Continuous flow (CF) chemistry has enjoyed considerable progress during the last two decades.1 With the mainstream success of microwave chemistry in its rear mirror, these two fields have taken separates lanes in their development, with only few exceptions where modified single-mode batch, or multi-mode microwave equipment have been utilized as the heating source. We find the prospect of a microwave applicator fully dedicated to CF applications to offer many advantages over traditional heating methods, such as fast and controlled heating and a higher level of safety regarding explosive reagents and pressure-producing reactions.A few inhibitors of insulin-regulated aminopeptidase (IRAP), also known as the AT?4 receptor have been reported.2 IRAP is a novel target for cognitive enhancers, and administration of inhibitors has resulted in facilitation of memory and enhanced performance in spatial memory tasks. Thus, there is a need for new more drug-like compounds that can be used as pharmacological tools. We will present the synthesis of some new small compounds that inhibit IRAP. The synthesis is performed with a unique non-resonant microwave heating applicator purpose-built for CF. This device heats the entire borosilicate (MW-transparent) or Si/C (MW-absorbing) tube reactor without pronounced hot and cold spots (Figure 1), allowing method development in small scale and subsequent scale-out without scale-up translation. Figure 1.   Thermal image of MW-heated reactors, borosilicate (left) and Si/C (right).(1) �hrngren, P.; Fardost, A.; Russo, F.; Schanche, J.-S.; Fagrell, M.; Larhed, M. Org. Process Res. Dev. 2012  , 16, 1053�1063.(2) Andersson, H.; Hallberg, M. Int. J. Hypertens. 2012  , 2012, 789671.

Nonresonant microwave heated continuous flow synthesis in medicinal chemistry

248th National Meeting (2014)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.