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
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
收藏
页码:322 / 326
页数:5
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