Chemistry Reference
In-Depth Information
CHAPTER 16
Palladium Detection
Techniques for Active
Pharmaceutical Ingredients
Prepared via Cross-Couplings
KAZUNORI KOIDE
Department of Chemistry, University of Pittsburgh, 219 Parkman Avenue,
Pittsburgh, PA 15260, USA
Email: koide@pitt.edu
16.1 Palladium Catalysis in the Pharmaceutical
Industry
The generality of palladium catalysis in forming carbon-carbon and carbon-
heteroatom bonds has made it an indispensable tool in organic synthesis.
Most of the known palladium-catalyzed cross-coupling reactions and closely
related reactions were discovered in the 1960s and 1970s.
1-11
However, the
pharmaceutical industry did not adopt these reactions until the 1980s and
early 1990s.
12
The adoption was delayed partly because residual palladium in
synthetic compounds could not be removed to meet safety standards. Re-
moving palladium from synthetic materials is not yet a solved problem, but
dozens of palladium-scavenging techniques have become available,
13-24
making palladium-catalyzed reactions employable in pharmaceutical pro-
duction.
12,25
In the syntheses of 128 drugs carried out at AstraZeneca,
Search WWH ::
Custom Search