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Berberine is natural product with various biological properties such as antibacterial,anticancer,antidiabetic and anti-inflammatory.Nevertheless,the clinically used berberine drugs display one or more limitations including toxicity,an urgent need is to improve bioavailability and pharmacological effect via modifying berberine.Thus the synthesis of berberine derivatives has been attracting an increasing interest.Herein a key intermediate containing an aldehyde group at 12-position of ±-tetrahydroprotoberberrubine was developed via an efficient and convenient procedure.