Identification of 1,5,7-Triazabicyclododecene and Polystyrene-Supported Superbases as Efficient Hydroxylaminolysis Agents of Sterically Hindered and Epimerizable Esters,Synlett

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Identification of 1,5,7-Triazabicyclododecene and Polystyrene-Supported Superbases as Efficient Hydroxylaminolysis Agents of Sterically Hindered and Epimerizable Esters
Synlett ( IF 1.7 ) Pub Date : 2018-04-13 , DOI: 10.1055/s-0036-1591551
Loic Tomas ₁ , Craig Harris ₁ , Romain Pierre ₁ , Frédéric Gaigne ₁ , Ghizlane El-Bazbouz ₁ , Grégoire Mouis ₁ , Gilles Ouvry ₁

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In modern pharmaceutical research, the need for reliable protocols for the preparation of chemical libraries in a controlled manner is quintessential to driving the Design-Make-Test cycle in drug discovery programs. In this letter, we communicate the identification of 1,5,7-triazabicyclododecene and polystyrene-supported superbases as efficient hydroxylaminolysis agents of sterically hindered and epimerizable esters and, to some extent, amides, using iChem Explorer® as the conditions scouting tool.

中文翻译：

鉴定 1,5,7-三氮杂双环十二烯和聚苯乙烯负载的超碱作为位阻和差向异构酯的有效羟氨解剂

在现代药物研究中，需要以受控方式制备化学库的可靠方案对于推动药物发现计划中的设计-制造-测试循环至关重要。在这封信中，我们使用 iChem Explorer® 作为条件探索工具，将 1,5,7-三氮杂双环十二烯和聚苯乙烯支持的超强碱鉴定为位阻和差向异构酯的有效羟氨解剂，在某种程度上，酰胺。

更新日期：2018-04-13

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