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2.2.1 Cross-Coupling Methods for Methylation

DOI: 10.1055/sos-SD-213-00015

Molander, G. A.; Ryu, D.Science of Synthesis: C-1 Building Blocks in Organic Synthesis, (2014231.

General Introduction

The methylation reaction is the least efficient carbon–carbon bond-forming reaction imaginable. The inherent lack of atom economy and diminutive increase in molecular complexity gained in such a process often makes it wholly undesirable from a strategic point of view. Nevertheless, from time to time the lack of suitable starting materials for target-oriented synthesis or the demands of library synthesis from substrates that allow modular elaboration may require or benefit from a simple methylation. Additionally, the need for appropriately radiolabeled substances may also provide a rationale for such a transformation. In these cases, a reliable and high-yielding methylation process that is tolerant of embedded functional groups is of utmost necessity.


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