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Y Hayashi---二苯脯氨硅醚催化剂一锅生成药物先导ABT

已有 3034 次阅读 2011-1-27 17:10 |系统分类:论文交流

ABT-341 was synthesized in high yield with excellent diastereo- and enantioselectivity in a one-pot process mediated by a diphenylprolinol silyl ether (see scheme; TMS=trimethylsilyl). Thus, an asymmetric Michael reaction, a domino Michael/Horner–Wadsworth–Emmons reaction combined with a retro-aldol reaction, base-catalyzed isomerization, amide-bond formation, and reduction of the nitro group all took place in a single flask.




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