Stereoselective synthesis of 2-azetidinones as cholesterol-absorption inhibitors

被引：21

作者：

Annunziata, R

Benaglia, M

Cinquini, M

Cozzi, F

机构：

[1] Univ Milan, Ctr CNR, I-20133 Milan, Italy

[2] Univ Milan, Dipartimento Chim Organ & Ind, I-20133 Milan, Italy

来源：

TETRAHEDRON-ASYMMETRY | 1999年 / 10卷 / 24期

关键词：

D O I：

10.1016/S0957-4166(99)00566-2

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

The synthesis of two 2-azetidinones possessing powerful cholesterol-absorption inhibition properties has been accomplished by a short and highly stereoselective reaction sequence. The key step is the condensation of the titanium enolate of the easily prepared 2-pyridylthioester (R)-11 with imine 6 which affords the desired beta-lactam intermediate in the correct relative and absolute configuration. Conversion to the pharmacologically active compounds is readily accomplished by simple functional group manipulation. (C) 2000 Elsevier Science Ltd. AII rights reserved.

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页码：4841 / 4849

页数：9

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