Process for the preparation of insulin derivatives
First Claim
1. A process for the preparation of an insulin derivative of the formula I ##STR4## in which R30 represents the radical of a neutral L-amino acid selected from the group consisting of Ala, Thr, and Ser,n=1, 2 or 3,X represents identical or different radicals of naturally occurring L-amino acids which can be genetically coded, at least one of which is a basic amino acid, and, where n is 2 or 3, the C-terminal member may also be homoserine-lactone,Y=Phe or Hby splitting of proinsulin intermediates, proinsulin, preproinsulin or analogs thereof, which comprises carrying out the splitting reaction at a pH in the range from 1 pH unit below the isoelectric point of each individual insulin derivative of the formula I to 1 pH unit above said isoelectric point in the presence of at least one phenol.
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Abstract
The invention relates to a process for the preparation of insulin derivatives of the formula I ##STR1## in which R30 represents the radical of a neutral L-amino acid which can be genetically coded, X represents identical or different radicals of L-amino acids which can be genetically coded, at least one of which is a basic amino acid, it being possible for the C-terminal member to be homoserine-lactone, Y denotes Phe or H and n denotes 1, 2 or 3, by splitting of intermediates, proinsulin, preproinsulin or analogs thereof, which comprises carrying out the splitting reaction close to the isoelectric point of the insulin derivatives of the formula I in the presence of an aromatic hydroxy compound.
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10 Claims
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1. A process for the preparation of an insulin derivative of the formula I ##STR4## in which R30 represents the radical of a neutral L-amino acid selected from the group consisting of Ala, Thr, and Ser,
n=1, 2 or 3, X represents identical or different radicals of naturally occurring L-amino acids which can be genetically coded, at least one of which is a basic amino acid, and, where n is 2 or 3, the C-terminal member may also be homoserine-lactone, Y=Phe or H by splitting of proinsulin intermediates, proinsulin, preproinsulin or analogs thereof, which comprises carrying out the splitting reaction at a pH in the range from 1 pH unit below the isoelectric point of each individual insulin derivative of the formula I to 1 pH unit above said isoelectric point in the presence of at least one phenol.
Specification