Application of cyclic sulfates in the synthesis of enantiomers of 1-[3-(4-aryl-piperazin-1-yl)-2-hydroxy-propyl]-pyrrolidin-2-one

被引：3

作者：

Kulig, Katarzyna ^{[1
]}

Boba, Agnieszka ^{[1
]}

Bielejewska, Anna ^{[2
]}

Gorska, Magdalena ^{[2
]}

Malawska, Barbara ^{[1
]}

机构：

[1] Jagiellonian Univ, Coll Med, Fac Pharm, Dept Physicochem Drug Anal, PL-30688 Krakow, Poland

[2] Polish Acad Sci, Inst Phys Chem, Warsaw, Poland

来源：

TETRAHEDRON-ASYMMETRY | 2009年 / 20卷 / 03期

关键词：

ADRENOLYTIC ACTIVITY; DERIVATIVES; ALCOHOLS; ESTERS;

D O I：

10.1016/j.tetasy.2009.01.029

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

The synthesis of enantiomers of 1-[3-(4-aryl-piperazin-1-yl)-2-hydroxy-propyl]-pyrrolidin-2-one derivatives is described. These enantiomers; were synthesized starting from (R)- or (S)-1-chloro-2,3-dihydroxypropane using relevant cyclic sulfates as chiral intermediates. The enantiomeric purities of the final compounds were in the range of 99.3-100.0%, as determined by high performance liquid chromatography. The final compounds were found to display moderate potency as ligands for alpha(1)-adrenoreceptors. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：322 / 326

页数：5

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