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lgq101木虫 (小有名气)
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[求助]
求翻译（有机合成）！！！~~~谢谢
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| Diversification of Sulfinamide Moiety and Library Cleavage. With these 10 classes of scaffolds in hand, we next investigated diversification of the tert-butylsulfinamide moieties. We had originally selected this lynchpin in part because of its known acid-lability (40), and were pleased to find that the support-bound sulfinamides could be cleaved with HCl [1 M in dioxane/THF, room temperature (RT)] to afford the corresponding secondary amines without compromising the TBDAS linker (Scheme 2). This result opens the door for additional diversification of this position in the future (N-acylation, N-alkylation, etc.). Alternatively, treatment of the sulfinamides with meta-chloroperbenzoic acid (m-CPBA) (CH2Cl2, 0 °C) also provided the corresponding tert-butylsulfonamides efficiently. |
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【答案】应助回帖
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sltmac(金币+1): 感谢应助，欢迎常来~ 2011-06-30 08:48:18
lgq101(金币+20, 翻译EPI+1): 2011-07-01 11:43:39
sltmac(金币+1): 感谢应助，欢迎常来~ 2011-06-30 08:48:18
lgq101(金币+20, 翻译EPI+1): 2011-07-01 11:43:39
| 半硫磺酰胺和库开裂的多元化，有这10个系列方案在手，随后我们研究了叔丁基半硫磺酰胺的多元化，起初我们选择了部分 lynchpin （核心）因为我们知道它的酸性，很高兴的发现支点绑定的硫磺酰胺在没有相应的TBDAS时可以用HCl 开裂（二恶烷，THF，RT）得到相应的二级胺(Scheme 2). 这个结果为将来在这个位置的额外多元化开启先河，（N-酰化，N-烷化）。或者，用金属的氯苯磺酸(m-CPBA)处理硫磺酰胺也高效的得到相应的叔丁基硫磺酰胺。 |
2楼2011-06-30 00:51:28