- Synthesis method of trelagliptin intermediate
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The invention belongs to the technical field of medicines, and particularly relates to a synthesis method of a trelagliptin intermediate (R)-3-aminopiperidine dihydrochloride. The synthesis method specifically comprises the following steps: 1) reducing carbonyl of a compound shown as a formula I in an organic solvent A by using a reducing agent to prepare a compound shown as a formula II; 2) splitting the compound shown in the formula II in an organic solvent B through a chiral reagent to prepare a compound shown in a formula III; and 3) removing the benzyl of the compound shown by the formula III by palladium on carbon to obtain the (R)-3-aminopiperidine dihydrochloride. The (R)-3-aminopiperidine dihydrochloride prepared by the method has high yield and purity, the HPLC purity is higher than 98.16%, and the optical purity is higher than 98.92%; and the synthesis method has the advantages of low price of initial raw materials, facilitation of reduction of industrial cost, short synthesis process route, mild reaction conditions and easy industrial realization.
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Paragraph 0020; 0064-0069
(2021/07/17)
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- SMALL MOLECULES AGAINST CEREBLON TO ENHANCE EFFECTOR T CELL FUNCTION
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Disclosed are small molecules against cereblon to enhance effector T cell function. Methodos of making thes molecules and methods of using them to treat various disease states are also disclosed.
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Page/Page column 112; 114
(2017/10/11)
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- Substituted glutarimides and their use as inhibitors of IL-12 production
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Substituted glutarimides of formula I 1and their method of making. Also disclosed are pharmaceutical compositions comprising the glutarimidie, particularly as immunomodulators and as inhibitors of angiopathies, or haematological or oncological diseases, as well as a method for treating various diseases using the glutarimides.
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