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本文报道了带保护基的四核苷三磷酸(Bz)A_(bzp)~(bz)U_(bzp)U_(bzp)C_(Bz)~(bz),(9),(Bz)A_(bzp)~(bz)U_(bzp)C_(bzp)~(bz)U(Bz_2(15),C_(bzp)~(bz)G_(ibup)~(ac)G_(ibup)~(ac)A_((Bz)_2)~((bz)_2)(24)和四核苷酸(Bz)一A_(bzp)~(bz)U_(bzp)U_(bzp) Cv_(bzp)~(bz)(29)的合成。三个四核苷三磷酸均用相应的二核苷二磷酸和二核苷一磷酸,即化合物9由(Bz)A_(bzp)~(bz)U_(bzp)(4)和U_(bzp)C_((Bz)_2)~(bz)(8),化合物15由4和C_(bzp)~(bz)U(Bz)_2(14),化合物24由(McOTr)C_(bzp)~(bz)G_(ibup)~(ac)(19)和G_(ibup)~(ac)A_(Bz)_2~((bz)_2)(23)缩合而得。四核苷酸(Bz)A_(bzp)~(bz)U_(bzp)U_(bzp)C_(bzp)~(bz)(29)由化合物4和二核苷酸U_(bzp)~(bz)(28)缩合而成。四者均用二环己基碳二亚胺为缩合剂。化合物9、15、24和29在去保护基、纯化后分别得到纯的ApUpUpC(10)、ApUpCpU(16)、CpGpGpA(25)和ApUpUpCp(30)。在反应后处理条件和二乙基氯乙基纤维素柱层析条件下,对化合物G_p~(ac)、G_p~(ibu)、G_(acp)~(ac)、G_(ibup)~(ac)、G_(bzp)~(ac)和G_(ibup)~(ibu)上的酰基保护基的稳定性作了比较。
In this paper, we reported the protection of tetranucleosides triphosphates (Bz) A_ (bzp) ~ (bz) U_ (bzp) U_ (bzp) C_ (Bz) ~ (bz), (9), (Bz) A_ ) bz U bzp C bzp bz U Bz_2 15 bzp bz G ibup ac G ibup ac - (Bz) _2) ~ ((bz) _2) (24) and tetranucleotide (Bz) -A bzp ~ (bz) U bzp U bzp Cv bzp ~ ). The three tetranucleosides triphosphates were treated with the corresponding dinucleoside diphosphate and dinucleoside monophosphate, that is, the compound 9 consisted of (Bz) A bzp bz U bzp 4 and (Bzp) C_ ((Bz) _2) ~ (bz) (8), Compound 15 consists of 4 and C_ (bzp) ~ (bz) U (bz) G_ (ibup) ~ (ac) (19) and G_ (ibup) ~ (ac) A_ (Bz) _2 ~ ((bz) _2) (23) (Bzp) ~ (bzp) U ~ (bzp) C ~ (bzp) ~ (bz) (29) is synthesized from the condensation of compound 4 and dinucleotides U bzp to bz 28 . All of them were dicyclohexylcarbodiimide as condensing agent.Compounds 9, 15, 24 and 29 were deprotected and purified to give pure ApUpUpC (10), ApUpCpU (16), CpGpGpA (25) and ApUpUpCp (30) .After the reaction conditions and diethylchloroethyl cellulose column chromatography, the compounds G_p ~ (ac), G_p ~ (ibu), G acp ac, G_ ibup) ~ (ac), G_ (bzp) ~ (ac), and G ibup ~ (ibu) were compared.