26-03-2015 дата публикации
Номер: US20150087828A1
Принадлежит:
A molecule with neural activities, especially 4-substituent-2-hydroxymorpholin-3-one, as a new intermediate of neurokinin-1 receptor antagonist aprepitant, and preparation method thereof. 6. The method according to claim 5 , which is characterized in that the solvent used in the reaction is selected from the group consisting of: ethyl acetate claim 5 , C-Calkane claim 5 , benzene claim 5 , toluene claim 5 , paraxylene claim 5 , chlorobenzene claim 5 , orthodichlorobenzene claim 5 , acetone claim 5 , dichloromethane claim 5 , chloroform claim 5 , nitromethane claim 5 , N claim 5 ,N-dimethyl formamide claim 5 , dimethyl sulfoxide claim 5 , 2-butanone claim 5 , C-Calcohols claim 5 , 1 claim 5 ,3-dioxane claim 5 , 1 claim 5 ,4-dioxane claim 5 , tetrahydrofuran claim 5 , acetonitrile claim 5 , 1 claim 5 ,2-dimethyl ethyl claim 5 , water and the mixture thereof; and preferably claim 5 , the solvent is selected from the solvent miscible with water claim 5 , including N claim 5 ,N-dimethyl formamide claim 5 , dimethyl sulfoxide claim 5 , 2-butanone claim 5 , C-Calcohols claim 5 , 1 claim 5 ,3-dioxane claim 5 , 1 claim 5 ,4-dioxane claim 5 , tetrahydrofuran claim 5 , acetonitrile claim 5 , 1 claim 5 ,2-dimethyl ethyl and a mixture thereof; and more preferably claim 5 , the solvent is selected from tetrahydrofuran claim 5 , acetonitrile and the mixture thereof; and most preferably claim 5 , the solvent is tetrahydrofuran.7. The method according to claim 5 , which is characterized in that the reaction temperature for the method is from 30 to 100° C.; and preferably claim 5 , is from 60 to 70° C.8. The method according to claim 5 , which is characterized in that the aqueous glyoxalic acid solution used in the method is selected from an aqueous solution of glyoxalic acid monohydrate claim 5 , and an aqueous glyoxalic acid solution with a mass ratio of 1-99%; and preferably claim 5 , the mass ratio of the aqueous glyoxalic acid solution is 50%.9. Use of the compound according to ...
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