Synthesis 2015; 47(06): 760-768
DOI: 10.1055/s-0034-1379733
short review
© Georg Thieme Verlag Stuttgart · New York

Popular Synthetic Approaches To Pharmaceuticals

David J. Ager*
DSM ChemTech R&D BV, PMB 150, 9650 Strickland Road Suite 103, Raleigh, NC 27615, USA   eMail: david.ager@dsm.com
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Publikationsverlauf

Received: 01. Juli 2014

Accepted after revision: 24. November 2014

Publikationsdatum:
22. Dezember 2014 (online)


Abstract

The pharmaceutical industry continues to look at the use of ‘green’ methods, including those that allow for shorter synthetic sequences. The use of biocatalysis continues to grow, including transformations that are difficult to perform by standard chemical means. Flow reactions are also growing in popularity, as the equipment becomes available at all scales. The use of flow techniques also allows for the use of high temperatures and pressures, as well as the preparation of hazardous intermediates and use of hazardous reagents, as inventories of these dangerous materials can be kept to a minimum. New reagents and reactions continue to be developed to improve important bond-forming reactions and to allow new types of reactivity, which can be exploited to provide shorter and more efficient reaction pathways.

1 Introduction

2 Green Chemistry

2.1 Biocatalytic Methods

2.2 Flow Chemistry

3 Bond-Forming Reactions

3.1 Aryl-Coupling Reactions

3.2 C–H Bond Activation

3.3 Alcohol Substitutions

3.4 Ammonolysis and Amide Bond Formation

4 Reactions In/On Water

5 Reductions

5.1 Amide Reductions

6 Summary