Method for the production of amino terminus protected naturally

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

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548496, 548497, 548532, 562445, 562562, 562563, 562570, 562554, C07D20920, C07D23318, C07C 9900

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active

048228907

ABSTRACT:
A method for the production of substantially 100% pure N.alpha.-urethane protected amino acids is disclosed. This method eliminates the formation of di-peptide and tri-peptide contaminants. Reaction of blocking reagents at the carboxylate site on a protected peptide is prevented by the application of labile amino acid esters. Subsequent removal of the ester yields, in ultra-high purity, the N.alpha.-protected amino acid. The substantially 100% pure N.alpha.-urethane protected amino acid are also disclosed.

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Barlos et al, "Efficient `One-Pot` Synthesis of N-Trityl Amino Acids", J. Org. Chem., 1982, 47:1324-1326.
Bodansky, Y. Klausner and Mr. Ondetti "Peptide Synthesis", 2nd Ed., "Protection of Amino Acids", pp. 43 and 44.
Chang et al. "Preparation and Properties of N.alpha.-9-Fluoroenylmethyloxy Carbonylamino Acids Bearing Protein Tert.-Butyl Side Chain Protection"-Int. J. Peptide Prot. Res. 1980 15 59-66.
Merrifield et al. "9-(2-Sulfo)fluorenylmethyloxycarbonyl Chloride, A New Reagent for the Purification of a Synthetic Peptide", J. Org. Chem. 1978, 43:4808-4816.
Carpino et al. "The 9-Fluorenylmethoxycarbonyl Amino Protecting Group", J. Org. Chem. 1972, 37:3404-3409.
Theodropolos et al. J. Org. Chem., 47 p. 1324 et seq. (1982).

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