Synthesis of a library of complex macrodiolides employing cyclodimerization of hydroxy esters

被引：39

作者：

Beeler, AB

Acquilano, DE

Su, QB

Yan, F

Roth, BL

Panek, JS

Porco, JA

机构：

[1] Boston Univ, Dept Chem, Boston, MA 02115 USA

[2] Boston Univ, Ctr Chem Methodol & Library Dev, Boston, MA 02115 USA

[3] Case Western Reserve Univ, Sch Med, NIMH, Psychoact Drug Screening Program, Cleveland, OH 44106 USA

[4] Case Western Reserve Univ, Sch Med, Dept Biochem, Cleveland, OH 44106 USA

来源：

JOURNAL OF COMBINATORIAL CHEMISTRY | 2005年 / 7卷 / 05期

关键词：

D O I：

10.1021/cc050064b

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

The synthesis of complex macrodiolides involving microwave-accelerated transesterification of chiral, nonracemic, hydroxy esters is described. Methodology development studies indicate that both microwave power and reaction temperature play an important role in the efficiency of cyclodimerizations. Hydroxy ester monomer pairs were evaluated using an analytical rehearsal leading to the preparation of a 127-member library of highly diverse and stereochemically well-defined macrodiolides. Preliminary assays identified a novel macrodiolide antagonist of the kappa opioid receptor.

引用

页码：673 / 681

页数：9

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