合成路线:In a different method,acetylation of 3-amino-1,2-propanediol (I) yields the amide diol (II).Ketalization of cyclohexanone (III) with diol (II) furnishes the spiro dioxolane (IV).The acetamide function of (IV) is then hydrolyzed to amine (V) employing aqueous hydrazine.Amine (V) is condensed with N,N'-di-(carbobenzoxy)-N''-(trifluoromethylsulfonyl)guanidine (VI) to produce the protected guanidine (VII).The N-carbobenzoxy groups of (VII) are finally removed by hydrogenolysis over Pd/C.Alternatively,amine (V) is condensed with cyanogen bromide to produce the cyanamide (VIII).Then,reaction of cyanamide (VIII) with ammonium chloride in aqueous ammonia furnishes the title guanidine compound
参考文献标题:Endogenous retinoic acid receptor (RAR)-retinoid X receptor (RXR) heterodimers are the major functional forms regulating retinoid-responsive elements in adult human keratinocytes.Binding of ligands to RAR only is sufficient for RAR.RXR heterodimers to co
文献作者:Xiao,J.-H.; Durand,B.; Chambon,P.; Voorhees,J.J.
参考来源:J Biol Chem 1995,270(7),3001
合成路线:In a different method,acetylation of 3-amino-1,2-propanediol (I) yields the amide diol (II).Ketalization of cyclohexanone (III) with diol (II) furnishes the spiro dioxolane (IV).The acetamide function of (IV) is then hydrolyzed to amine (V) employing aqueous hydrazine.Amine (V) is condensed with N,N'-di-(carbobenzoxy)-N''-(trifluoromethylsulfonyl)guanidine (VI) to produce the protected guanidine (VII).The N-carbobenzoxy groups of (VII) are finally removed by hydrogenolysis over Pd/C.Alternatively,amine (V) is condensed with cyanogen bromide to produce the cyanamide (VIII).Then,reaction of cyanamide (VIII) with ammonium chloride in aqueous ammonia furnishes the title guanidine compound
参考文献标题:N-Hydroxyl derivatives of guanidine based drugs as enzymatic NO donors
文献作者:Xian,M.; Li,X.; Tang,X.; Chen,X.; Zheng,Z.; Galligan,J.J.; Kreulen,D.L.; Wang,P.G.
参考来源:Bioorg Med Chem Lett 2001,11(17),2377
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