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

作者：Kulig Katarzyna^*; Boba Agnieszka; Bielejewska Anna; Gorska Magdalena; Malawska Barbara

来源：Tetrahedron: Asymmetry , 2009, 20(3): 322-326.

DOI：10.1016/j.tetasy.2009.01.029

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.

• 出版日期2009-2-26