合成路线:Acyclovir (I) was coupled with N-Cbz-L-valine (II) in the presence of DCC and DMAP to afford the Cbz-protected valyl ester (III).The N-benzyloxycarbonyl group of (III) was then removed by either hydrogenation over Pd/C or by transfer hydrogenation in the presence of formic acid.
参考文献标题:Guanine deriv.
文献作者:Partin,J.M.; Winnike,R.A.; Carter,B.H.; Lake,P.G.; Varlashkin,P.G.; Grubb,W.B.III; Conway,G.A.; Skinner,D.M.; Whatrup,D.J.(GlaxoSmithKline plc)
参考来源:WO 9622291
合成路线:In an alternative procedure,condensation of L-valine (IV) with methyl acetoacetate (V) in the presence of NaOH produced the enamine-protected valine sodium salt (VI).Condensation of (VI) with the tosylate (VII),(prepared from acyclovir (I) and tosyl chloride) afforded ester (VIII).Then,acidic hydrolysis of the enaminoester moiety of (VIII) furnished the target valine ester.Similar procedures were also reported using omega-mesyl and omega-chloro acyclovir.
参考文献标题:Process of preparation of valacyclovir and relevant intermediates
文献作者:Montoro,M.; Pirovano,S.
参考来源:WO 9803553
合成路线:The esterification of acyclovir (I) with N-(tert-butoxycarbonyl)-L-valine (II) by means of EDC,TEA and DMAP in DMF gives the corresponding ester (III) which is finally deprotected by means of HCl in water to afford the target valacyclovir.
参考文献标题:Synthesis and purification of valacyclovir
文献作者:Pertsikov,B.; Etinger,M.Y.; Yuzefovich,M.; Nisnevich,G.A.; Tishin,B.; Blasberger,D.; Yudovich,L.M.; Dolitzki,B.Z.(Teva Pharmaceutical Industries Ltd.; Teva Pharmaceuticals USA,Inc.)
参考来源:WO 0341647
合成路线:Acyclovir (I) was coupled with N-Cbz-L-valine (II) in the presence of DCC and DMAP to afford the Cbz-protected valyl ester (III).The N-benzyloxycarbonyl group of (III) was then removed by either hydrogenation over Pd/C or by transfer hydrogenation in the presence of formic acid.
参考文献标题:Amino acid ester prodrugs of acyclovir
文献作者:Beauchamp,L.M.; et al.
参考来源:Antivir Chem Chemother 1992,3(3),157
合成路线:Acyclovir (I) was coupled with N-Cbz-L-valine (II) in the presence of DCC and DMAP to afford the Cbz-protected valyl ester (III).The N-benzyloxycarbonyl group of (III) was then removed by either hydrogenation over Pd/C or by transfer hydrogenation in the presence of formic acid.
参考文献标题:Transport of acyclovir ester prodrugs through rabbit cornea and SIRC-rabbit corneal epithelial cell line
文献作者:Tak,R.V.; et al.
参考来源:J Pharm Sci 2001,90(10),1505
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