenyl ring respectively, was found to be the most active compound that inhibits α-glucosidase activity. Furthermore, molecular docking studies were performed to understand the binding interactions between the molecule and enzyme.
-
Mitta et al.
, p. 20,22 (1967)
-
-
Sakellarios
, p. 2822 (1948)
-
Bi(OTf)3-Catalysed Access to 2,3-Substituted Isoindolinones and Tricyclic N,O-Acetals by Trapping of Bis-N-Acyliminium Species in a Tandem Process
Aliyenne, Ahmed,Pin, Frédéric,Nimbarte, Vijaykumar D.,Lawson, Ata Martin,Comesse, Sébastien,Sanselme, Morgane,Tognetti, Vincent,Joubert, Laurent,Da?ch, Adam
, p. 3592 - 3602 (2016)
New 1,3-bis-N-acyliminium species generated easily with nontoxic Bi(OTf)3catalyst at very low loadings (2 mol-%) were trapped inter- and intramolecularly with various poly-nucleophiles. This mild, efficient, practical and general tandem approach provides an array of substituted isoindolinones and cyclic N,O-acetals.
Synthesis of soft alkyl phenolic ether prodrugs using Mitsunobu chemistry
Majumdar, Susruta,Juntunen, Juha,Sivendran, Sashi,Bharti, Neelam,Sloan
, p. 8981 - 8982 (2006)
The synthesis of soft alkyl phenolic ether prodrugs in excellent yields has been reported by coupling a phenol with a hydroxymethylimide using Mitsunobu chemistry. The imides used in this study include saccharin, phthalimide, succinimide and two other compounds containing acidic imide-like N-H groups, benzotriazole, and imidazole.
The novel product of cathodic reduction of phthalimide anion
Orzeszko, Andrzej,Maurin, Jan K.,Niedzwiecka-Kornas, Anna,Kazimierczuk, Zygmunt
, p. 7517 - 7524 (1998)
Cathodic reduction of phthalimide anion in methanol was studied. The novel product, N-hydroxymethyl-3-hydroxyphthalimidine, was found. Full characterization of this new compound was carried out by means of NMR, FT- IR, MS, and X-ray crystallography. The mechanism of electrolytic formation of N-hydroxymethyl-3-hydroxyphthalimidine is proposed.
Synthetic method N - hydroxymethyl phthalimide
-
Paragraph 0011-0021, (2021/08/25)
The invention discloses a method for synthesizing N - hydroxymethyl phthalimide, wherein phthalimide and solid paraformaldehyde are used as raw materials, water is used as a solvent, and N - hydroxymethyl phthalimide is prepared through reflux reaction. The filtered water produced by the reaction does not need to be treated and can be recycled to the next batch production, and the process itself realizes zero emission. The solid polyformaldehyde is used in the invention, so that the raw materials are transported. The links of storage, use and the like are safe and reliable, VOCS emission is reduced, and the sustainable development direction of clean production is represented. The process realizes the molar conversion rate of up to 98%, and the purity of the product reaches 99% or above.
Synthesis method of N-hydroxymethyl-3, 4, 5, 6-tetrahydrophthalimide
-
Paragraph 0010; 0030-0035; 0040-0045, (2021/06/13)
The invention discloses a synthesis method of N-hydroxymethyl-3, 4, 5, 6-tetrahydrophthalimide, which comprises the following steps of adding phthalimide and tetrabutylammonium bromide into water, dropwise adding a formaldehyde aqueous solution after adding, carrying out heat preservation reaction after dropwise adding, drying a solvent after reaction, recrystallizing by using an acetone aqueous solution, putting the recrystallized material into a high-pressure kettle, adding Pd/C, introducing hydrogen, conducting heat preservation and pressure retaining reaction, desiccating the solvent and recrystallizing toluene after the reaction is finished. According to the method, the two-step synthesis yield of the method can reach 80% or above, and the normalized content of a product liquid spectrum can reach 97.6%. The solvent used in the method can be used in a reaction system after being recycled, the reduction catalyst can be used for more than 10 times, and the method is simple in process, easy to operate, high in reaction selectivity, low in product yield, quality and energy consumption and free of phosphorus and nitrogen-containing wastewater, the production field environment is remarkably improved, and industrial clean production is facilitated.