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Industrializable Synthesis of Fmoc-Ala-Thr-OH Pseudodipeptide as a Key Intermediate of Peptide Drugs.

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Title: Industrializable Synthesis of Fmoc-Ala-Thr-OH Pseudodipeptide as a Key Intermediate of Peptide Drugs.
Authors: Li, Xi-An1,2 (AUTHOR) lxa_1981@163.com, Yue, Li-rong1 (AUTHOR), Xu, Jiao1 (AUTHOR), Liang, Xiao-feng2 (AUTHOR), Zhou, Meng-jiao2 (AUTHOR), Hu, Dong-yan1 (AUTHOR), Ren, Hua-zhong1 (AUTHOR), Feng, Jia-fu1 (AUTHOR), Han, Guang-tian1 (AUTHOR)
Source: Synthesis. Aug2025, Vol. 57 Issue 16, p2486-2489. 4p.
Subjects: Peptide drugs, Recrystallization (Chemistry), Peptidomimetics, Product quality, Chemical purification, Biosynthesis, Cost control
Abstract: A new process for industrially synthesizing Fmoc-Ala-Thr-OH pseudodipeptide, which is a key intermediate for the synthesis of peptide drugs, is presented in four steps in overall 46% yield from Fmoc-L-Ala-OH. The process did not use column chromatography, and the characteristic of dipeptide salting with some organic base was cleverly utilized for purification. The suitable organic base for forming salt with the dipeptide was found after screening, and finally the synthesis was completed by recrystallization. The whole synthesis process is beneficial to industrial production and cost control. The purity of the product was over 99%. [ABSTRACT FROM AUTHOR]
Copyright of Synthesis is the property of Georg Thieme Verlag Stuttgart and its content may not be copied or emailed to multiple sites without the copyright holder's express written permission. Additionally, content may not be used with any artificial intelligence tools or machine learning technologies. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)
Database: Engineering Source
FullText Text:
  Availability: 0
Header DbId: egs
DbLabel: Engineering Source
An: 187006236
AccessLevel: 6
PubType: Academic Journal
PubTypeId: academicJournal
PreciseRelevancyScore: 0
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  Label: Title
  Group: Ti
  Data: Industrializable Synthesis of Fmoc-Ala-Thr-OH Pseudodipeptide as a Key Intermediate of Peptide Drugs.
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  Data: <searchLink fieldCode="AR" term="%22Li%2C+Xi-An%22">Li, Xi-An</searchLink><relatesTo>1,2</relatesTo> (AUTHOR)<i> lxa_1981@163.com</i><br /><searchLink fieldCode="AR" term="%22Yue%2C+Li-rong%22">Yue, Li-rong</searchLink><relatesTo>1</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Xu%2C+Jiao%22">Xu, Jiao</searchLink><relatesTo>1</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Liang%2C+Xiao-feng%22">Liang, Xiao-feng</searchLink><relatesTo>2</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Zhou%2C+Meng-jiao%22">Zhou, Meng-jiao</searchLink><relatesTo>2</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Hu%2C+Dong-yan%22">Hu, Dong-yan</searchLink><relatesTo>1</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Ren%2C+Hua-zhong%22">Ren, Hua-zhong</searchLink><relatesTo>1</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Feng%2C+Jia-fu%22">Feng, Jia-fu</searchLink><relatesTo>1</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Han%2C+Guang-tian%22">Han, Guang-tian</searchLink><relatesTo>1</relatesTo> (AUTHOR)
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  Data: <searchLink fieldCode="JN" term="%22Synthesis%22">Synthesis</searchLink>. Aug2025, Vol. 57 Issue 16, p2486-2489. 4p.
– Name: Subject
  Label: Subjects
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  Data: <searchLink fieldCode="DE" term="%22Peptide+drugs%22">Peptide drugs</searchLink><br /><searchLink fieldCode="DE" term="%22Recrystallization+%28Chemistry%29%22">Recrystallization (Chemistry)</searchLink><br /><searchLink fieldCode="DE" term="%22Peptidomimetics%22">Peptidomimetics</searchLink><br /><searchLink fieldCode="DE" term="%22Product+quality%22">Product quality</searchLink><br /><searchLink fieldCode="DE" term="%22Chemical+purification%22">Chemical purification</searchLink><br /><searchLink fieldCode="DE" term="%22Biosynthesis%22">Biosynthesis</searchLink><br /><searchLink fieldCode="DE" term="%22Cost+control%22">Cost control</searchLink>
– Name: Abstract
  Label: Abstract
  Group: Ab
  Data: A new process for industrially synthesizing Fmoc-Ala-Thr-OH pseudodipeptide, which is a key intermediate for the synthesis of peptide drugs, is presented in four steps in overall 46% yield from Fmoc-L-Ala-OH. The process did not use column chromatography, and the characteristic of dipeptide salting with some organic base was cleverly utilized for purification. The suitable organic base for forming salt with the dipeptide was found after screening, and finally the synthesis was completed by recrystallization. The whole synthesis process is beneficial to industrial production and cost control. The purity of the product was over 99%. [ABSTRACT FROM AUTHOR]
– Name: AbstractSuppliedCopyright
  Label:
  Group: Ab
  Data: <i>Copyright of Synthesis is the property of Georg Thieme Verlag Stuttgart and its content may not be copied or emailed to multiple sites without the copyright holder's express written permission. Additionally, content may not be used with any artificial intelligence tools or machine learning technologies. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract.</i> (Copyright applies to all Abstracts.)
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RecordInfo BibRecord:
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      – Type: doi
        Value: 10.1055/a-2602-4547
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      – Code: eng
        Text: English
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      Pagination:
        PageCount: 4
        StartPage: 2486
    Subjects:
      – SubjectFull: Peptide drugs
        Type: general
      – SubjectFull: Recrystallization (Chemistry)
        Type: general
      – SubjectFull: Peptidomimetics
        Type: general
      – SubjectFull: Product quality
        Type: general
      – SubjectFull: Chemical purification
        Type: general
      – SubjectFull: Biosynthesis
        Type: general
      – SubjectFull: Cost control
        Type: general
    Titles:
      – TitleFull: Industrializable Synthesis of Fmoc-Ala-Thr-OH Pseudodipeptide as a Key Intermediate of Peptide Drugs.
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            NameFull: Li, Xi-An
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            NameFull: Yue, Li-rong
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            NameFull: Xu, Jiao
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            – D: 15
              M: 08
              Text: Aug2025
              Type: published
              Y: 2025
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              Value: 57
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