Nghiên cứu thuỷ phân chọn lọc lập thể (RS)-1-(4-(2-amino-2-oxoethyl)phenoxy)-3-cloropropan-2-yl acetat bằng enzym lipase ứng dụng trong tổng hợp (S)-(−)-atenolol

The present study describes an efficient lipase-catalyzed enantioselective kinetic resolution of (RS)-1-(4-(2-amino-2-oxoethyl)phenoxy)-3-chloropropane-2-yl acetate. Various reaction parameters (lipase, (RS)-ester/lipase ratio, reaction time, reaction medium) were optimized in order to achieve good enantioselectivity.  The enantiopure (R)-ester acetate was obtained in 70% yield by using the lipase from Pseudomonas fluorescens with the  (RS)-ester/lipase ratio = 2,85/10 (w/w) in phosphate buffer pH 7.0 at 37 ^oC for 2.5 hours.  The (R)-enantiomer intermediate was then used for (S)-(−)-atenolol synthesis.

Keywords: (S)-(−)-atenolol, lipase, Pseudomonas fluorescens, atenolol, β-blocker.

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