287930-75-0Relevant articles and documents
Production process of aprepitant key intermediate
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, (2022/03/27)
The invention relates to the field of chemical pharmacy, in particular to a production process of an aprepitant key intermediate, which comprises the following steps: dissolving a glyoxylic acid aqueous solution in tetrahydrofuran, adding benzyl ethanolamine, distilling to recover tetrahydrofuran, crystallizing, filtering, washing and drying to obtain an intermediate AR-B; dissolving the intermediate AR-B in acetonitrile, adding trifluoroacetic anhydride and boron trifluoride acetonitrile, carrying out reduced pressure distillation to obtain acetonitrile, carrying out extraction, washing, configuration overturning and acetic acid quenching, adding a sodium bicarbonate solution, and carrying out extraction, filtration, washing and drying to obtain an intermediate AR-0; dropwise adding a tetrahydrofuran solution of p-phenylfluoro magnesium bromide into a mixture of the intermediate AR-0 and tetrahydrofuran, adding methanol and toluenesulfonic acid, filtering, adding toluenesulfonic acid and palladium carbon, hydrogenating, filtering out palladium carbon, extracting, washing and drying to obtain the key intermediate AR-1. The synthesis efficiency of the aprepitant key intermediate can be effectively improved, and the production cost is reduced.
A preparation method of the midbody arab league swiss tanzania (by machine translation)
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Paragraph 0025; 0028; 0029; 0032; 0033; 0036; 0037; 0040, (2019/04/14)
The invention discloses a method of preparing intermediates of arab league swiss tanzania, the method to (R)- 1 - [3, 5 - di (trifluoromethyl) phenyl] ethanol as the starting material, and trifluoroacetic anhydride reaction the compound of formula II, the formula II compound in the catalyst and under strongly alkaline conditions with 4 - benzyl - 2 - hydroxy - morpholine - 3 - one the response results in the type I the target compound (2 R) - 4 - benzyl - 2 - [(1 R) - 1 - [3, 5 - double-(trifluoromethyl) phenyl] ethoxy] morpholine - 3 - one. The method of simple process steps, operation is simple and easy, the resulting product has high purity, high yield, low production cost, and the reagent for economic and environmental protection, and is suitable for industrial production. (by machine translation)
Aprepitant intermediate and preparation method thereof
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Paragraph 0040-0041, (2017/04/22)
The invention relates to the technical field of medicinal chemical production, in particular to an aprepitant intermediate and a preparation method thereof. The preparation method comprises the following preparation steps: by using 4-benzyl-2-hydroxy-morpholine-3-ketone II and (R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl alcohol III as raw materials, making a condensation reaction under the effect of a catalyst to obtain a compound IV; adding the obtained compound IV into a Grignard reagent to make a Grignard reaction; converting the compound IV into a compound V under reducing conditions; making a hydrochlorination reaction on the obtained compound V to obtain a target compound I. The aprepitant intermediate and the preparation method have the advantages that the preparation flow process is simple; the total effectiveness is high; the intermediate purification is convenient; the purity of a target product is high, and the like. The aprepitant intermediate and the preparation method are suitable for industrial production.