PROCESS FOR PREPARATION OF PHARMACOLOGICALLY ACTIVE alpha-ASARONE DERIVED FROM TOXIC beta-ASARONE-RICH CALAMUS OIL

PROBLEM TO BE SOLVED: To develop a simple process for preparation of α-asrone exclusively with no inclusion of any other asarone isomers (namely β-isomer and/or γ-isomer). SOLUTION: This invention relates to a process for preparing high-purity α-asarone or trans-2,4,5-trimetoxycinnamaldehyde, and 2,4,5-trimethoxyphenylpropiophenone with a high yield from β-asarone-rich Acorus calmus oil including β-asarone or α-asarone and γ-asarone. The process comprise hydrogenation and following treatment with DDQ in a dried organic solvent, or α-asarone is further treated with β-asarone or β-asarone rich Acorus calamus oil in aqueous organic solvent to prepare the intermediate products, 2,4,5-trimethoxypropiophenone, then the product is reduced with sodium borohydride to prepare corresponding 2,4,5-trimethoxypropanol, and is finally treated with an dehydrogenation agent. COPYRIGHT: (C)2008,JPO&INPIT