155270-98-7Relevant articles and documents
A Iraq curved theophylline preparation of intermediate
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Paragraph 0023-0034, (2019/02/08)
The invention relates to a preparation method of an istradefylline intermediate, which comprises the following steps: by using (E)-1,3-diethyl-6-amino-5-(3,4-dimethoxyphenylacryloyl)amino-uracil (YQ-1) as a raw material and 1,4-dioxane as a solvent, heating under the alkaline condition of a NaOH water solution to perform condensation and cyclization to generate (E)-8-[2-(3,4-dimethoxyphenyl)vinyl]-1,3-diethyl-3,7-dihydro-1H-purinyl-2,6-dione (YQ-2), and carrying out rotary evaporation, acid regulation and vacuum filtration to obtain a YQ-2 crude product; and by using toluene as a solvent, recrystallizing the YQ-2 crude product to obtain the YQ-2 refined product. The method has the advantages of simple route, accessible raw materials and mild conditions, and is convenient to operate; the total yield is greater than 85%, and the purity is up to higher than 97%; and thus, the method is suitable for scale-up production.
Istradefylline raw material drug and preparation method thereof
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Paragraph 0062-0072, (2018/12/14)
The invention relates to an istradefylline raw material drug and a preparation method thereof. Specifically, the invention relates to an istradefylline raw material drug. A compound shown in formula III is not higher than 0.5% and is a medicine preparation consisting of the istradefylline raw material drug and a pharmacologically acceptable carrier and/ or diluent. The raw material drug and the preparation thereof have better safety, effectiveness and stability. The formula III is shown in the description.
An efficient route to xanthine based A2A adenosine receptor antagonists and functional derivatives
Labeaume, Paul,Dong, Ma,Sitkovsky, Michail,Jones, Elizabeth V.,Thomas, Rhiannon,Sadler, Sara,Kallmerten, Amy E.,Jones, Graham B.
supporting information; scheme or table, p. 4155 - 4157 (2010/10/21)
A one-pot route to 8-substituted xanthines has been developed from 5,6-diaminouracils and carboxaldehydes. Yields are good and the process applicable to a range of substrates including a family of A2A adenosine receptor antagonists. A new route to the KW-6002 family of antagonists is presented including a pro-drug variant, and application to related image contrast agents developed.