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有机化学
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有机化学 ›› 2007, Vol. 27 ›› Issue (01): 103-108. 上一篇    下一篇

研究论文

酰基辅酶A : 胆固醇酰基转移酶抑制剂Beauveriolide I的全合成

田华，焦晓臻，谢平*，梁晓天   

  1. (中国协和医科大学中国医学科学院药物研究所 北京 100050)
  • 收稿日期:2006-04-03 修回日期:2006-06-27 发布日期:2006-12-30
  • 通讯作者: 谢平

Total Synthesis of Acyl-CoA: Cholesterol Acyltransferase Inhibitor Beauveriolide I

TIAN Hua,JIAO Xiao-Zhen,XIE Ping*,LIANG Xiao-Tian   

  1. (Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050)
  • Received:2006-04-03 Revised:2006-06-27 Published:2006-12-30
  • Contact: XIE Ping

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报道了酰基辅酶A : 胆固醇酰基转移酶抑制剂beauveriolide I的全合成. Beauveriolide I结构中的饱和脂肪酸具有两个相邻的手性中心, 是合成的关键中间体, 以 (4R)-4-苄基-3-丙酰基-2-噁唑烷酮和3-苄氧丙醛为起始原料制备得到. Beauveriolide I的结构经1H NMR, 13C NMR, MS和IR谱确定.

关键词: 全合成, 胆固醇酰基转移酶抑制剂, beauveriolide I

The total synthesis of beauveriolide I, an inhibitor of acyl-CoA: cholesterol acyltransferase (ACAT), was described. The fatty acid moiety with two contiguous chiral centers in beauveriolide I, a key intermediate, has been prepared via (4R)-4-benzyl-3-propionyl-2-oxazolidinone and 3-benzyloxypropio- naldehyde as starting materials. The structure of beauveriolide I was confirmed by 1H NMR, 13C NMR, MS and IR spectra.

Key words: total synthesis, beauveriolide I, chole-sterol acyltransferase inhibitor