Diquafosol tetrasodium, DE-089, U2P4, Up4U, KPY-998, INS-365

地夸磷索四钠 地夸磷索 Chemical Name: P1,P4-Di(uridine-5'-tetraphosphate) tetrasodium salt; Uridine-5'-(pentahydrogen tetraphosphate) P'''--5'-ester with uridine tetrasodium salt; P1,P4-Bis(5'uridyl)tetrahydrogen tetraphosphate tetrasodium salt
CAS No. 211427-08-6, 59985-21-6 (free acid)
项目整合开发状态: Pre-Registered
项目研究机构: University of North Carolina (Originator), Allergan (Licensee), Inspire Pharmaceuticals (Licensee), Santen (Licensee)
合成路线:INS-365 can also been obtained by the following ways:4) Dimerization of uridine-5'-monophosphate tributyl-ammonium salt (I) with bis(tributylammonium) pyrophosphate (II) by means of CDI,followed by purification by semipreparative ion璭xchange chromatography.5) Dimerization of uridine-5'-monophosphate tributyl-ammonium salt (I) with pyrophosphoryl chloride (III) in pyridine,followed by chromatographic purification as before.6) Condensation of uridine (IV) with POCl3 and bis(tributylammonium) pyrophosphate (II) by means of tributylamine in trimethyl phosphate,followed by chromatographic purification as before.7) Dimerization of uridine-5'-diphosphate tributylammonium salt (V) by means of CDI in DMF,followed by purification over Dowex 50Wx4 Na+.8) Condensation of uridine-5'-triphosphate tributylammonium salt (VI) with uridine-5'-monophosphate tributyl-ammonium salt (I) by means of DCC in DMF,followed by chromatographic purification as before.9) Reaction of uridine-5'-monophosphate tributylammonium salt (I) with CDI in DMF,followed by condensation with uridine-5'-triphosphate (VI) and chromatographic purification as before.