Novel Process for Preparing Taltirelin and Its Intermediates
The present invention relates to a novel method for manufacturing taltirelin and an intermediate thereof. More specifically, the present invention discloses: a manufacturing method which uses a fluorenylmethoxycarbonyl (Fmoc)-trityl-histidine as a starting material, and manufactures taltirelin through a process of manufacturing histidyl-trityl-prolineamide, which is an intermediate of talthyreline by an in situ reaction, thereby being suitable for industrial mass production by manufacturing taltirelin in a high yield and high purity in a short time compared to existing technology; and a method for manufacturing histidyl-trityl-prolineamide for the same.
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Paragraph 0118-0126
(2020/09/30)
Novel Preparation for Taltirelin by Solid Phase Peptide Synthetic Method
PURPOSE: A novel method for preparing taltirelin by solid phase peptide synthesis is provided to quickly terminate compound synthesis and to obtain a final compound in high yield and purity. CONSTITUTION: A method for preparing taltirelin comprises: a step of preparing resin in which a Fmoc[9H-fluoren-9-ylmethoxycarbonyl]; protection group is removed; a step of coupling the Fmoc-proline with the resin; a step of removing the Fmoc protection group from the coupled proline; a step of coupling Fmoc-histidine to the proline; a step of removing the Fmoc protection group from the histidine; a step of coupling 1-methyl-4,5-dihydro orotic acid with the histidine; and a step of isolating peptides from the resin. The method further comprises a step of purifying the taltirelin; a step of converting the crystalline form of taltirelin into an alpha form; and a step of freeze-drying the taltirelin.
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Paragraph 0054-0075
(2016/10/07)
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