关于在磷酸丝氨酸肽合成中使用2,2,2-三氯乙基基团进行磷酸盐保护的进一步研究。
Further studies on the use of 2,2,2-trichloroethyl groups for phosphate protection in phosphoserine peptide synthesis.
作者信息
Paquet A
机构信息
Food Research Centre, Department of Agriculture, Ottawa, Ontario, Canada.
出版信息
Int J Pept Protein Res. 1992 Jan;39(1):82-6. doi: 10.1111/j.1399-3011.1992.tb01559.x.
Boc-Ser(PO3Tc2)-OH, Z-Ser(PO3Tc2)-OH and Fmoc-Ser(PO3Tc2)-OH, derivatives useful for peptide synthesis, have been obtained in high yields by acylation of H-Ser(PO3Tc2)-OH.CF3COOH. The latter was obtained from Boc- or Z-Ser(PO3Tc2)-OBzl by simultaneous removal of the amino- and carboxy-protecting groups by Pd-catalyzed hydrogenolysis in acetic acid-trifluoroacetic acid solution. Removal of the Tc-protecting group was efficiently achieved by hydrogenolysis in aqueous ethanol.
用于肽合成的衍生物Boc-Ser(PO3Tc2)-OH、Z-Ser(PO3Tc2)-OH和Fmoc-Ser(PO3Tc2)-OH，通过H-Ser(PO3Tc2)-OH.CF3COOH的酰化反应以高产率获得。后者是由Boc-或Z-Ser(PO3Tc2)-OBzl在乙酸 - 三氟乙酸溶液中通过钯催化氢解同时去除氨基和羧基保护基团而得到的。通过在乙醇水溶液中进行氢解有效地实现了Tc保护基团的去除。
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