Methods for synthesis and preparation of alpha-glycosphingolipids are provided. Methods for synthesis of a-galactosyl ceramides, and pharmaceutically active analogs and variants thereof are provided. Novel alpha-glycosphingolipids are provided, wherein the compounds are immunogenic compounds which serve as ligands for NKT (natural killer T) cells. A process for preparing a chiral compound comprising an R-form or S- form of a glycosphingolipid of formula (1 ) is provided, wherein R
