7170-38-9Relevant articles and documents
Acid activated montmorillonite K-10 mediated intramolecular acylation: Simple and convenient synthesis of 4-chromanones
Begum, Ayisha F.,Balasubramanian, Kalpattu K.,Shanmugasundaram, Bhagavathy
supporting information, (2021/09/13)
3-Aryloxyproionic acids undergo intramolecular cyclization in the presence of AA.Mont.K-10 in toluene under reflux for 30–45 min in good to excellent yields. Phenyl ring bearing various substituents at the ortho, meta, para positions undergo this cyclization reaction. This method involves simple work up and amenable for large scale preparations. The heterogeneous acid treated catalyst can be regenerated and used for up to three cycles with minimum loss of activity.
Chroman-4-one hydrazones derivatives: synthesis, characterization, and in vitro and in vivo antileishmanial effects
Upegui, Yulieth,Rios, Karina,Qui?ones, Wiston,Echeverri, Fernando,Archbold, Rosendo,Murillo, Javier D.,Torres, Fernando,Escobar, Gustavo,Vélez, Iván D.,Robledo, Sara M.
, p. 2184 - 2199 (2019/11/03)
In searching for better therapeutic alternatives to treat cutaneous leishmaniasis (CL), this study aimed to obtain and evaluate the efficacy and toxicity of new chroman-4-one hydrazones derivatives. Compounds were prepared and characterized, and then transformed into hydrazonas for molecular optimization. Their cytotoxicity was tested in different cell types using an in vitro MTT assay and the efficacy was evaluated using an in vitro macrophage intracellular amastigotes of Leishmania (Viannia) panamensis and L. (V) braziliensis by flow cytometry. The therapeutic effect of two formulations of chroman-4-one hydrazones on the CL induced by L. (V) braziliensis in golden hamsters was determined according to the size of lesions after treatment. The effect of these compounds in the production of inflammatory mediators and cell migration was also determined by in vitro assays using human fibroblasts models. Neither cytotoxicity nor genotoxicity was observed. The benzoic acid hydrazone derivative 2-(2,3-dihydro-4H-1-benzopyran-4-ylidene) hydrazide (4), produced a higher percentage of clinical cures, followed by benzoic acid, 2-(2,3-dihydro-4H-1-benzothiopyran-4-ylidene) hydrazide (3), while benzoic acid, 2-(2,3-dihydro-1,1-dioxide-4H-1-benzothiopyran-4-ylidene) hydrazide (5) and 4-pyridinecarboxylic acid, 2-(4H-1-benzopyran-4-ylidene) hydrazide (6) caused a poor therapeutic response. The compound 4 also showed an effect in the inflammatory and fibroblast migration processes. In conclusion, this is the first report of antileishmanial activity combined with inflammatory and wound healing properties. Results obtained here suggest that this strategy could be a good alternative for development of new drugs for the treatment of CL.
Microchannel reactor-based cyano hydrolysis reaction method
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Paragraph 0099-0108, (2018/08/04)
The invention discloses a microchannel reactor-based cyano compound hydrolysis reaction method, and particularly, a compound comprising a cyano group in the molecule has the cyano hydrolysis reactionby using a microchannel reactor under the action of alkaline or acid-alkaline substances. By using the microchannel reactor in the process, the raw material is instantaneously evenly mixed and efficiently transfers heat; the most important danger of rushing of the material in the production process, caused by hydrolysis of the cyano compound through the alkali, is avoided; meanwhile, the equivalence ratio of the raw material in the reaction process is also reduced; the side reaction is reduced; the reaction time is shortened to dozens of minutes or even dozens of seconds. In a word, the process improves the operation safety of the reaction, the safe enlarged production of the cyano compound is realized, the time for the hydrolysis reaction of the cyano compound is shortened, the reaction selectivity and the reaction efficiency are improved, the energy consumption of the production is reduced, the use ratio of the raw material is increased, the production process is more environmentallyfriendly, the production cost is low, meanwhile, the used equipment occupies a small area, the production capacity of the equipment is high, and the production efficiency and the production capacityare greatly improved.
