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

12.Wapakatikati 4-(4-aminophenyl)-3-morpholinone (1) wa anticoagulant rivaroxaban anakonzedwa ndi njira ziwiri: ①Bromobenzene anachita motsatizana ndi ethanolamine ndi chloroacetyl chloride kupeza 4-benzene The morpholinone kuchepetsedwa kuti nitrated 1, ndipo zokolola zonse ndi pafupifupi 32%;②Bromobenzene imayamba kulowetsedwa ndi ethanolamine kuti ipeze 2-(4-nitroanilino)ethanol, yomwe imatsekedwa ndi chloroacetyl chloride.Kuchepetsa kumapanga 1, ndipo zokolola zonse ndi pafupifupi 47%.

Rivaroxaban ndi mtundu watsopano wa anticoagulant womwe ungatengedwe mwachindunji pakamwa.Imalepheretsa mwachindunji kuyambitsa kwa coagulation factor Xa, imakhala ndi anticoagulant yotsimikizika, safuna kuwunika mosalekeza, ndipo imakhala ndi chitetezo chokwanira.Ndi ntchito yachipatala ya rivaroxaban, Kufunika kwa rivaroxaban kudzawonjezeka pang'onopang'ono.Dzina la mankhwala a rivaroxaban ndi 5-chloro-N-(((5S) -2-oxo-3--[4- (3-oxo- 4-morpholinyl)phenyl)-1,3-oxazolidine-5-yl) methyl. -2-thiophenecarboxymide.Pakalipano pali njira ziwiri zopangira zomwe zimafotokozedwa m'mabuku, ndipo njira zonsezi zimagwiritsidwa ntchito An intermediate 4- (4-aminophenyl) -3-morpholinone.Ngakhale pali malipoti okhudza kaphatikizidwe ka 4-(4-aminophenyl) -3-morpholinone kunyumba ndi kunja, pali mtengo wokwera kwambiri wazinthu zopangira.Mkulu, wovuta kugula, kapena zomwe zimafunikira ntchito ndizokwera kwambiri, zovuta kuzimvetsa, sizigwirizana ndi chitetezo cha chilengedwe ndi zofooka zina, ndipo sizikwaniritsa zofunikira zamakampani opanga misa.Konzani fungulo lapakati la rivaroxaban 4- (4-aminophenyl)- Njira yopangira 3-morpholinone ndi kuchepetsa mtengo wa zopangira zidzalimbikitsadi kukwezedwa ndi kugwiritsa ntchito rivaroxaban.Palibe lipoti lokhudza kaphatikizidwe ka rivaroxaban ku China.Tili pa rivaroxaban Chinsinsi chapakati 4-(4-aminophenyl) -3-morpholinone njira yopangira ndi ukadaulo waphunziridwa mwatsopano.Ma bromobenzene awiri ndi p-nitrobromobenzene ngati zida zoyambira akufunsidwa.Njira yopangira.Yang'anani pamayendedwe a cyclization a 3-morpholinone mphete.