Objective: The design and improve synthesis of the key intermediate of D-biotin (lactone); Methods: A new half-ester was formed using inexpensive alcohol such as isopropanol, ethanol or methanol, instead of cyclohexanol which is expensive, followed by the resolution with the different chiral amines, reduction, the lactone was obtained; Results: The cost of the key process was decreased significantly. The optically active lactone was obtained with yield 32.58%. Conclusion: The improved process of D-biotin was successfully completed. The process will benefit from its simple operation and low cost, which is suit for large-scale industrial manufacture. |