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

12.The intermediate 4- (4-aminophenyl) -3-morpholinone (1) nke anticoagulant rivaroxaban kwadebere site na ụzọ abụọ: ①Bromobenzene na-emeghachi omume na ethanolamine na chloroacetyl chloride iji nweta 4-benzene morpholinone bụ mgbe ahụ nitrated iji belata. 1, na mkpokọta mkpụrụ bụ ihe dịka 32%;② A na-ebu ụzọ mee bromobenzene nitrated, wee meghachi omume na ethanolamine iji nweta 2- (4-nitroanilino) ethanol, nke chloroacetyl chloride mechiri.Mmeghachi omume mbelata na-emepụta 1, na mkpokọta mkpụrụ bụ ihe dịka 47%.

Rivaroxaban bụ ụdị ọgwụ mgbochi obi ọhụrụ nke enwere ike were ọnụ.Ọ na-egbochi ngwa ngwa nke coagulation factor Xa, nwere mmetụta anticoagulant doro anya, ọ dịghị achọ nlekota na-aga n'ihu, ma nwee nchekwa dị elu.Site na ngwa ụlọ ọgwụ nke rivaroxaban, ọchịchọ maka rivaroxaban ga-eji nwayọọ nwayọọ na-abawanye.Aha kemịkal nke rivaroxaban bụ 5-chloro-N-(((5S) -2-oxo-3-[4- (3-oxo- 4-morpholinyl) phenyl)) -1,3-oxazolidine-5-yl) methyl -2-thiophenecarboxamide.E nwere ugbu a ụzọ abụọ sịntetik na-akọ na akwụkwọ ndị ahụ, a na-ejikwa ụzọ abụọ ahụ An intermediate 4- (4-aminophenyl) -3-morpholinone.Ọ bụ ezie na e nwere akụkọ banyere njikọ nke 4- (4-aminophenyl) -3-morpholinone n'ụlọ na ná mba ọzọ, e nwere ọnụ ahịa dị elu nke mmeghachi omume akụrụngwa.Elu, siri ike ịzụta, ma ọ bụ ihe mmeghachi omume chọrọ chọrọ dị oke elu, siri ike ịghọta, adịghị akwado nchebe gburugburu ebe obibi na adịghị ike ndị ọzọ, ma ghara imezu ihe achọrọ nke mmepụta ihe mmepụta ihe.Na-ebuli isi etiti nke rivaroxaban 4- (4-aminophenyl) - Usoro mmepụta nke 3-morpholinone na mbelata ọnụahịa nke akụrụngwa ga-akwalite nkwalite na ngwa nke rivaroxaban.Enweghị akụkọ gbasara njikọ nke rivaroxaban na China.Anyị nọ na rivaroxaban Isi etiti 4- (4-aminophenyl) -3-morpholinone synthetic ụzọ na teknụzụ ka amụrụ ọhụrụ.A na-atụ aro bromobenzene abụọ na p-nitrobromobenzene dị ka ihe mmalite.Usoro ụzọ.Lekwasị anya na usoro ịgba ígwè nke mgbanaka 3-morpholinone.