4--[4-[(5S)-5-(Aminomethyl)-2-oxo-3-oxazolidinyl]phenyl]-3-morpholinone Hydrochloride

12.Iyo yepakati 4-(4-aminophenyl) -3-morpholinone (1) ye anticoagulant rivaroxaban yakagadzirwa nenzira mbiri: ①Bromobenzene yakaitwa zvakatevedzana ne ethanolamine uye chloroacetyl chloride kuti iwane 4-benzene The morpholinone inoderedza kusvika nitrated 1, uye goho rose rinenge 32%;②Bromobenzene inotanga kunyudzwa, yozoitwa ne ethanolamine kuwana 2-(4-nitroanilino) ethanol, inozovharwa nechloroacetyl chloride.Kuita kwekudzikisa kunoburitsa 1, uye goho rose rinenge 47%.

Rivaroxaban rudzi rutsva rwe anticoagulant inogona kutorwa zvakananga nemuromo.Iyo inodzivirira zvakananga kushandiswa kweiyo coagulation factor Xa, ine chaiyo anticoagulant mhedzisiro, haidi kuramba ichitariswa, uye ine kuchengetedzwa kwakanyanya.Nekushandiswa kwekiriniki ye rivaroxaban, Kudiwa kwe rivaroxaban kuchawedzera zvishoma nezvishoma.Zita remakemikari ye rivaroxaban ndeye 5-chloro-N- (((5S) -2-oxo-3--[4- (3-oxo- 4-morpholinyl)phenyl) -1,3-oxazolidine-5-yl) methyl. -2-thiophenecarboxemide.Parizvino pane nzira mbiri dzekugadzira dzakataurwa mumabhuku, uye nzira mbiri dzinoshandiswa An yepakati 4-(4-aminophenyl) -3-morpholinone.Kunyange zvazvo kune mishumo pamusoro pekugadzirwa kwe4-(4-aminophenyl) -3-morpholinone kumba nekune dzimwe nyika, kune mutengo wakakura wekuita zvinhu zvakasvibirira.Yakakwirira, yakaoma kutenga, kana maitiro ekuvhiya zvinodiwa zvakanyanyisa, zvakaoma kubata, hazvienderane nekuchengetedzwa kwezvakatipoteredza uye zvimwe zvinoshomeka, uye hazvizadzise zvinodiwa zvekugadzirwa kwemaindasitiri akawanda.Gadzirisai kiyi yepakati ye rivaroxaban 4- (4-aminophenyl)- Nzira yekugadzira ye3-morpholinone uye kuderedzwa kwemutengo wezvinhu zvakasvibirira zvichanyatsokurudzira kukurudzirwa uye kushandiswa kwe rivaroxaban.Iko hakuna mushumo weiyo synthesis ye rivaroxaban muChina.Isu tiri pa rivaroxaban Kiyi yepakati 4- (4-aminophenyl) -3-morpholinone nzira yekugadzira uye tekinoroji yakadzidzwa nehunyanzvi.Bromobenzene mbiri uye p-nitrobromobenzene semidziyo yekutanga inokurudzirwa.Process nzira.Tarisa pane cyclization maitiro e3-morpholinone mhete.