کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
70523 | 48835 | 2010 | 9 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Lipase resolution of new (±)-3-aryloxy-1-halogenopropan-2-ols: Versatile building blocks for β-adrenergic receptor antagonists
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
مهندسی شیمی
کاتالیزور
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چکیده انگلیسی
Using two commercial immobilized lipases Lipozyme® TL and Novozym® 435 effective kinetic resolution of several novel 3-aryloxy-1-halogenopropan-2-ols was achieved by acyl transfer reaction in organic solvents, yielding both enantiomers with 89–99% ee. In preparative resolutions carried out in tert-butyl methyl ether at 25 °C with vinyl acetate as acyl donor enantioselectivity ratio E was from 64 to 99. The resolved enantiomers were successfully used as chiral building blocks in the synthesis of new 1-alkylamino-3-aryloxypropan-2-ols, by nucleophilic halogen substitution with isopropylamine and tert-butylamine. The obtained products will be evaluated in vitro as potential new β-adrenergic receptors antagonists.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Molecular Catalysis B: Enzymatic - Volume 62, Issues 3–4, March 2010, Pages 248–256
Journal: Journal of Molecular Catalysis B: Enzymatic - Volume 62, Issues 3–4, March 2010, Pages 248–256
نویسندگان
Maciej Maciejewski, Krzysztof Półtorak, Janina E. Kamińska,