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A PROCESS FOR PRODUCTION OF THE SOMATOSTATIN ANALOG, OCTREOTIDE
A PROCESS FOR PRODUCTION OF THE SOMATOSTATIN ANALOG, OCTREOTIDE
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机译:一种生长抑素类似物奥曲肽的生产方法
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摘要
The present invention relates to a process for commercial production of octreotide using solution peptide chemistry and inexpensive amino acid derivatives. Thus the hexapeptide (Boc) D-Phe-Cys(Acm)-Phe-D-Trp-Lys(Boc)-Thr-OMe is synthesised by condensation of two tripeptide fragments, saponified and condensed with Cys(Acm)-Thr-OL to give the linear octapeptide alcohol. The linear peptide alcohol is trated with iodine, after removal of Boc groups, to give the cyclic peptide octreotide. The linear octapeptide alcohol can alternately be made by condensation of the protected hexapeptide acid with the dipeptide Cys(Acm)-Thr-OMe, followed by reduction with borohydride.
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