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

12.4-(4-aminophenyl)-3-morpholinone (1) ea anticoagulant rivaroxaban e lokisitsoe ka mekhoa e 'meli: ①Bromobenzene e ile ea sebelisoa ka tatellano ka ethanolamine le chloroacetyl chloride ho fumana 4-benzene The morpholinone e fokotsoa ho fokotsa nit. 1, mme kakaretso ea lihlahisoa ke hoo e ka bang 32%;②Bromobenzene e qala ka nitrate, ebe e sebetsa ka ethanolamine ho fumana 2-(4-nitroanilino)thanol, ebe e koaloa ke chloroacetyl chloride.Karabelo ea phokotso e hlahisa 1, mme kakaretso ea lihlahisoa e ka ba 47%.

Rivaroxaban ke mofuta o mocha oa anticoagulant o ka nkoang ka ho toba ka molomo.E thibela ka ho toba ts'ebetso ea coagulation factor Xa, e na le phello e tobileng ea anticoagulant, ha e hloke ho hlahlojoa ho tsoelang pele, 'me e na le tšireletso e phahameng.Ka ts'ebeliso ea bongaka ea rivaroxaban, Tlhokahalo ea rivaroxaban e tla eketseha butle-butle.Lebitso la lik'hemik'hale la rivaroxaban ke 5-chloro-N-(((5S) -2-oxo-3-[4- (3-oxo- 4-morpholinyl)phenyl)-1,3-oxazolidine-5-yl)methyl -2-thiophenecarboxamide.Hona joale ho na le litsela tse peli tsa maiketsetso tse tlalehiloeng libukeng, 'me litsela ka bobeli li sebelisoa An intermediate 4-(4-aminophenyl) -3-morpholinone.Le hoja ho na le litlaleho tse mabapi le ho qaptjoa ha 4-(4-aminophenyl) -3-morpholinone lapeng le linaheng tse ling, ho na le theko e batlang e phahame ea lihlahisoa tse tala.E phahameng, e thata ho reka, kapa litlhoko tsa ts'ebetso ea karabelo li phahame haholo, ho thata ho li utloisisa, ha li lumellane le ts'ireletso ea tikoloho le mefokolo e meng, 'me ha li fihlelle litlhoko tsa tlhahiso ea boima ba indasteri.Ntlafatsa senotlolo sa bohareng ba rivaroxaban 4- (4-aminophenyl)- Ts'ebetso ea tlhahiso ea 3-morpholinone le ho fokotseha ha theko ea thepa e tala ka sebele e tla khothalletsa ts'ebetso le ts'ebeliso ea rivaroxaban.Ha ho na tlaleho mabapi le ho qaptjoa ha rivaroxaban Chaena.Re ho rivaroxaban The key intermediate 4-(4-aminophenyl) -3-morpholinone synthetic route le thekenoloji li ithutile ka mokhoa o mocha.Li-bromobenzene tse peli le p-nitrobromobenzene e le lisebelisoa tsa ho qala lia sisinngoa.Tsela ea ho sebetsa.Tsepamisa maikutlo ts'ebetsong ea cyclization ea lesale la 3-morpholinone.