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

12. Ua hoʻomākaukau ʻia ka 4-(4-aminophenyl)-3-morpholinone (1) waena o ka anticoagulant rivaroxaban e nā ʻano ʻelua: ①Bromobenzene i hui pū ʻia me ka ethanolamine a me ka chloroacetyl chloride e loaʻa ai ka 4-benzene a laila hoʻemi ʻia ka morpholinone. 1, a he 32% ka huina hoonui;②Hoʻomaka mua ʻia ʻo Bromobenzene, a laila hana ʻia me ka ethanolamine e loaʻa ai ka 2-(4-nitroanilino) ethanol, a laila pani ʻia e ka chloroacetyl chloride.ʻO ka hopena hōʻemi e hoʻopuka i ka 1, a ʻo ka huina o ka hua ma kahi o 47%.

ʻO Rivaroxaban kahi ʻano anticoagulant hou e hiki ke lawe pololei ʻia ma ka waha.Hoʻopili pololei ia i ka hoʻoulu ʻana o ka coagulation factor Xa, he hopena anticoagulant paʻa, ʻaʻole koi i ka nānā mau ʻana, a he palekana kiʻekiʻe.Me ka noi lapaʻau o rivaroxaban, E piʻi mālie ka noi no rivaroxaban.ʻO ka inoa kemika o rivaroxaban he 5-chloro-N-(((5S) -2-oxo-3-[4- (3-oxo- 4-morpholinyl)phenyl) -1,3-oxazolidine-5-yl)methyl -2-thiophenecarboxamide.Aia i kēia manawa ʻelua ala synthetic i hōʻike ʻia ma ka palapala, a ua hoʻohana ʻia nā ala ʻelua ʻO kahi waena 4-(4-aminophenyl) -3-morpholinone.ʻOiai aia nā hōʻike e pili ana i ka synthesis o 4-(4-aminophenyl) -3-morpholinone ma ka home a ma waho, aia ke kumu kūʻai kiʻekiʻe o nā mea maka.ʻO ke kiʻekiʻe, paʻakikī ke kūʻai, a i ʻole nā ​​koi o ka hana pane ʻana he kiʻekiʻe loa, paʻakikī ke hopu, ʻaʻole kūpono i ka mālama ʻana i ke kaiapuni a me nā hemahema ʻē aʻe, a ʻaʻole hoʻi e hoʻokō i nā koi o ka hana ʻoihana nui.E hoʻonui i ke kī waena o rivaroxaban 4-(4-aminophenyl)- ʻO ke kaʻina hana o 3-morpholinone a me ka hoʻohaʻahaʻa ʻana i ke kumukūʻai o nā kumu waiwai e hoʻoikaika maoli i ka hoʻolaha a me ka noi ʻana o rivaroxaban.ʻAʻohe hōʻike e pili ana i ka synthesis o rivaroxaban ma Kina.Aia mākou ma rivaroxaban Ua aʻo hou ʻia ke ala waena 4-(4-aminophenyl)-3-morpholinone synthetic a me ka ʻenehana.ʻElua bromobenzene a me p-nitrobromobenzene i mea hoʻomaka.Alanui kaʻina hana.E nānā i ke kaʻina hana cyclization o ke apo 3-morpholinone.