1033418-57-3Relevant articles and documents
Use of a Curtius Rearrangement as Part of the Multikilogram Manufacture of a Pyrazine Building Block
Steven, Alan,Hopes, Phillip
, p. 77 - 81 (2018)
Commercial route definition for a glucokinase activator called for a reevaluation of the synthesis and processes used to access multikilogram quantities of 2-amino-5-methylpyrazine. After consideration of different options, a variation of the Curtius rearrangement used by the medicinal chemistry route was selected for further development. The formation of an acyl azide for the Curtius rearrangement required a process safety control strategy to be put in place. The process developed was used to successfully deliver multikilogram quantities of 2-amino-5-methylpyrazine in an overall yield of 68%, starting from 5-methylpyrazine-2-carboxylic acid.
CHEMICAL PROCESS 632
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Page/Page column 21, (2010/08/22)
A process for preparing pharmaceutically active compounds of formula (I) or a salt thereof wherein R1, n, m, R3, R6, X1, X2, X3 and X4 are as defined in the specification, is described. Novel intermediates are also described and claimed.