889852-02-2Relevant academic research and scientific papers
Preparation method of fosaprepitant dimeglumine pharmaceutical salt
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Paragraph 0027; 0028, (2019/01/07)
The invention belongs to the technical field of medicine chemistry, and particularly relates to a novel preparation method of fosaprepitant dimeglumine. According to the preparation method, triethyl silane is used for replacing hydrogen, and high-pressure
A process for the preparation of [3 - [(2 R) - [(1 R) - 1 - [3, 5 - di (trifluoromethyl) phenyl] ethoxy] - 3 (S)- (4 - fluorophenyl) morpholine - 4 - yl] methyl] - 5 - oxo - 4, 5 - dihydro - [1, 2, 4] - triazole - 1 - yl] phosphine acid animal pen ester new method
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Paragraph 0027; 0028; 0033; 0038; 0043; 0044; 0048, (2017/08/26)
The invention relates to a new method for preparing fosaprepitant intermediate, namely, [3-[(2R)-[(1R)-1-(3, 5-bi (trifluoromethyl) phenyl] ethyoxyl]-3 (S)-(4-fluorophenyl) morpholine 4-group] methyl]-5-oxo-4, 5-dihydro-[1, 2, 4]-triazole-1-group] phosphonic acid-benzyl ester. The compound is an important medicine intermediate, and is used for preparing antiemetic drug fosaprepitant. The new method comprises the steps of: enabling newly prepared phosphorylation agent dibenzyl phosphorus oxychloride and aprepitant to have reaction in organic solvent under the action of steric hindrance alkali, treating the product with methyl alcohol to obtain the fosaprepitant intermediate. The method is simple in operation and low in cost, thus being more suitable for industrial production.
PROCESS FOR [3-[3(R)-[(R)-1-[3,5-BIS(TRIFLUOROMETHYL)PHENYL]HOXY]-3(S)-(4-FLUOROPHENYL)MORPHOLIN-4-YL-5-OxO-4,5-DIHYDRO-[1,2,4]-TRIAZOL-1-YL PHOSPHONIC ACID
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Page/Page column 5-6, (2008/06/13)
The present invention is concerned with a process for the preparation of the compound {3-[2(R)-[(1R)-1-[3,5-bis(tri-fluoromethyl)phenyl]ethoxy]-3(S)-(4-fluorophenyl)-morpholin-4-yl]methyl]-5-oxo-4,5-dihydro-[1,2,4]-triazol-1-yl}phosphonic acid, and pharmaceutically acceptable salts thereof. This compound is useful as a substance P (neurokinin-1) receptor antagonist. In particular, the compound is useful e.g., in the treatment of emesis and inflammatory diseases.
