IB-643, SPA-S-753, -Drug Synthesis Database

【结构式】

【药物名称】IB-643, SPA-S-753

【化学名称】21-[3,6-Dideoxy-3-[2-(dimethylamino)acetamido]-beta-D-mannopyranosyloxy]-N-[2-(dimethylamino)ethyl]-15,19-epoxy-3,7,9,11,13,15,17,41-octahydroxy-36,38-dimethyl-43-[4-(methylamino)phenyl]-5,43-dioxo-22(E),24(E),26(E),28(E),30(E),32(E),34(E)-tritetracontaheptaeno-37-lactone diaspartate
　　　　　　33-[3,6-Dideoxy-3-[2-(dimethylamino)acetamido]-beta-D-mannopyranosyloxy]-N-[2-(dimethylamino)ethyl]-1,3,5,7,9,13,37-heptahydroxy-17-[4-hydroxy-1-methyl-6-[4-(methylamino)phenyl]-6-oxohexyl]-18-methyl-11,15-dioxo-16,39-dioxabicyclo[33.3.1]nonatriaconta-19(E),21(E),23(E),25(E),27(E),29(E),31(E)-heptaene-36-carboxamide diaspartate

【CA登记号】143563-20-6, 143483-67-4 (free base)

【分子式】C₇₅H₁₁₇N₇O₂₇

【分子量】1548.79944

【开发单位】SPA (Originator), IntraBiotics (Licensee), Kaken (Licensee)

【药理作用】Antifungal Agents, ANTIINFECTIVE THERAPY, Treatment of Protozoal Diseases

合成路线1

By condensation of partricin A 2-(dimethylamino)ethylamide (I) with N,N-dimethylglycine (II) by means of triethylamine and diphenyl phosphoroazidate (DPAZ) in dimethylacetamide.

参考文献中间体

【1】 Castañer, J.; Fromtling, R.A.; SPA-S-753. Drugs Fut 1997, 22, 8, 846.
【2】 Bruzzese, T.; Signorini, M.; Ottoni, F. (SPA (Societa Prodotti Antibiotici)); Partricin derivs. EP 0489308; US 5298495 .

中间体序号	中间体编号	品名	CAS号	分子式	供应商	用于合成
(I)	16764	33-[[(2R,3S,4S,5S,6R)-4-amino-3,5-dihydroxy-6-methyltetrahydro-2H-pyran-2-yl]oxy]-N-[2-(dimethylamino)ethyl]-1,3,5,7,9,13,37-heptahydroxy-17-[4-hydroxy-1-methyl-6-[4-(methylamino)phenyl]-6-oxohexyl]-18-methyl-11,15-dioxo-16,39-dioxabicyclo[33.3.1]nonatriaconta-19,21,23,25,27,29,31-heptaene-36-carboxamide		C₆₃H₉₆N₄O₁₈	详情	详情
(II)	16765	2-(dimethylamino)acetic acid; N,N-Dimethylglycine	1118-68-9	C₄H₉NO₂	详情	详情

Extended Information