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探索利用三甲基铝作为裂解试剂的砜键：磺酰胺和脲的固相合成。

Exploring a sulfone linker utilizing trimethyl aluminum as a cleavage reagent: solid-phase synthesis of sulfonamides and ureas.

机构信息

Department of Applied Chemistry, National Chiao Tung University, Hsinchu 30050, Taiwan.

出版信息

Mol Divers. 2012 Aug;16(3):463-76. doi: 10.1007/s11030-012-9380-3. Epub 2012 Jun 30.

DOI:10.1007/s11030-012-9380-3
PMID:22752658
Abstract

A novel and efficient cleavage reagent, trimethyl aluminum, for traceless sulfinate-functionalized resin has been developed. The synthesis of sulfonamide and urea derivatives via a traceless solid-phase sulfone linker strategy through six synthetic steps comprising utilization of trimethyl aluminum as a novel cleavage reagent was also established. An insight of the plausible mechanism of the cleavage reaction was discussed.

摘要

一种新颖高效的脱保护试剂三甲基铝已被开发用于无残留亚磺酸盐功能化树脂。通过使用三甲基铝作为一种新型的裂解试剂，建立了通过无残留固相砜连接基策略合成磺酰胺和脲衍生物的方法，该方法共包含六个合成步骤。还讨论了裂解反应可能的机理。

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A nonpeptidic reverse-turn scaffold stabilized by urea-based dual intramolecular hydrogen bonding.一种基于脲基双分子内氢键稳定的非肽反向转弯支架。
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Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer.
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J Med Chem. 2011 Jun 23;54(12):4092-108. doi: 10.1021/jm200112k. Epub 2011 May 24.
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