200616-18-8Relevant academic research and scientific papers
Synthetic method of cyclic dipeptide containing aspartic acid and glutamic acid
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Paragraph 0009; 0065; 0067; 0068, (2021/07/08)
The invention discloses a synthetic method of cyclic dipeptide containing aspartic acid and glutamic acid, which comprises the following steps: by taking Fmoc-Asp (OtBu)-OH or Fmoc-Glu (OtBu)-OH as a raw material, reacting with 9-fluorene methanol to obtain fluorene methyl ester of fully protected amino acid, and then removing side chain tert-butoxy to obtain protected amino acid Fmoc-Asp-OFm or Fmoc-Glu-OFm; 2-CTC Resin resin is used as a carrier to be bonded with Fmoc-Asp-OFm or Fmoc-Glu-OFm side chain gamma-carboxyl, solid-phase cyclization is carried out to synthesize full-protection cyclic dipeptide, and the cyclic dipeptide with aspartic acid or glutamic acid at the carbon end is obtained through cutting and cracking. According to the method, 9-fluorene methanol is introduced to protect carboxyl, the carboxyl can be smoothly removed in the solid-phase synthesis process of the dipeptide, the whole process is easy to operate, the solid-phase cyclization efficiency is high, the purity is high, and the method can be suitable for batch synthesis of cyclic dipeptide with aspartic acid or glutamic acid at the carbon end.
