FIELD: chemistry.
SUBSTANCE: claimed is method of obtaining N-pyrazinoyl-(L)-phenylalanyl-(L)-leucine boronic acid or its anhydride with application of reaction of (1S,2S,3R,5S)-pinandiol-(S)-1-clor-3-methylbutane-I-boronate with lithium bis(trimethylsilyl)-amide with formation of (1S,2S,3R,5S)-pinandiol-(R)-1-bis(trimethylsilyl)amino-3-methylbutane-1-boronate, which is subjected to extractive purification with water and is isolated in pure form and with further interaction with trifluoroacetic acid with formation of corresponding acid-additive salt, which is condensed with N-pyrazinoil-(L)-phenylalanine in presence of condensing agent TBTU and diisopropylethylamine in methylene chloride, N-pyrazinoil-(L)-phenylalanine being obtained by condensation of N,O-bis-silyl derivative of (L)-phenylalanine, formed from (L)-phenylalanine under impact of N,O-bis(trimethylsilyl)acetamide, and imidazolyl of pyrazine carbonic acid, with formation of (1S,2S,3R,5S)- pinandiol-N-pyrazinoil-(L)-phenylalanyl-(L)-leucine boronate, which is subjected to acid hydrolysis with formation of N-pyrazinoyl-(L)-phenylalanyl-(L)-leucine boronic acid or its anhydride.
EFFECT: method allows top obtain target product with high output, high purity using simpler and safer technology.
8 ex
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