Pyridoxal hydrochloride → Lhrh

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The synthesis of peptide Ac-D-Nal(2)-D-Phe(4 Cl)-D-Trp-Ser-Arg-D-Lys[(Cu++)(POL)2 (DL-A2 pr)]-Leu-Arg-Pro-D-Ala-NH2 was performed by reacting [Ac-D-Nal(2)1, D-Phe(4Cl)2, D-Trp3, Arg5,D-Lys(DL-A2 pr)6, D-Ala10 ]LHRH (Preparation VIII, 40 mg of a TFA salt) in DMF (0.2 ml) at pH 8 (adjusted with sodium hydroxide and sodium acetate) with pyridoxal hydrochloride (Aldrich, 4 mg) then, after standing at room temperature for 1 hour, with copper(II) acetate (3 mg in 0.05 ml water). The crude product was purified by HPLC under conditions given in Example XI (system iv) to yield [Ac-D-Nal(2)1,D-Phe(4Cl)2,D-Trp3,Arg5,D-Lys[(Cu++)(POL)2 (DL-A2 pr)]6,D-Ala10 ]LHRH (40 mg) with HPLC retention time of 6.3 min.

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