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

12.Agbedemeji 4- (4-aminophenyl) -3-morpholinone (1) ti anticoagulant rivaroxaban ti pese sile nipasẹ awọn ọna meji: ①Bromobenzene ti ni aṣeyọri pẹlu ethanolamine ati chloroacetyl chloride lati gba 4-benzene morpholinone ti wa ni idinku lati dinku lati dinku lati dinku. 1, ati ikore lapapọ jẹ nipa 32%;②Bromobenzene jẹ iyọ akọkọ, lẹhinna fesi pẹlu ethanolamine lati gba 2- (4-nitroanilino) ethanol, eyiti o wa ni pipade nipasẹ chloroacetyl chloride.Idahun idinku naa ṣe agbejade 1, ati ikore lapapọ jẹ nipa 47%.

Rivaroxaban jẹ oriṣi tuntun ti anticoagulant ti o le mu ni ẹnu taara.O taara ṣe idiwọ imuṣiṣẹ ti ifosiwewe coagulation Xa, ni ipa anticoagulant pato, ko nilo ibojuwo lemọlemọ, ati pe o ni aabo giga.Pẹlu ohun elo ile-iwosan ti rivaroxaban, ibeere fun rivaroxaban yoo maa pọ si.Orukọ kemikali ti rivaroxaban jẹ 5-chloro-N-(((5S) -2-oxo-3-[4- (3-oxo- 4-morpholinyl) phenyl)) -1,3-oxazolidine-5-yl)methyl -2-thiophenecarboxamide.Lọwọlọwọ awọn ipa-ọna sintetiki meji ti a royin ninu awọn iwe-iwe, ati pe awọn ipa-ọna mejeeji lo An agbedemeji 4- (4-aminophenyl) -3-morpholinone.Botilẹjẹpe awọn ijabọ wa lori iṣelọpọ ti 4- (4-aminophenyl) -3-morpholinone ni ile ati ni okeere, idiyele ti o ga julọ wa ti awọn ohun elo aise.Ga, nira lati ra, tabi awọn ibeere iṣiṣẹ ifaseyin ga ju, nira lati di, ko ṣe itara si aabo ayika ati awọn ailagbara miiran, ati pe ko pade awọn ibeere ti iṣelọpọ ibi-iṣẹ iṣelọpọ.Mu agbedemeji bọtini ti rivaroxaban 4- (4-aminophenyl) - Ilana iṣelọpọ ti 3-morpholinone ati idinku idiyele ti awọn ohun elo aise yoo dajudaju igbega igbega ati ohun elo ti rivaroxaban.Ko si ijabọ lori iṣelọpọ ti rivaroxaban ni Ilu China.A wa ni rivaroxaban Bọtini agbedemeji 4- (4-aminophenyl) -3-morpholinone sintetiki ipa-ọna ati imọ-ẹrọ ti ni iwadi ni imotuntun.Bromobenzene meji ati p-nitrobromobenzene bi awọn ohun elo ti o bẹrẹ ni a dabaa.Ọna ilana.Fojusi lori ilana gigun kẹkẹ ti iwọn 3-morpholinone.