677021-08-8Relevant articles and documents
Synthetic method of cyclic dipeptide containing cysteine
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Paragraph 0073-0086, (2021/06/26)
The invention discloses a synthetic method of cyclic dipeptide containing cysteine, the synthetic method comprises the following steps: taking Teoc-L-Cys-OFm as a raw material, connecting a solid-phase carrier 2-CTC Resin resin with a side chain sulfydryl, removing a Teoc protecting group by using tetrabutylammonium fluoride, taking Fmoc-L-A (X)-OH (A to represent alpha-amino acid, wherein X represents a side chain protecting group of the alpha-amino acid, when the alpha-amino acid has no side chain protecting group, X is equivalent to H atom) is the second connected amino acid, after connection is completed, removing Fmoc and Fm protecting groups by piperidine/DMF to enable carboxyl and carboxyl to be exposed, finally, enabling the amino and carboxyl exposed on the resin to perform self-cyclization by the DMF solution of HBTU/DIEA to form cyclic dipeptide to be hung on the resin, and cutting the resin to enable the cyclic dipeptide to fall off, and precipitating in diethyl ether to generate various cyclic dipeptides. The method disclosed by the invention has the advantages of large-scale operation, simple synthesis process, safety in operation, easiness in purification, capability of avoiding cysteine polymerization and capability of integrally synthesizing the cyclic dipeptide containing cysteine in batches.
