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

12.I-4-(4-aminophenyl)-3-morpholinone (1) ye-anticoagulant rivaroxaban ilungiswe ngezindlela ezimbili: ①I-Bromobenzene yaphendulwa ngokulandelana nge-ethanolamine kanye ne-chloroacetyl chloride ukuze ithole i-4-benzene I-morpholinone iyancipha ibe yi-nitrated 1, kanti isamba sesivuno singaba ngu-32%;②I-Bromobenzene iqala i-nitrate, bese isabela nge-ethanolamine ukuze ithole i-2-(4-nitroanilino)thanol, ezovalwa nge-chloroacetyl chloride.Ukusabela kokunciphisa kukhiqiza u-1, futhi isivuno esiphelele singama-47%.

I-Rivaroxaban uhlobo olusha lwe-anticoagulant olungathathwa ngokuqondile ngomlomo.Ivimbela ngokuqondile ukusebenza kwe-coagulation factor Xa, inomphumela oqondile we-anticoagulant, ayidingi ukuqapha okuqhubekayo, futhi inokuphepha okuphezulu.Ngokusetshenziswa komtholampilo kwe-rivaroxaban, Isidingo se-rivaroxaban sizokhula kancane kancane.Igama lekhemikhali le-rivaroxaban yi-5-chloro-N-(((5S) -2-oxo-3-[4- (3-oxo- 4-morpholinyl)phenyl)-1,3-oxazolidine-5-yl)methyl -2-thiophenecarboxemide.Njengamanje kunemizila emibili yokwenziwa ebikwe ezincwadini, futhi yomibili imizila isetshenziswa I-4-(4-aminophenyl) emaphakathi -3-morpholinone.Nakuba kukhona imibiko mayelana nokuhlanganiswa kwe-4-(4-aminophenyl) -3-morpholinone ekhaya naphesheya, kunenani eliphakeme uma kuqhathaniswa lezinto zokusetshenziswa zokusetshenziswa.Iphezulu, okunzima ukuyithenga, noma izidingo zokusebenza zokusabela ziphakeme kakhulu, kunzima ukuzibamba, azihambisani nokuvikelwa kwemvelo nokunye ukusilela, futhi azihlangabezani nezidingo zokukhiqiza ngobuningi bezimboni.Lungiselela ukhiye omaphakathi we-rivaroxaban 4-(4-aminophenyl)- Inqubo yokukhiqiza ye-3-morpholinone kanye nokwehliswa kwentengo yezinto ezingavuthiwe nakanjani kuzokhuthaza ukukhuthazwa nokusetshenziswa kwe-rivaroxaban.Awukho umbiko mayelana nokuhlanganiswa kwe-rivaroxaban e-China.Sise-rivaroxaban Ukhiye ophakathi nendawo 4-(4-aminophenyl)-3-morpholinone umzila wokwenziwa kanye nobuchwepheshe bufundwe ngendlela entsha.I-bromobenzene emibili ne-p-nitrobromobenzene njengezisetshenziswa zokuqala ziyaphakanyiswa.Umzila wokucubungula.Gxila kunqubo ye-cyclization ye-3-morpholinone ring.