- Method for preparing alogliptin midbody
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The invention discloses a method for preparing an alogliptin midbody. The method comprises the following steps: carrying out contact reaction on 1-(2-isocyan benzyl)-3-methylurea and diethyl malonate in acetonitrile in the presence of a compound shown in a formula I and cesium carbonate; pouring the product into water after the reaction is ended; carrying out filtration and filtering out the solid for washing, and recrystallizing the product with ethanol to obtain the alogliptin midbody 1-(2-isocyan benzyl)-3-methyl pyrimidine-2,4,6(1H,3H,5H)-trione shown in the specification. By the method for preparing the alogliptin midbody, the yield is high; and the reaction time is greatly shortened.
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Paragraph 0025; 0026; 0027; 0028; 0029
(2017/01/02)
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- PROCESS FOR THE PREPARATION OF ALOGLIPTIN
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The present invention is based on the discovery of a process for preparing pyrimidin- dione compounds, especially alogliptin and its derivatives, which comprises the reaction of a urea derivative of formula (VIII) with a malonic acid or its derivatives to form intermediates of formulae (VII) or (VII-A), which are subsequently converted to a compound of formula (II) upon introduction of a leaving group X. Compound (II) then reacts with an amine to form compound (I), which is optionally converted to its salts of formula (IV).
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Page/Page column 25
(2010/11/05)
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