Journal of Medicinal Chemistry p. 1854 - 1868 (2016)
Update date:2022-07-29
Topics:
Sergeyev, Sergey
Yadav, Ashok Kumar
Franck, Philippe
Michiels, Johan
Lewi, Paul
Heeres, Jan
Vanham, Guido
Ari?n, Kevin K.
Vande Velde, Christophe M. L.
De Winter, Hans
Maes, Bert U. W.
New non-nucleoside reverse transcriptase inhibitors (NNRTI), which are similar in structure to earlier described di(arylamino)pyrimidines but featuring a 2,6-di(arylamino)-3-fluoropyridine, 2,4-di(arylamino)-5-fluoropyrimidine, or 1,3-di(arylamino)-4-fluorobenzene moiety instead of a 2,4-disubstituted pyrimidine moiety, are reported. The short and practical synthesis of novel NNRTI relies on two sequential Pd-catalyzed aminations as the key steps. It is demonstrated through direct comparison with reference compounds that the presence of a fluorine atom increases the in vitro anti-HIV activity, both against the wild type virus and drug-resistant mutant strains.
View MoreChangzhou Screw International Trading Co., Ltd.
Contact:13906149256,18001495888
Address:Jiangsu,Jintanqu
Beijing Century Richap Chemistry Co.,Ltd
Contact:+86- 010-64455497
Address:Guannan County, Lianyungang City, Jiangsu Province, China
SHANDONG ZHANHUA YONGHAO PHARMACEUTICAL TECH.CO.,LTD
Contact:+86-576-88685096
Address:GENGJU VILLAGE NORTH ONE KILOMETER,ZHANHUA DISTRICT,BINZHOU CITY,SHANDONG PROVINCE,CHINA.
Contact:+86-27-87204219, +86-27-87215023
Address:2402, HuiGu Space-time Building, 8 Forest Road, East Lake Hi-Tech Development Zone
Shanghai Witshoot Internet Technology Co Ltd
Contact:+86-21-66390020
Address:Room 419, No.285 Luochuan Road (E)
Doi:10.1002/adsc.201100809
(2012)Doi:10.1016/S0040-4039(00)99273-6
(1989)Doi:10.1246/cl.2010.1052
(2010)Doi:10.1016/S0040-4039(00)61634-9
(1993)Doi:10.1039/c0nj00586j
(2010)Doi:10.1039/c39920000341
(1992)