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.

中文翻译：

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化学酶法合成哌咯烷，前s，地博z和多沙唑嗪

1,4-苯并二恶烷-2-羧酸1的两种对映异构体的合成，是通过节杆菌获得的，具有高收率和高对映选择性，是治疗剂哌咯烷，脯氨酰胺，地波氮烷和多沙唑嗪的关键合成中间体。脂肪酶酯（±）的催化动力学拆分- 17A。助溶剂和脂肪酶固定化对动力学拆分的影响表明，在存在正丁醇作为助溶剂的情况下，固定化全细胞可导致底物的最佳拆分（ee〜99％，E 底物浓度为258 mmol（50 g / L）时= 535）。