6639-79-8Relevant articles and documents
Novel molecular targeting anti-tumor aza-steroid derivative based on lipid toxicity and preparation and application thereof
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Paragraph 0178; 0180; 0181; 0192; 0221, (2021/08/19)
The invention provides a novel molecular targeting anti-tumor aza-steroid derivative based on lipid toxicity and a preparation method and application thereof, and belongs to the field of chemical medicines. The derivative is a compound as shown in a formula I, or a salt thereof, or a stereoisomer thereof. The compound is low in toxicity or basically non-toxic to normal cells, has an obvious inhibition effect to tumor cell lines, particularly has good lipid toxicity selectivity to tumor cells such as liver cancer, lung cancer and the like in vivo, and has an obvious inhibition effect; meanwhile, the compound can effectively activate SREBP1 and PPAR gamma, inhibit lipid transport MTTP, cause lipid aggregation in tumor cells and cause lipid toxicity of the tumor cells. The compound can be used for treating liver cancer, lung cancer and the like in a molecular targeting manner, is low in toxicity or even non-toxic, and has a good application prospect.
Synthesis method of 2,3-dihydroxy-6-chloroquinoxaline
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Paragraph 0028-0044, (2020/08/06)
The invention relates to a synthetic method of 2,3-dihydroxy-6-chloroquinoxaline, and belongs to the technical field of organic synthesis. The synthesis method comprises the following synthesis steps:(1) adding 4-chloro-o-phenylene diamine, diethyl oxalate and an alkali into a reaction flask, controlling a reaction system to be at a negative pressure, and heating a reaction solution to reflux tostart a reaction; (2) after the reaction is finished, adding active carbon for de-coloration, and performing hot filtration to obtain filtrate I; (3) cooling the filtrate I obtained in the step (2) to0-5 DEG C, crystallizing for 1-2 hours, and filtering to obtain a filter cake. The method has the advantages that (1) the side reactions are reduced by reducing the reaction temperature; (2) the reaction substrate is activated by using an alkali, so that the reaction is promoted; (3) a byproduct namely ethanol is extracted through rectification to promote forward proceeding of the reaction, so that the reaction time is shortened; and (4) the product quality is improved, and a 2,3-dihydroxy-6-chloroquinoxaline standard substance meeting the requirements is obtained.
Rationalization of benzazole-2-carboxylate versus benzazine-3-one/ benzazine-2,3-dione selectivity switch during cyclocondensation of 2-aminothiophenols/phenols/anilines with 1,2-biselectrophiles in aqueous medium
Dhameliya, Tejas M.,Chourasiya, Sumit S.,Mishra, Eshan,Jadhavar, Pradeep S.,Bharatam, Prasad V.,Chakraborti, Asit K.
, p. 10077 - 10091 (2018/05/31)
The cyclocondensation reaction of 2-aminothiophenols with 1,2-biselectrophiles such as ethyl glyoxalate and diethyl oxalate in aqueous medium leads to the formation of benzothiazole-2-carboxylates via the 5-endo-trig process contrary to Baldwin's rule. On the other hand, the reaction of 2-aminophenols/anilines produced the corresponding benzazine-3-ones or benzazine-2,3-diones via the 6-exo-trig process in compliance with Baldwin's rule. The mechanistic insights of these cyclocondensation reactions using the hard-soft acid-base principle, quantum chemical calculations (density functional theory), and orbital interaction studies rationalize the selectivity switch of benzothiazole-2-carboxylates versus benzazine-3-ones/ benzazine-2,3-diones. The presence of water facilitates these cyclocondensation reactions by lowering of the energy barrier.
