Peptide(s) prepn. using proteolytic enzymes - carried out in the absence of solvents, using substance contg. water of crystallisation to provide necessary water

摘要

The prepn. of peptides by reacting amino-protected amino acid or peptide as the acylating components, with another amino acid or peptide as the amino component in the presence of a proteolytic enyzme comprises subjecting mixt. of the acylating component, the amino component and the protolytic enzyme in anhydrous condition to mechanical action and the mixt. contains substance that has water of crystallisation. Pref. the substance contg. water of crystallisation can be the acylating component, the amino component and/or the proteolytic enzyme, or a basic (in)organic substance added to the reaction mixt., esp. Na2CO3.IOH2O, Na2CO3.7H2O, Na2CO3.H2O, Na2HOP4.12H2O, NaHCO3, Na2CO3.NaHCO3.2H2O or MeCOONa.3H2O. The amino component is carboxy-protected, esp. as the amide or ester (esp. pref. t-butylester) and/or is in the form of its acid addn.-salt (esp. hydrochloride or hydrobromide. USE/ADVANTAGE - The process is carried out in the total absence of an inorganic or organic solvents and is thus economical and ecologically friendly. The use of toxic chemicals and solvents is fully excluded. The substrate contg. water of crystallisation can be any one of the 3 reactants or can be an additional substance. There is is no problem of racemisation in the peptide formation, unlike in conventional processes using solvents