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US 2014/0005394 A1Published application
Preparation method of intermediate of sitagliptin
AssigneeSt Pharm Co., Ltd.
InventorsGeun Gho Lim, Sun Ki Chang, Chang Ho Byeon
Life of this patent
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Abstract
The present invention provides a method which enables the simple, economical and high-yield production which is a key intermediate of antidiabetic drug Januvia.
Claims18
A method for preparing a compound of Formula 2:
- wherein R is t-butyloxycarbonyl (Boc), benzyloxycarbonyl (Cbz), fluorenylmethyloxycarbonyl (Fmoc), acetyl or benzoyl, comprising:
- reacting a compound of Formula 3:
- wherein R is t-butyloxycarbonyl (Boc), benzyloxycarbonyl (Cbz), fluorenylmethyloxycarbonyl (Fmoc), acetyl or benzoyl,
- with 3-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-α]pyrazine or a salt thereof in an organic solvent in the presence of 2-chloro-4,6-dimethoxy-1,3,5-triazine and a tertiary organic amine to produce a compound of Formula 2.
1 more element
Dependencies are inferred from the claim text.