氨基的脱保护？ 对甲苯磺酰基的脱去 tos非常稳定，它经得起一般酸解(tfa和hcl等）、皂化、催化氢解等多种条件得处理比受影响，常用萘钠、na/nh3(液) 和 li/nh3(液) 处理脱去。hbr/苯酚和mg/meoh 也是比较好的去保护方法。值得注意的是，na/nh3(液)的操作比较麻烦，并且会引起一些肽键的断裂和肽链的破坏。另外，有时hf/mecn回流也能脱去tos基。具体可以参考下面具体文献： 1. masuda, yui; mori, kenji et al., biosci. biotechnol. biochem., 2002, 66(7), 1531-1537; kaiser, alexander; balbi, miriam et al., tetrahedron: asymmetry, 1999, 10(5), 1001-1014; takikawa, hirosato; muto, shiu-etsu et al., tetrahedron, 1998, 54(13), 3141-3150; sugimura, hideyuki; miura, masayuki et al., tetrahedron: asymmetry, 1997, 8(24), 4089-4100 2. j. kovacs, u. r. ghatak., chem. ind. (london)., 1963, 913; dolence, e. kurt; roylance, jason b et al., tetrahedron: asymmetry, 2004, 15(20), 3307-3322; amat, mercedes; seffar, fatima et al., synthesis, 2001, 2, 267-275; hoye, thomas r; chen, minzhang et al., tetrahedron lett., 1996, 37(18), 3099-3100; hoye, thomas r; chen, minzhang et al., j. org. chem., 1999, 64(19), 7184-7201 3. burgess, kevin; liu, lee t et al., j. org. chem., 1993, 58(17), 4758-4763 4. kotek, jan; lebduskova, petra et al., chem. europ. j., 2003, 9(23), 5899-5915; calvisi, giuseppina; dell-uomo, natalina et al., eur. j. org. chem., 2003, 23, 4501-4506; currie, gordon s; drew, micheal g. b et al., j. chem. soc. perkin trans. 1, 2000, 17, 2982-2990; davis, franklin a; srirajan, vaidyanathan et al., j. org. chem., 2000, 65(10), 3248-3251; davis, franklin a; liu, hu et al., j. org. chem., 1999, 64(20), 7559-7567; drury, william j; ferraris, dana et al., j. am. chem. soc., 1998, 120(42), 11006-11007 5. y. yokoyama, t. matsumoto et al., j. org. chem., 1995, 60, 1486; b. nyasse, l. grehn et al., j. chem. soc. chem. commun., 1997, 1017; nenajdenko, valentine g; karpov, alexei s et al., tetrahedron: asymmetry, 2001, 12(18), 2517-2528 6. takikawa, hirosato; maseda, takeshi et al., tetrahedron lett., 1995, 36(42), 7689-7692查看更多
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