Accelerating lead development by microwave-enhanced medicinal chemistry

William D Shipe; Scott E Wolkenberg; Craig W Lindsley

doi:10.1016/j.ddtec.2005.05.002

Accelerating lead development by microwave-enhanced medicinal chemistry

Drug Discov Today Technol. 2005 Summer;2(2):155-61. doi: 10.1016/j.ddtec.2005.05.002.

Authors

William D Shipe¹, Scott E Wolkenberg¹, Craig W Lindsley²

Affiliations

¹ Merck Research Laboratories, Department of Medicinal Chemistry, West Point, PA 19486, USA.
² Merck Research Laboratories, Department of Medicinal Chemistry, West Point, PA 19486, USA. Electronic address:craig_lindsley@merck.com.

PMID: 24981843
DOI: 10.1016/j.ddtec.2005.05.002

Abstract

Microwave-assisted organic synthesis (MAOS) addresses the need for accelerated chemical synthesis by providing many advantages over classical thermal conditions. Microwave instruments produced by Biotage, CEM and Milestone enable chemistry to be safely and reproducibly performed on various scales and in a parallel fashion. To illustrate the high utility of this technology for lead development, our Akt kinase program will be described wherein MAOS played a pivotal role in the identification of isozyme-selective Akt inhibitors.: