- Synthetic method of vildagliptin
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The invention relates to the technical field of drug synthesis and particularly relates to a synthetic method of vildagliptin. The synthetic method comprises the following steps: carrying out imino group protection and acylamino dehydration on a starting raw material, namely L-prolinamide, and carrying out deproteciton salification by virtue of p-toluene sulfonic acid so as to obtain p-toluenesulfonate of (S)-2-cyanopyrrolidine; substituting and hydrolyzing 3-amino-1-adamantanol so as to obtain 3-iminoacetic acid-1-adamantanol; carrying out condensation acylation by virtue of 3-iminoacetic acid-1-adamantanol and (S)-2-cyanopyrrolidine under the action of 1-ethyl-(3-dimethylaminopropyl)carbodiimide hydrochloride, so as to obtain the vildagliptin. The synthetic method has the beneficial effects that reaction conditions are mild, an intermediate does not absorb moisture and is easy to store, the purity of the synthesized vildagliptin is high and is more than or equal to 99.50%, and the maximum single impurity content is less than or equal to 0.10%.
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Paragraph 0070; 0072; 0092; 0112; 0128
(2017/09/01)
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- NOVEL ECONOMIC PROCESS FOR VILDAGLIPTIN
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The present invention relates to a commercially viable novel process for manufacturing Vildagliptin in high yield with high chemical and chiral purity.
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Page/Page column 17
(2015/09/28)
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- PROCESS FOR PREPARATION OF DPP-IV INHIBITORS
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Process for the preparation of DPP-IV inhibitors, such as 1-[[(3-hydroxy-1-adamantyl) amino] acetyl]-2-cyano-(S)-pyrrolidine are disclosed.
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Page/Page column 17-18
(2011/09/19)
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