CN118660878A - 用于制造大环肽的方法 - Google Patents

用于制造大环肽的方法 Download PDF

Info

Publication number
CN118660878A
CN118660878A CN202380019392.3A CN202380019392A CN118660878A CN 118660878 A CN118660878 A CN 118660878A CN 202380019392 A CN202380019392 A CN 202380019392A CN 118660878 A CN118660878 A CN 118660878A
Authority
CN
China
Prior art keywords
compound
formula
fmoc
boc
reaction mixture
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CN202380019392.3A
Other languages
English (en)
Chinese (zh)
Inventor
J-M·亚当
F·布利斯
P·J·C·多特
F·R·霍夫曼-埃默里
U·G·拉尔森
K·普恩特纳
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
F Hoffmann La Roche AG
Original Assignee
F Hoffmann La Roche AG
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Publication of CN118660878A publication Critical patent/CN118660878A/zh
Pending legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0815—Tripeptides with the first amino acid being basic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D209/20—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals substituted additionally by nitrogen atoms, e.g. tryptophane
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D209/26—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with an acyl radical attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/107—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides
    • C07K1/1072—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides by covalent attachment of residues or functional groups
    • C07K1/1077—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides by covalent attachment of residues or functional groups by covalent attachment of residues other than amino acids or peptide residues, e.g. sugars, polyols, fatty acids
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Medicinal Chemistry (AREA)
  • Analytical Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
CN202380019392.3A 2022-02-14 2023-02-13 用于制造大环肽的方法 Pending CN118660878A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP22156480.0 2022-02-14
EP22156480 2022-02-14
PCT/EP2023/053409 WO2023152347A1 (en) 2022-02-14 2023-02-13 Process for manufacturing macrocyclic peptides

Publications (1)

Publication Number Publication Date
CN118660878A true CN118660878A (zh) 2024-09-17

Family

ID=80683163

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202380019392.3A Pending CN118660878A (zh) 2022-02-14 2023-02-13 用于制造大环肽的方法

Country Status (12)

Country Link
US (1) US20250109166A1 (https=)
EP (1) EP4479396A1 (https=)
JP (1) JP2025505521A (https=)
KR (1) KR20240144894A (https=)
CN (1) CN118660878A (https=)
AR (1) AR128501A1 (https=)
AU (1) AU2023217269A1 (https=)
CA (1) CA3237617A1 (https=)
IL (1) IL313664A (https=)
MX (1) MX2024009210A (https=)
TW (1) TW202342493A (https=)
WO (1) WO2023152347A1 (https=)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2026068674A1 (en) 2024-09-27 2026-04-02 F. Hoffmann-La Roche Ag Process for deprotection of aminoacid derivatives

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6136934B2 (ja) 2011-12-15 2017-05-31 味の素株式会社 Ｆｍｏｃ基の除去方法
US11819532B2 (en) 2018-04-23 2023-11-21 Hoffmann-La Roche Inc. Peptide macrocycles against Acinetobacter baumannii

Also Published As

Publication number Publication date
EP4479396A1 (en) 2024-12-25
TW202342493A (zh) 2023-11-01
CA3237617A1 (en) 2023-08-17
IL313664A (en) 2024-08-01
WO2023152347A1 (en) 2023-08-17
JP2025505521A (ja) 2025-02-28
AR128501A1 (es) 2024-05-15
MX2024009210A (es) 2024-08-06
US20250109166A1 (en) 2025-04-03
KR20240144894A (ko) 2024-10-04
AU2023217269A1 (en) 2024-05-16

Similar Documents

Publication Publication Date Title
KR101467598B1 (ko) Ｈｃｖ 프로테아제 억제제 중간체의 제조방법
CN1173872A (zh) 凝血酶抑制剂
JP2016539931A (ja) テトラペプチド化合物及びその製造方法
CN107810189B (zh) 用于制备氮芥衍生物的方法
CN118660878A (zh) 用于制造大环肽的方法
CN105408317A (zh) 用于生产Sovaprevir的方法
RU2499792C2 (ru) Усовершенствованный способ получения ингибитора дипептидилпептидазы-iv и промежуточного соединения
JP2002502378A (ja) グアニジル化試薬
CN113912670B (zh) 血管紧张素转化酶2抑制剂及应用、抗冠状病毒感染药物
CN114728923B (zh) 用于制备氧杂环丁烷-2-基甲胺的方法和中间体
CN110423265A (zh) 一种环肽类trf2抑制剂的制备方法和用途
HK40111281A (zh) 用於制造大环肽的方法
CA2186605A1 (en) Process for peptide segment condensation
WO2005007634A1 (en) 3-hydroxy-4-oxo-1,2,3-triazines and derivatives thereof for amide and ester bond formation
JP2007501250A (ja) ペプチジル複素環式ケトン誘導体および製造方法
AU770530B2 (en) Process for the production of N-protected azetidine-2-carboxylic acids (AzeOHs)
CN1162318A (zh) 新活性肽及其制备
US20040082759A1 (en) Process for preparing distamycin derivatives
HK40074616B (en) Process and intermediate for the preparation of oxetan-2-ylmethanamine
WO2025118133A1 (zh) 一种(s)-来那度胺-5-位衍生物及其合成方法和应用
BR112022008892B1 (pt) Processo e intermediário para a preparação de oxetan-2- ilmetanamina, composto e seu uso
EP1572661A1 (en) Crystalline form of quinapril hydrochloride and process for preparing the same
WO2019200114A1 (en) Methods for preparing substituted dihydroindene-4-carboxamide compounds
CA3057997A1 (en) Process for making arylomyin ring analogs
WO2019066578A1 (ko) 의약품 합성용 중간체 화합물의 제조 방법

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 40111281

Country of ref document: HK

SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination