A practical synthesis of the serotonin 5-HT2A receptor antagonist MDL 100907, its enantiomer and their 3-phenolic derivatives as precursors for [11C]labeled PET ligands
A practical synthesis of the serotonin 5-HT2A receptor antagonist MDL 100907, its enantiomer and their 3-phenolic derivatives as precursors for [11C]labeled PET ligands
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DOI：
10.1016/s0968-0896(00)00175-9
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发表时间：
2000-10-01
影响因子：
3.5
通讯作者：
Rice, KC
中科院分区：
文献类型：
--
作者：
Ullrich, T;Rice, KC
本文报道了选择性5-HT2A受体拮抗剂MDL-100907的3-酚类前体的合成方法。该路线还应用于对映体系列，从而提供了3-[C-11]MDL 100907及其对映体的直接前体作为正电子发射断层扫描的配体。类似的方法也被开发用于直接合成MDL 100907及其对映体MDL 100009。这些路线利用了N-NOR中间体的经典光学拆分，至少有98%的对映体过量，并且很容易得到多种N-和3-O-取代对映体的多克数量的手性前体。(C)2000爱思唯尔科学有限公司。保留所有权利。
A practical synthesis of the 3-phenolic precursor of MDL 100907, a selective 5-HT2A receptor antagonist, is described. The route was also applied to the enantiomeric series, thus affording the direct precursors of both 3-[C-11]MDL 100907 and its enantiomer as ligands for positron emission tomography. Similar methodology was developed for the direct synthesis of MDL 100907 and its enantiomer, MDL 100009. The routes utilized classical optical resolution of the N-nor intermediates in at least 98% enantiomeric excess and easily afforded multigram amounts of the chiral precursors of a variety of N- and 3-O-substituted enantiomers. (C) 2000 Elsevier Science Ltd. All rights reserved.