Strong-acid mono-salts of alpha-N-formyl-lysine - prepd. by reacting a lysine mono-salt with acetic anhydride and formic acid

摘要

The mono-salts (I) of alpha-N-formyl-D-, L- or DL-lysine with strong acids are prepd. by reacting a strong-acid mono-salt of D-, L- or DL-lysine with formic acid and acetic anhydride; treating the resulting symmetric anhydride with H2O; and isolating (I). (I) are useful as alpha-N-protected inters. for the prepn. of SIGMA-N-substd. lysine derivs. e.g. biocytin, poly-SIGMA-lyine, lysine-aniline and SIGMA-N-salicyloyllysine. The process gives yields of =95%. The starting material is pref. the lysine hydrochloride. The acetic anhydride is pref. used in the stoichiometric amt., and the HCOOH is pref. used in excess (also cating as solvent.) The reaction is pref. effected at 5-50 degrees C (esp. 5-30 degrees C) and atmospheric press.