FIELD: chemistry.
SUBSTANCE: method involves reaction of trifluoroacetate (1S,2S,3R,5S)-pinanediol-(R)-1-ammonium-3-methylbutane-1-boronate with N-pyrazinoyl-L-phenylalanyl with ultrasonic activation using a suitable condensing agent in the presence of a suitable base. The formed (1S,2S,3R,5S)-pinanediol N-pyrazinoyl-L-phenylalanyl-L-leucine-boronate undergoes an exchange reaction with isobutyl boronic acid in an acidic medium to form N-pyrazinoyl-L-phenylalanyl-L-leucine boronic acid or anhydride thereof.
EFFECT: method enables to obtain an end product of higher purity and high output, and a more efficient and safer technique.
7 cl, 5 ex
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Authors
Dates
2012-05-10—Published
2010-10-26—Filed