- One-pot synthesis of N-protected β-chiral amino alcohols
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N-tert-butyloxycarbonyl-S-benzyl-cysteine, N-fluorenylmethyloxycarbonyl-alanine-, S-trityl-cysteine-, O-tert-butyl-serine- and O-tertbutyl-tyrosine were converted to the corresponding alcohols via sodium borohydride reduction of their in situ formed methy
- Somlai, Csaba,Peter, Antal,Forgo, Peter,Penke, Botond
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- Method for preparing Fmoc-Tyr (tBu)-OH
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The invention relates to a method for preparing FmocTyr (tBu)-OH, and belongs to the technical field of medical intermediate chemical engineering. The technical problem to be solved by the invention is to provide a method for preparing Fmoc-Tyr (tBu)-OH with good safety. The method comprises the following steps: a, mixing an Fmoc-Tyr-OR solid, tert-butyl acetate, perchloric acid and tert-butyl alcohol to react, adjusting the pH value to 5-6, separating out a solid, filtering, washing and drying to obtain an Fmoc-Tyr (tBu)-OR solid, wherein R is a C1-C4 alkyl; and b, carrying out hydrolysis onthe Fmoc-Tyr (tBu)-OR solid to obtain an Fmoc-Tyr (tBu)-OH product. The method is improved on the basis of the existing synthetic route, isobutene is not added when tert-butyl is introduced, the operation is simple and controllable, the safety is good, the cost is low, the production steps can be effectively shortened, the production efficiency and the yield are improved, and the method is suitable for modern industrial production.
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