CAS: 2185-03-7; (S)-3-Aminodihydrofuran-2(3H)-One Hydrochloride

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L-蛋氨酸置于盐酸,四丁基溴化铵,氯乙酸甲酯体系中,用 水 用作溶剂,以83 %的收率获得(S)-α-氨基-γ-丁内酯 盐酸盐
参考文献:环三肽天然产物anacine,Aurantiomide C,Polonimides A和c,Verrucine F的全合成
标题:环三肽天然产物anacine,Aurantiomide C,Polonimides A和c,Verrucine F的全合成
摘要:通过涉及亲电子高丝氨酸内酯中间体的关键环缩合的原始策略描述了具有中心哌嗪[2,1-B ]喹唑啉-3,6-二酮核心的环三肽天然产物的全合成.亚烷基是在环缩合过程中通过自氧化自发安装的,而丙酰胺侧链是通过溴乙基中间体的镍催化氨基羰基化引入的.对于这种高度功能化的中间体来说,最后的反应是前所未有的.最后,我们探索了天然产物的结构修饰和相互转化.总体而言,这项工作产生了 Anacine,Aurantiomide C,Polonimides A 和 C 以及 Verrucine F.
Doi:10.1021/acs.Orglett.4C00658

专利信息

专利号:US-8580998-B2
优先权日:2008-12-11
标题 :Preparation of alkenes by mild thermolysis of sulfoxides
发明人：LONG TIMOTHY EDWARD; PATEL SRAVAN KUMAR
权利人:LONG TIMOTHY EDWARD; PATEL SRAVAN KUMAR; UNIV GEORGIA
摘要:Embodiments of this disclosure, among others, encompass methods for generating alkenes under mild thermolytic conditions that can provide almost total conversion of a precursor compound to an alkene without isomerization or the need to chromatographically purify the final product By selectively blocking the amino and carboxy groups of the derivatized amino acid, the methods of the disclosure provide for the synthesis of a peptide having the vinylglycine moiety at either the carboxy or the amino terminus of the peptide The mild conditions for the thermolytic removal of an o-NO 2 -phenyl substituted aryl group ensure that there is minimal if any damage to thermally sensitive conjugates such as a peptide bearing the vinylglycine The methods of the present disclosure have practical applications for the preparation of unsaturated compounds under mild, thermolytic conditions.

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