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lgq101木虫 (小有名气)
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[求助]
求翻译~~~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. Accordingly, seven scaffolds (5, 6, 8, 26–29) were produced with three variations at this position (amine, sulfinamide, sulfonamide). Three scaffolds required prior oxidation to the tertbutylsulfonamide to enable the cycloaddition reactions (7, 9, 10) and were limited to this functionality because it could not be cleaved effectively under a variety of conditions (e.g., PhSH, K2CO3; TFA, anisole; TfOH, anisole). |
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zuodg
铁杆木虫 (正式写手)
有为青年
- 翻译EPI: 180
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【答案】应助回帖
lgq101(金币+15, 翻译EPI+1): 谢谢~~~~ 2011-06-10 19:25:54
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磺胺基团的多样性与文库裂解 我们手头已有10类结构骨架，接下来我们研究叔正丁基亚磺酸胺基团的结构多样性。最初我们选择lynchpin部分原因是其对酸不稳定（40）。我们很高兴的发现，磺胺可以被1 M 盐酸（常温，二噁英/THF溶解）水解产生相应次级胺二不会损坏TBDAS（流程图2）。还结果为将来修饰此位置（N-乙酰化，N-烷基化，等）产生更多的化学多样性创造了条件。另外，间氯过氧苯甲酸(m-CPBA)处理磺胺（二氯甲烷, 0 °C)也能高效的产生对应的叔丁基亚磺酸胺。相应的，产生了7个（5, 6, 8, 26–29）结构骨架，对应位置具有三种变化（胺，亚磺酸胺，磺酸胺）。三个结构骨架需要预先氧化生成叔丁基磺酸胺，进而发生环化加成反应（7,9,10）。在诸多反应条件下（如PhSH, K2CO3; TFA, anisole; TfOH, anisole）不能够被裂解下来导致其功能局限于此。 |
2楼2011-06-10 16:01:15
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