219821-37-1Relevant articles and documents
Method for preparing intermediate of the Fosaprepitant
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Paragraph 0017; 0030-0039, (2018/05/16)
The invention discloses a method for preparing an intermediate of the Fosaprepitant, and specifically relates to a new method for preparing a drug 5-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl] ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-3H-1,2,4-triazole-3-one, i.e., Aprepitant. The method comprises the steps of: synthesizing a compound (IV) in the presence of a condensation system, and then performing cyclization on the compound (IV) at 139 DEG C or below to obtain the target compound (I). The preparation method is green, environmentally friendly and efficient and has easy industrialization.
A kind of preparation method of dimethyl luck Sha Pitan cyclophosphadenosine
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Paragraph 0042-0044, (2017/04/07)
The invention relates to a method for preparing fosaprepitant. The fosaprepitant is shown as a formula (I). The method comprises steps 1, 2, 3 and 4, finally, a compound shown as the formula (I) is obtained through hydrogenation reduction; in the step 1, a compound in a formula (II) reacts with a Grignard reagent to generate a compound shown as a formula (III) in the presence of palladium carbon and ammonium formate. The method for preparing is simple in production step, has high reaction yield and less side products, is easy in control of the reaction conditions and is suitable for medical industrial production.
A METHOD OF PREPARING 3- ( ( (2R, 3S) -2- ( (R) -1- (3, 5 -BIS (TRIFLUOROMETHYL) PHENYL) ETHOXY) -3 - (4 - FLUOROPHENYL) MORPHOLINO) METHYL) - 1H- 1, 2, 4 -TRIAZOL- 5 (4H) -ONE (APREPITANT) IN POLYMORPH FORM I OR II
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Page/Page column 6; 7, (2013/09/26)
The present solution relates to a method of preparing aprepitant of formula (1) in the desired crystalline form II or I, wherein the intermediate of formula (12) is extracted with a water immiscible high-boiling solvent selected from an alcohol, ester or ketone and, after washing with water and/or brine, the solution is heated up to the boiling point of the given solvent, which results in cyclization to aprepitant, and, after cooling, the produced aprepitant is isolated.