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| - Application of in Situ Silylation for Improved,Convenient Preparation ofFluorenylmethoxycarbonyl (Fmoc)-ProtectedPhosphinate Amino Acids
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| - A convenient and efficient method has been developed forthe preparation of 9-fluorenylmethoxycarbonyl (Fmoc)-protected 1-aminoalkylphosphinic acids. Reproducible procedures for the synthesis and purification of free α-aminoH-phosphinates are provided. Protection of free aminophosphinates as the N-Fmoc derivative was achieved by insitu trimethylsilylation of aminoalkylphosphinic acids, whichthen reacted with Fmoc-Cl to provide corresponding productsin excellent yields and in high purity after simple extractiveisolation. Mechanistic aspects of the silylation are discussed,and the application of the procedure to another class of aminophosphorus acids is presented.
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