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US 11,236,054 B2Granted
Method for preparing aryl 2-tetrazol-1-yl keto with improved selectivity
AssigneeSK Biopharmaceuticals Co., Ltd.
InventorsKyuwoong Lee, Kyungmi Cha, Suyeon Yeom, Jiseon Woo
Life of this patent
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Abstract
The present disclosure relates to a method for preparing aryl 2-tetrazol-2-yl ketone of the following Formula 1a with improved selectivity: wherein R1 and R2 are the same as defined herein.
Claims15
A method for preparing a compound of Formula 1a, comprising:
- reacting a compound of Formula 2 with a salt of a compound of Formula 3:
- wherein
- R1 and R2 are each independently selected from the group consisting of hydrogen, halogen, perfluoroalkyl having 1 to 8 carbon atoms, alkyl having 1 to 8 carbon atoms, thioalkoxy having 1 to 8 carbon atoms, and alkoxy having 1 to 8 carbon atoms;
- and
- X is a leaving group.
2 more elements
A method for preparing a compound of Formula 4, comprising:
- (1) reacting a compound of Formula 2 with a salt of a compound of Formula 3;
- (2) separating the compound of Formula 1a from a mixture obtained from the reaction of step (1);
- and
- (3) reducing the compound of Formula 1a separated in step (2) and carbamating the reduced compound of Formula 1a:
- wherein
- R1 and R2 are each independently selected from the group consisting of hydrogen, halogen, perfluoroalkyl having 1 to 8 carbon atoms, alkyl having 1 to 8 carbon atoms, thioalkoxy having 1 to 8 carbon atoms, and alkoxy having 1 to 8 carbon atoms;
- and
- X is a leaving group.
5 more elements
Dependencies are inferred from the claim text.