- Application of kinetic modeling and competitive solvent hydrolysis in the development of a highly selective hydrolysis of a nitrile to an amide
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A combination of mechanism-guided experimentation and kinetic modeling was used to develop a mild, selective, and robust hydroxide-promoted process for of a nitrile to an amide using a substoichiometric amount of aqueous sodium hydroxide in a mixed water and N-methyl-2-pyrrolidone solvent system. The new process eliminated a major reaction impurity, minimized overhydrolysis of the product amide by selection of a solvent that would be sacrificially hydrolyzed, eliminated genotoxic impurities, and improved the intrinsic safety of the process by eliminating the use of hydrogen peroxide. The process was demonstrated in duplicate on a 90 kg scale, with 89% isolated yield and greater than 99.8% purity.
- Niemeier, Jeffry K.,Rothhaar, Roger R.,Vicenzi, Jeffrey T.,Werner, John A.
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p. 410 - 416
(2014/04/17)
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- QUINOLINYL-PYRROLOPYRAZOLES
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A compound according to formula II and the pharmaceutically acceptable salts thereof and the method of treating cancer in a patient in need thereof by administration of said compound.
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