Method for the production of phenylalanine derivatives
View Patent ↗The invention relates to an improved method for the production of 3-amidinophenylalanine derivatives, especially triisopropylphenyl-sulfonyl-substituted 3-amidinophenylalanine derivatives.
1. A method for the production of 3-amidinophenplalanine derivatives, comprising:
reaction of a N-protected 3-cyanophenylalanine with a piperazine derivative to form an N-protected 3-cyanophenylalanine piperazide and subsequent reaction thereof with an optionally substituted phenylsulfonyl halide.
2. The method as claimed in claim 1 wherein the optionally substituted phenylsulfonyl halide is a TIPPS halide.
3. The method as claimed in claim 2 , wherein the TIPPS halide is TIPPS-Cl.
4. The method as claimed in claim 1 wherein N-ethoxycarbonylpiperazine is used as piperazine derivative.
5. The method as claimed in claim 1 , wherein N -(2,4,6-triisopropylphenylsulfonyl)-3-amidino-(D,L)-phenyl-alanine 4-ethoxycarbonylpiperazide or the L enantiomers thereof are prepared.