187393-68-6Relevant articles and documents
A Iraq curved theophylline preparation of intermediate
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Paragraph 0027; 0028; 0029; 0030; 0031; 0032, (2019/06/30)
The present invention provides a kind of Iraq curved theophylline intermediate (E)- 1, 3 - diethyl - 6 - amino - 5 - (3, 4 - dimethoxy acryloyl) amino uracil preparation method, comprising the following steps: 1, 3 - diethyl - 5, 6 - diamino uracil as raw materials, methylene chloride as the solvent, triethylamine as acid-binding agent, slowly add (E) 3, 4 - dimethoxy acryloyl chloride, reaction, washes the acid, water crystallization, shall (E)- 1, 3 - diethyl - 6 - amino - 5 - (3, 4 - dimethoxy acryloyl) amino uracil; the invention provides a preparation method, to separate out the product from the organic layer, can make the reactant and by-product effective separation, get of the Iraqi curved theophylline intermediate high purity, the operation is simple.
Istradefylline raw material drug and preparation method thereof
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Paragraph 0059-0061, (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.
Multigram-Scale Syntheses, Stability, and Photoreactions of A2A Adenosine Receptor Antagonists with 8-Styrylxanthine Structure: Potential Drugs for Parkinson's Disease
Hockemeyer, Joerg,Burbiel, Joachim C.,Mueller, Christa E.
, p. 3308 - 3318 (2007/10/03)
The improved multigram-scale syntheses of the important 8-styrylxanthine A2A adenosine receptor antagonist MSX-2 (8), its water-soluble prodrug MXS-3 (9), and KW-6002 (16) are described. N-Alkylation reactions at different positions of uracil derivatives were optimized. Two different methods for xanthine formation from 6-amino-5-cinnainoylaminouracil precursors were investigated, (a) the elimination of water by alkaline catalysis and (b) hexamethyldisilazane as a condensing agent; the latter was found to be superior. The photosensitivity of 8-styrylxanthines was studied. The (E)-configurated stryrylxanthine MSX-2 (8) isomerized in diluted solution, and the resulting (Z)-isomer (10a) was isolated and characterized. Furthermore, we describe for the first time that solid 8-styrylxanthines can dimerize upon exposition to daylight or irradiation with UV light. The resulting cyclobutane derivatives with head-to-tail (syn) configuration exhibited a considerably lower A 2A adenosine receptor affinity than their parent compounds. The dimerization product of MSX-2 was a moderately potent nonselective A 1 and A2A antagonist (Ki(Ai) = 273 nM, Ki(A2A) = 175 nM) while the dimer of the related compound KW-6002 was inactive at A1 and only weakly active at A 2A adenosine receptors (Ki = 1.57 μM). The light sensitivity of 8-styrylxanthine derivatives, not only in solution, but also in the solid state, has to be considered when using those compounds as pharmacological tools or drugs.