1253056-05-1Relevant articles and documents
Preparation method of Sitagliptin midbody of beta-amino acid
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Paragraph 0064-0065; 0066-0067, (2018/02/04)
The invention discloses a preparation method of a Sitagliptin midbody of beta-amino acid. The method comprises the following steps of 2,4,5-fluorobenzene acetaldehyde 2, L-benzedrine alcohol and tributyl allyl tin alkanes perform asymmetrical allylation reaction under the effect of a catalyst A to obtain a compound 3; the compound 3 is oxidized to remove chiral auxiliary radials to obtain a compound 4; the compound 4 is subjected to amino radial protection to obtain a compound 5; the compound 5 is subjected to double-bond oxidation to obtain beta-aminobutyric acid 1. The method provided by the invention has the advantages that the raw materials are cheap and can be easily obtained; the reaction route is short; the operation is simple and convenient; the reaction conditions are mild; no special requirements exist on the equipment; the yield is high; the selectivity is high; good industrial application and economic values are realized.
PROCESS FOR THE PREPARATION OF SITAGLIPTIN AND ITS INTERMEDIATES
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Page/Page column 59-60, (2010/11/05)
The present invention relates to novel and improved processes for the preparation of Sitagliptin compound of formula (1) and its intermediates.