合成路线1

In a further synthetic strategy, an azido precursor of spermidine (CXXX) was used in the reductive amination step. Condensation between 1,3-diaminopropane (CXXIV) and 4-chloro-1-butanol (CXXV) provided the diamino alcohol (CXXVI). Protection of the amino groups of (CXXVI) with di-tert-butyl dicarbonate yielded alcohol (CXXVII), which was converted to mesylate (CXXVIII) by treatment with methanesulfonyl chloride and triethylamine. Subsequent mesylate displacement in (CXXVIII) with NaN3 in DMF furnished the di-Boc-protected azide (CXXIX). The Boc protecting groups of (CXXIX) were then removed by treatment with HCl to give the desired diamino azide (CXXX). Reductive amination of the 3-keto steroid (CXXI) with amine (CXXX) yielded the 3-beta amino steroid (CXXXI). The azido group of (CXXXI) was finally reduced to the title triamino compound by catalytic hydrogenation over Raney-Ni.