ACS Combinatorial Science p. 672 - 680 (2018)
Update date:2022-08-04
Topics:
Tolmachova, Kateryna A.
Moroz, Yurii S.
Konovets, Angelika
Platonov, Maxim O.
Vasylchenko, Oleksandr V.
Borysko, Petro
Zozulya, Sergey
Gryniukova, Anastasia
Bogolubsky, Andrey V.
Pipko, Sergey
Mykhailiuk, Pavel K.
Brovarets, Volodymyr S.
Grygorenko, Oleksandr O.
Multigram synthesis of (chlorosulfonyl)benzenesulfonyl fluorides is described. Selective modification of these building blocks at the sulfonyl chloride function under parallel synthesis conditions is achieved. It is shown that the reaction scope includes the use of (hetero)aromatic and electron-poor aliphatic amines (e.g., amino nitriles). Utility of the method is demonstrated by preparation of the sulfonyl fluoride library for potential use as covalent fragments, which is demonstrated by a combination of in silico and in vitro screening against trypsin as a model enzyme. As a result, several inhibitors were identified with activity on par with that of the known inhibitor.
View Morewebsite:http://www.shengmaochem.com
Contact:86-27-82853423, 82819281
Address:Rm 202, A Unit Huaqiao Building No. 2, Lihuangpi Road, Wuhan, China
Shandong united-rising pharmaceutical cooperation.,ltd.
Contact:008653187965009
Address:171No., Jing5 Road, Shizhong District, Jinan, China
Beijing Mashi Fine Chemical Co.,Ltd.
Contact:+86-10-61271592
Address:Room 506, Section B, Kaichi Mansion, Industrial Development
website:http://www.afinechem.com
Contact:+86-571-85134551
Address:No. 206 Zhen Hua Road, Hangzhou 310030, Zhejiang, China
ANHUI CHEM-BRIGHT BIOENGINEERING CO.,LTD
Contact:86-561-4080321
Address:No.8 Lieshan Industrial Zone of Huaibei
Doi:10.1021/jo00818a014
(1971)Doi:10.1021/jo0011383
(2000)Doi:10.1016/0040-4020(96)00799-5
(1996)Doi:10.1016/S0040-4039(00)99974-X
(1970)Doi:10.1016/S0040-4039(00)01220-X
(2000)Doi:10.1002/1521-3765(20000915)6:18<3426::AID-CHEM3426>3.0.CO;2-B
(2000)