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

12. Ko te takawaenga 4-(4-aminophenyl)-3-morpholinone (1) o te anticoagulant rivaroxaban i whakaritea e nga tikanga e rua: ①Bromobenzene i tauhohehia ki te ethanolamine me te chloroacetyl chloride kia whiwhi ai te 4-benzene Ko te morpholinone ki te whakaheke katahi ka paati. 1, a ko te katoa o nga hua ko te 32%;②Ko te Bromobenzene i te tuatahi ka whakahaehae, katahi ka tauhohe ki te ethanolamine kia whiwhi 2-(4-nitroanilino)ethanol, ka katihia e te chloroacetyl chloride.Ko te tauhohenga whakaheke ka puta te 1, a ko te katoa o nga hua ko te 47%.

Ko te Rivaroxaban he momo anticoagulant hou ka taea te tango tika ma te waha.Ka aukati tika i te whakahohenga o te tauwehe coagulation Xa, he tino whai hua anticoagulant, kaore e hiahiatia te aro turuki tonu, he nui te haumaru.Na te tono haumanu o rivaroxaban, Ka piki haere te tono mo te rivaroxaban.Ko te ingoa matū o rivaroxaban ko 5-chloro-N-(((5S) -2-oxo-3-[4- (3-oxo- 4-morpholinyl)phenyl)-1,3-oxazolidine-5-yl)methyl -2-thiophenecarboxamide.I tenei wa, e rua nga ara waihanga kua korerotia i roto i nga tuhinga, a ka whakamahia nga huarahi e rua He takawaenga 4-(4-aminophenyl)-3-morpholinone.Ahakoa he purongo mo te whakahiatotanga o te 4-(4-aminophenyl)-3-morpholinone i te kainga me nga whenua o waho, he nui te utu o nga rauemi mata tauhohenga.He tiketike, he uaua ki te hoko, he nui rawa atu ranei nga whakaritenga mahi tauhohenga, he uaua ki te hopu, kaore e pai ki te tiaki i te taiao me etahi atu ngoikoretanga, kaore hoki e tutuki i nga whakaritenga o te hanga papatipu ahumahi.Whakanuia te takawaenga matua o te rivaroxaban 4-(4-aminophenyl)- Ko te tukanga whakaputa o te 3-morpholinone me te whakahekenga o te utu o nga rauemi mata ka tino whakatairanga i te whakatairanga me te tono o te rivaroxaban.Kaore he ripoata mo te whakahiatotanga o te rivaroxaban i Haina.Kei rivaroxaban matou Ko te huarahi hangahanga 4-(4-aminophenyl)-3-morpholinone matua me te hangarau kua rangahaua houtia.E rua nga bromobenzene me te p-nitrobromobenzene hei rauemi timata.Ara tukanga.Arotahi ki te tukanga huringa o te mowhiti 3-morpholinone.