Preparation of optically pure 4-(hydroxymethyl)-2-pentadecyl-1,3-dioxolanes and their corresponding phosphodiester ether lipid derivatives

Chem Phys Lipids. 2001 Nov;113(1-2):111-22. doi: 10.1016/s0009-3084(01)00185-2.

Abstract

Semi-preparative HPLC on a chiral stationary phase (Chiracel OD) was utilized in the course of this synthesis to separate the four possible diastereomers [cis-(2R,4S)-2a, trans-(2S,4S)-2b, cis-(2S,4R)-2a', and trans-(2R,4R)-2b'] of a 2,4-disubstituted-1,3-dioxolane into optically pure forms (100% de, 100% ee). The syntheses of phosphodiester head group derivatives from each of these four conformationally constrained diastereomeric dioxolanes gave phospholipids which are monocyclic ether lipid analogs. First, the series of four [[(2-pentadecyl-1,3-dioxolan-4-yl)methyl]oxy]phosphocholines 5 were synthesized to give optically pure conformationally constrained analogues of ET-16-OCH(3). A head group variation was also demonstrated by the syntheses of the four diastereomeric [[(2-pentadecyl-1,3-dioxolan-4-yl)-methyl]oxy]phospho-beta-(N-methylmorpholino)ethanols 6.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Chemistry, Pharmaceutical
  • Dioxolanes / chemical synthesis*
  • Dioxolanes / chemistry
  • Drug Design
  • Optical Rotation
  • Phospholipid Ethers / chemical synthesis*
  • Phospholipid Ethers / chemistry
  • Stereoisomerism

Substances

  • Dioxolanes
  • Phospholipid Ethers