Stereocontrolled syntheses of epimeric 3-aryl-6-phenyl-1-oxa-7-azaspiro[4.5]decane NK-1 receptor antagonist precursors

被引：31

作者：

Kulagowski, JJ ^{[1
]}

Curtis, NR ^{[1
]}

Swain, CJ ^{[1
]}

Williams, BJ ^{[1
]}

机构：

[1] Merck Sharp & Dohme Res Labs, Neurosci Res Ctr, Dept Med Chem, Harlow CM20 2QR, Essex, England

来源：

ORGANIC LETTERS | 2001年 / 3卷 / 05期

关键词：

D O I：

10.1021/ol006944a

中图分类号：

O62 [有机化学];

学科分类号：

070303 [有机化学]; 081704 [应用化学];

摘要：

[GRAPHICS] Complementary stereoselective syntheses of individual C3 epimers of the NK-1 receptor antagonist precursor 1 have been developed. Both diastereomers were derived from the common intermediate 3; introduction of the 3S stereocenter in 1a was achieved through hydrogenation of an arylated dihydrofuran, whereas the corresponding stereogenic center in 1b was installed using a stereo- and regioselective alkene hydroarylation.

引用

页码：667 / 670

页数：4

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