Chemoenzymatic synthesis of piperoxan,prosympal, dibozane,and doxazosin |
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Authors: | Abdul Rouf Pankaj Gupta Mushtaq A Aga Brijesh Kumar Asha Chaubey Rajinder Parshad Subhash C Taneja |
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Institution: | CSIR-Indian Institute of Integrative Medicine, Canal Road, Jammu 180001, J&K, India |
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Abstract: | The synthesis of both enantiomers of 1,4-benzodioxan-2-carboxylic acid 1, a key synthetic intermediate for the therapeutic agents piperoxan, prosympal, dibozane, and doxazosin was achieved with good yields and high enantioselectivities via the Arthrobacter sp. lipase catalyzed kinetic resolution of ester (±)-17a. The influence of the co-solvents and the immobilization of the lipase upon kinetic resolution demonstrated that immobilized whole cells, in the presence of n-butanol as a co-solvent, resulted in the optimal resolution of the substrate (ee ~99%, E = 535) at 258 mmol (50 g/L) substrate concentration. |
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