38605-63-9Relevant articles and documents
An efficient multi-component synthesis of N-1-alkylated 5-nitrouracils from α-amino acids
Boiteau, Jean-Guy,Bouix-Peter, Claire,Chambon, Sandrine,Clary, Laurence,Daver, Sebastien,Dumais, Laurence,Fournier, Jean-Fran?ois,Harris, Craig S.,Mebrouk, Kenny,Millois, Corinne,Pierre, Romain,Rodeville, Nicolas,Talano, Sandrine,Tomas, Lo?c
supporting information, p. 2367 - 2371 (2016/05/19)
The preparation of N-1 selectively alkylated uracil intermediates usually requires selective protection at N-3 followed by alkylation at N-1 and subsequent removal of the protecting group. In this Letter, we show the limitations of this approach when quaternary C centres at N-1 became a key target for the programme. To access this key substructure, we developed an efficient multi-component reaction (MCR) from readily available α-amino acid precursors.
PROCESS FOR PRODUCING OPTICALLY ACTIVE alpha-METHYLCYSTEINE DERIVATIVE
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, (2008/06/13)
The present invention provides a simple industrial process for producing an L- or D-optionally active α-methylcysteine derivative or its salt, which is a useful pharmaceutical intermediate, from readily available, inexpensive raw materials. In a process for producing an L- or D-optically active α- methylcysteine derivative or its salt, a racemic N-carbamoyl-α- methylcysteine derivative or its salt is D-selectively cyclized with hydantoinase to produce a D-5-methyl-5-thiomethylhydantoin derivative or its salt and an N-carbamoyl-α-methyl-L-cysteine derivative or its salt, which are then subjected to deprotection of the amino group and the sulfur atom, and hydrolysis.
