FIELD: chemical pharmaceutical industry.
SUBSTANCE: method for the synthesis of aryl-2-tetrazol-2-yl ketone of Formula 1a, used as an intermediate for the large-scale production of (R)-1-aryl-2-tetrazolylethyl ester of carbamic acid, used in the treatment of diseases of the central nervous system. A method for preparing a compound of Formula 1a involves reacting a compound of Formula 2 with a salt of a compound of Formula 3, where each R is1 and R2 is independently selected from the group consisting of hydrogen, halogen, perfluoroalkyl having 1-8 carbon atoms, alkyl having 1-8 carbon atoms, thioalkoxy having 1-8 carbon atoms, and alkoxy having 1-8 carbon atoms, and X is a leaving group.
EFFECT: providing a method with increased yield of carbamate compound due to more selective synthesis of aryl-2-tetrazol-2-yl ketone.
24 cl, 3 dwg, 12 ex
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Authors
Dates
2023-11-23—Published
2020-10-23—Filed