39070-63-8Relevant articles and documents
A preparing method of a mebendazole intermediate (3,4-diaminophenyl)phenyl methanone
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Paragraph 0064-0066, (2017/06/14)
A preparing method of a mebendazole intermediate (3,4-diaminophenyl)phenyl methanone is disclosed. The method includes adding 4-amino-3-nitro diphenylmethanone and a catalyst into an organic solvent, adding a hydrogen donor, and performing transfer hydrogenation reduction to obtain the (3,4-diaminophenyl)phenyl methanone, wherein the catalyst is a Pd-X/C catalyst, and the X is one of Ni, Ru, La, Ce, Co, Li, K, Mg, Ti, Cu or Mo. The method has advantages of mild conditions, simple operation, a high reduction rate, a low cost, high environment protection performance, easy industrial production, and the like.
Design and synthesis of a novel candidate compound NTI-007 targeting sodium taurocholate cotransporting polypeptide [NTCP]-APOA1-HBx-Beclin1-mediated autophagic pathway in HBV therapy
Zhang, Jin,Fu, Lei-Lei,Tian, Mao,Liu, Hao-Qiu,Li, Jing-Jing,Li, Yan,He, Jun,Huang, Jian,Ouyang, Liang,Gao, Hui-Yuan,Wang, Jin-Hui
, p. 976 - 984 (2015/03/04)
Sodium taurocholate cotransporting polypeptide (NTCP) is a multiple transmembrane transporter predominantly expressed in the liver, functioning as a functional receptor for HBV. Through our continuous efforts to identify NTCP as a novel HBV target, we designed and synthesized a series of new compounds based on the structure of our previous compound NT-5. Molecular docking and MD simulation validated that a new compound named NTI-007 can tightly bind to NTCP, whose efficacy was also measured in vitro virological examination and cytotoxicity studies. Furthermore, autophagy was observed in NTI-007 incubated HepG2.2.15 cells, and results of q-PCR and Western blotting revealed that NTI-007 induced autophagy through NTCP-APOA1-HBx-Beclin1-mediated pathway. Taken together, considering crucial role of NTCP in HBV infection, NTCP-mediated autophagic pathway may provide a promising strategy of HBV therapy and given efficacy of NTI-007 triggering autophagy. Our study suggests pre-clinical potential of this compound as a novel anti-HBV drug candidate.
6-Lithioquinoxalines and Their Transformations
Dobrodei,El'tsov
, p. 620 - 629 (2007/10/03)
6-Bromo-2,3-diphenylquinoxaline reacts with butyllithium to give the 6-lithio derivative in a yield of more than 80%, which reacts with electrophiles such as benzophenone, Michler ketone, methyl ethyl ketone, iodine, selenium, and dimethylformamide to give the corresponding quinoxaline derivatives. 6-Bromo-2,3-dimethylquinoxaline is metallated with butyl- and phenyllithium at the methyl groups and benzene ring. These organolithium compounds react with benzophenone to give the corresponding diphenyl- and triaryl-carbinols, whose yield and ratio were determined by HPLC. These results open prospects for preparing new quinoxaline derivatives substituted at the annelated benzene ring.