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- Title
A Synthesis Route of an Oral Antidiabetic Drug-Linagliptin based on the Removal of Protective Group.
- Authors
Zhiwen Zeng; Xiang Li; Fuxing Zhang
- Abstract
In this paper, a synthetic route of oral antidiabetic drug-linagliptin based on the removal of protective group was studied. The key intermediate was obtained from methyl urea by 6 steps of cyclization, nitrosation, reduction, cyclization, Bromination and substitution. The intermediate 2-chloromethyl-4-methylouwarin was synthesized from o-aminoacetophenone by condensation, cyclization and reduction. Based on these two intermediates, linagliptin was prepared by a series of substitution reactions. The experimental results show that the synthesis efficiency of this method is high. In addition, the raw material of the synthesis method is cheap and easy to obtain, the reaction conditions are mild, and the post-treatment is simple, which lays a foundation for industrial production.
- Publication
Acta Microscopica, 2020, Vol 29, Issue 1, p244
- ISSN
0798-4545
- Publication type
Academic Journal