Chimia p. 262 - 269 (2003)
Update date:2022-07-29
Topics:
Altorfer, Michael
Ermert, Philipp
Faessler, Juerg
Farooq, Saleem
Hillesheim, Elke
Jeanguenat, Andre
Klumpp, Klaus
Maienfisch, Peter
Martin, Joseph A.
Merrett, John H.
Parkes, Kevin E.B.
Obrecht, Jean-Pierre
Pitterna, Thomas
Obrecht, Daniel
Parallel synthesis of focused compound libraries for hit confirmation and lead optimization are certainly important drivers for shortening the lead discovery phase in the pharmaceutical and crop protection industries. In this article we show with permission of Roche and Syngenta three real case studies where Polyphor synthesized focused libraries for lead validation and optimization using high-throughput parallel synthesis and purification techniques. The three examples differ significantly in the synthetic strategies which were employed as well as in the chemical complexity of the final products. A multigeneration approach towards insecticidal triazines, the application of a sequential three-component reaction towards insecticidal and fungicidal thiazoles and finally a multistep synthesis approach of advanced building blocks followed by a two-step final derivatization towards novel antiviral N-hydroxy-indolin-2-ones are presented. In all cases 100-200 analogues were synthesized using parallel synthesis in solution followed by purification of the final products by parallel flash or high-throughput (unattended) HPLC (coupled to MS) within four months. Promising biological results were obtained in all three cases.
View Morewebsite:http://www.hanwayschem.com
Contact:+86-18502787239(whatsapp)
Address:18-1-802, Green Garden, Jianghan District, Wuhan 430023, China
website:http://www.simagchem.com
Contact:+86-592-2680277
Address:21/F Hualong Office Building,No.6 Hubin East Road, Xiamen,China
Beijing Apis Biotechnology Co., Ltd.
Contact:86-010-67856775-8551
Address:NO.4PUHUANGYU ROAD,FENTAI DISTRICT, BEIJING, CHINA
Angelisun(Chongqing) Pharmaceutical Co., LTD.
Contact:+86-23-68030926-816
Address:D1-7 Tech & Entrepreneurs Park, Kecheng Road, Erlang Hi-Tech Areas, Chongqing, China
Chengdu Gelipu Biotechnology Co., Ltd.
website:http://www.glp-china.com
Contact:86-28-82610909
Address:chegndu
Doi:10.1021/ja01303a048
(1936)Doi:10.1021/jo0265129
(2003)Doi:10.1246/cl.2003.34
(2003)Doi:10.1055/s-0037-1611577
(2019)Doi:10.1007/s00044-018-2267-9
(2019)Doi:10.1246/bcsj.78.1121
(2005)