C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 277/64 (2006.01) C07D 277/82 (2006.01)
Patent
CA 2375625
The present invention aims at providing a process for producing a substituted alkylamine derivative useful as an intermediate for medicine or agrochemical, from a 2-aminothiophenol derivative at a high yield industrially. The present invention lies in a process for producing a substituted alkylamine derivative represented by the following general formula (3): (see formula 3) (wherein X is a halogen atom, an alkyl group, an alkoxy group, a cyano group or a nitro group; n is an integer of 1 to 4; and R1 and R2 are each independently a hydrogen atom or a phenyl group-substituted or unsubstituted alkyl group and may together form a 5- or 6-membered ring) or an acid addition salt thereof, which process comprises adding a salt of a 2- aminothiophenol derivative represented by the following general formula (1): (see formula 1) (wherein X and n have the same definitions as given above) into an acid to allow the system to have a pH of 6 or less and convert the salt into a free 2-aminothiophenol of the general formula (1) and then reacting the 2-aminothiophenol derivative with an amino acid-N-carboxyanhydride represented by the following general formula (2): (see formula 2) (wherein R1 and R2 each have the same definitions as given above).
L'invention concerne un procédé de production de dérivé d'alkylamine substituée représenté par la formule générale (3), ou d'un sel d'addition acide, qui consiste à ajouter un sel d'un dérivé 2-aminothiophénol, représenté par la formule générale (1), à un acide, à ajuster le pH du mélange à 6, ou à une valeur inférieure, afin de faire passer le sel sous sa forme libre, puis à faire réagir le composé sous sa forme libre avec un N-carboxyanhydride d'acide aminé représenté par la formule générale (2). (Dans les formules, X, n, R1 et R2 sont les mêmes que ceux définis dans les revendications).
Ihara Chemical Industry Co. Ltd.
Smart & Biggar
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