H De Pury

K Rose

R E Offord

Reaction conditions are described that permit the enzyme-assisted semi-synthetic replacement of residue B30 of pig insulin (or of analogue) to proceed in very high yield in 2 h or less. Immobilized trypsin may be used as catalyst, and excess amino acid ester may be recycled after a simple extraction. Alanine-B30 may be replaced by a variety of nucleophiles, including threonine O-t-butyl ether t-butyl ester, in which case the yield of crude product is about 99%. De-protection of the B30 threonyl ester analogue of insulin thus formed then affords human insulin in an overall yield of about 92%, based on pig starting material. The product has full biological potency, as determined by depression of blood glucose concentration in rats, and showed the expected behaviour on radioimmunoassay.</jats:p

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Biochemical Journal

Rapid preparation of human insulin and insulin analogues in high yield by enzyme-assisted semi-synthesis

http://www.biochemj.org/content/ppbiochemj/211/3/671.full.pdf

Rapid preparation of human insulin and insulin analogues in high yield by enzyme-assisted semi-synthesis

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