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

SYNLETT(2018)

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摘要
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 (R) as the conditions scouting tool.
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关键词
hydroxylaminolysis,hydroxamic acid,TBD,polymer-supported superbases,superbases,non-racemizing process
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