67152-20-9Relevant academic research and scientific papers
Preparation method of fluorine-containing aryl compound
-
Paragraph 0151-0158, (2021/06/12)
The invention relates to the field of organic synthesis, and especially relates to a preparation method of a fluorine-containing aryl compound. The invention provides a preparation method of a compound as shown in a formula 1. The preparation method comprises the following steps: fluorination reaction: reacting a compound as shown in a formula 2 with alkali metal fluoride in the presence of a phase transfer catalyst to prepare the compound as shown in the formula 1. According to the preparation method of the fluorine-containing aryl compound provided by the invention, a reaction system does not contain a solvent, the boiling point of the phase transfer catalyst is relatively high, solvent interference is avoided during rectification or short steaming after the reaction is finished, the distillation yield is high, and the product purity is good.
A 4, 6 - double-halogenated isophthalonitrile preparation method (by machine translation)
-
Paragraph 0106; 0107; 0138; 0139, (2017/07/21)
The present invention relates to the technical field of the synthesis of pharmaceutical intermediates, in particular to a 4, 6 - double-halogenated isophthalonitrile preparation method, through the use of cheap and easily obtained 2, 4 - double-halo benzoic acid as the raw material, the reaction of the halide, the amidation reaction, dehydration reaction, the nitration reaction, reduction reaction, the diazotization reaction, the substitution reaction for the synthesis of 4, 6 - double-halogenated isophthalonitrile; the total yield can be 21.5%. The process route is easily obtained and cheap materials, few by-products, the purification treatment is the process is simple, easy to realize industrial production. (by machine translation)
CHEMICAL COMPOUNDS
-
Page/Page column 59, (2008/06/13)
This invention relates to novel compounds having the formula (I); and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.
CHEMICAL COMPOUNDS
-
Page/Page column 40, (2008/06/13)
This invention relates to novel compounds having the formul and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.
2-(2-Hydroxy-3-alkoxyphenyl)-1H-benzimidazole-5-carboxamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors
Mackman, Richard L.,Hui, Hon C.,Breitenbucher,Katz, Bradley A.,Luong, Christine,Martelli, Arnold,McGee, Danny,Radika, Kesavan,Sendzik, Martin,Spencer, Jeffrey R.,Sprengeler, Paul A.,Tario, James,Verner, Erik,Wang, Jing
, p. 2019 - 2022 (2007/10/03)
The development of potent and selective urokinase-type plasminogen activator (uPA) inhibitors based on the lead molecule 2-(2-hydroxy-3-ethoxyphenyl)-1H-benzimidazole-5-carboxamidine (3a) is described.
Compounds and compositions as anticoagulants
-
, (2008/06/13)
The present invention relates to novel biheterocyclic derivatives which are factor Xa inhibitors; the pharmaceutically acceptable salts and N-oxides thereof; their uses as therapeutic agents and the methods of their making.
6-(1H-imidazol-1-yl)-7-nitro-2,3 (1H,4H)-quinoxalinedione hydrochloride (YM90K) and related compounds: Structure-activity relationships for the AMPA- type non-NMDA receptor
Ohmori,Sakamoto,Kubota,Shimizu-Sasamata,Okada,Kawasaki,Hidaka,Togami,Furuya,Murase
, p. 467 - 475 (2007/10/02)
A novel series of quinoxalinediones possessing imidazolyl and related heteroaromatic substituents was synthesized and evaluated for their activity to inhibit [3H]AMPA binding from rat whole brain. From the structure- activity relationships, it was found that the 1H-imidazol-1-yl moiety could function as a bioisostere for the cyano and nitro groups, and that 6-(1H- imidazol-yl)-7-nitro-2,3(1H,4H)-quinoxalinedione (11) showed the most potent activity for the AMPA receptor. Compound 11 was evaluated for selectivity versus other excitatory amino acid receptors, and its action against AMPA at its receptor in the rat striatum was characterized. These data showed that compound 11 was a selective antagonist for the AMPA receptor with a K(i) value of 0.084 μM, being approximately equipotent with 2,3-dihydro-6-nitro- 7-sulfamoylbenzo(f)quinoxaline (3) (NBQX; K(i) = 0.060 μM). Compound 11 was also found to give protection against sound-induced seizure on DBA/2 mice at the minimum effective dose of 3 mg/kg ip (3; 10 mg/kg ip).
