Method of removing n-formyl group

C - Chemistry – Metallurgy – 07 – K

Patent

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530/5.06

C07K 5/075 (2006.01)

Patent

CA 1187075

ABSTRACT OF THE DISCLOSURE A formyl protective group on the amino group of the aspartyl residue of an L-aspartyl-L-phenylalanine lower alkyl ester is removed efficiently and selectively with a strong acid at an elevated temperature in a very short time typically of the order of 15 seconds to 60 minutes, while the splitting of the ester bond or the peptide bond is suppressed, the process is particularly useful in the manufacture of ?-APM (?-L-aspartyl-L-phenylalanine methyl ester), a dipeptide sweetener.

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