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

12.Qhov nruab nrab 4-(4-aminophenyl)-3-morpholinone (1) ntawm cov tshuaj anticoagulant rivaroxaban tau npaj los ntawm ob txoj kev: ①Bromobenzene tau ua tiav nrog ethanolamine thiab chloroacetyl chloride kom tau 4-benzene Cov morpholinone tom qab ntawd txo qis. 1, thiab tag nrho cov txiaj ntsig yog kwv yees li 32%;②Bromobenzene yog thawj nitrated, thiab ces reacted nrog ethanolamine kom tau 2-(4-nitroanilino) ethanol, uas yog ces kaw los ntawm chloroacetyl chloride.Cov tshuaj tiv thaiv txo qis ua rau 1, thiab tag nrho cov txiaj ntsig yog li 47%.

Rivaroxaban yog ib hom tshuaj anticoagulant tshiab uas tuaj yeem noj ncaj qha rau ntawm qhov ncauj.Nws ncaj qha inhibits kev ua kom coagulation yam Xa, muaj cov nyhuv anticoagulant tseeb, tsis tas yuav tsum tau saib xyuas tas li, thiab muaj kev nyab xeeb siab.Nrog rau kev kho mob daim ntawv thov ntawm rivaroxaban, Qhov kev thov rau rivaroxaban yuav maj mam nce.Lub npe tshuaj rivaroxaban yog 5-chloro-N-(((5S) -2-oxo-3-[4- (3-oxo- 4-morpholinyl)phenyl)-1,3-oxazolidine-5-yl)methyl 2-thiophenecarboxamide.Tam sim no muaj ob txoj kev siv hluavtaws tshaj tawm hauv cov ntaub ntawv, thiab ob txoj hauv kev tau siv Ib qho nruab nrab 4-(4-aminophenyl)-3-morpholinone.Txawm hais tias muaj cov ntaub ntawv qhia txog kev sib txuas ntawm 4-(4-aminophenyl)-3-morpholinone hauv tsev thiab txawv teb chaws, muaj tus nqi siab ntawm cov khoom siv raw khoom.Siab, nyuaj rau yuav, lossis cov kev xav tau ntawm kev ua haujlwm siab dhau lawm, tsis yooj yim rau kev tuav, tsis ua rau muaj kev tiv thaiv ib puag ncig thiab lwm yam tsis zoo, thiab tsis ua raws li cov kev cai ntawm kev tsim khoom loj.Txhim kho qhov tseem ceeb nruab nrab ntawm rivaroxaban 4-(4-aminophenyl) - Cov txheej txheem tsim khoom ntawm 3-morpholinone thiab txo tus nqi ntawm cov khoom siv raw yuav twv yuav raug hu txhawb kev txhawb nqa thiab kev siv ntawm rivaroxaban.Tsis muaj ntawv tshaj tawm txog kev sib txuas ntawm rivaroxaban hauv Suav teb.Peb nyob ntawm rivaroxaban Qhov tseem ceeb nruab nrab 4-(4-aminophenyl)-3-morpholinone hluavtaws txoj kev thiab thev naus laus zis tau kawm tshiab.Ob bromobenzene thiab p-nitrobromobenzene raws li cov ntaub ntawv pib tau npaj.Txheej txheem txoj kev.Tsom ntsoov rau cov txheej txheem cyclization ntawm 3-morpholinone nplhaib.