1785764-26-2Relevant articles and documents
Novel preparation method for Istradefylline
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Paragraph 0020, (2017/08/28)
The invention relates to a preparation method for Istradefylline represented by a formula (I) shown in the description. The method comprises the following steps: subjecting 6-amino-1,3-diethyl-5-nitroso-1H-pyrimid-2,4-dione represented by a formula (II) shown in the description, which serves as a raw material, to catalytic reduction and salt forming, so as to obtain 5,6-diamino-1,3-diethyl-1H-pyrimid-2,4-dione hydrochloride represented by a formula (III) shown in the description; then, carrying out acetylation on the compound (III), so as to obtain N-(6-amino-1,3-diethyl-2,4-dioxo-1,2,3,4-tetrahydropyrimid-5-yl)acetamide represented by a formula (IV) shown in the description; carrying out further ring closing, so as to obtain 1,3-diethyl-8-methyl-1H-purin-2,6(3H,7H)-dione represented by a formula (V) shown in the description; and carrying out methylation on the compound (V) firstly, and then, subjecting the methylation product to a condensation reaction with veratraldehyde represented by a formula (VII) shown in the description, thereby obtaining the end product Istradefylline. According to the novel preparation method for the Istradefylline, provided by the invention, raw materials, which are readily available industrially and are low in price, are used, the production process is more environmentally friendly, and the obtained product Istradefylline is high in yield and purity, thereby having a relatively high practical value.