RO85073B - Procedeu pentru prepararea unor derivati de aminoacizi - Google Patents

Procedeu pentru prepararea unor derivati de aminoacizi

Info

Publication number
RO85073B
RO85073B RO108580A RO10858079A RO85073B RO 85073 B RO85073 B RO 85073B RO 108580 A RO108580 A RO 108580A RO 10858079 A RO10858079 A RO 10858079A RO 85073 B RO85073 B RO 85073B
Authority
RO
Romania
Prior art keywords
protecting group
formula
boc
give
preparation
Prior art date
Application number
RO108580A
Other languages
English (en)
Other versions
RO85073A (ro
Inventor
A. Arthur Patchett
E. Elbert Harris
J. Matthew Wyvratt
W. Edwuard Tristram
Original Assignee
Merck & Co. Inc.
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=25513965&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=RO85073(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck & Co. Inc. filed Critical Merck & Co. Inc.
Publication of RO85073A publication Critical patent/RO85073A/ro
Publication of RO85073B publication Critical patent/RO85073B/ro

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
    • C07K5/06—Dipeptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/022—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -X-C(=O)-(C)n-N-C-C(=O)-Y-; X and Y being heteroatoms; n being 1 or 2
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/022—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -X-C(=O)-(C)n-N-C-C(=O)-Y-; X and Y being heteroatoms; n being 1 or 2
    • C07K5/0222—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -X-C(=O)-(C)n-N-C-C(=O)-Y-; X and Y being heteroatoms; n being 1 or 2 with the first amino acid being heterocyclic, e.g. Pro, Trp
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • 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
    • Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10S530/00—Chemistry: natural resins or derivatives; peptides or proteins; lignins or reaction products thereof
    • Y10S530/80—Antihypertensive peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Indole Compounds (AREA)

Abstract

Inventia se refera la un procedeu pentru prepararea unui derivat cu formula generala I: (vezi formula) în care R este hidrogen sau etil, R2 este fenil sau clorfenil, caracterizat prin aceea ca, se prepara o solutie apoasa de dipeptida protejata cu formula II: (vezi formula) în care t-Boc este grupa de protectie t-butiloxicarbonil si un derivat de acid 2-oxo-4-fenil butiric cu formula generala III: (vezi formula) în care R1 si R2 au semnificatiile susmentionate, se corecteaza pH-ul solutiei la 7 cu hidroxid de sodiu, se condenseaza dipeptida protejata si acidul în prezenta cianbrohidrurii de sodiu, compusul condensat se absoarbe pe rasina schimbatoare de ioni puternic acida, astfel încît grupa protectoare t-Boc este scindata complet, se elueaza rasina schimbatoare de ioni cu solutie apoasa de amoniac 10%, obtinîndu-se un produs brut care se purifica prin filtrare prin gel si se trateaza produsul purificat cu acetat de etil în acid clorhidric gazos 4n, pentru a îndeparta restul de grupa protectoare t-Boc si a se obtine clorhidratul compusului cu formula I, care este cromatografiat pe rasina de polistiren, folosind acetonitril 3,5% în NH4OH.
RO108580A 1978-12-11 1979-12-08 Procedeu pentru prepararea unor derivati de aminoacizi RO85073B (ro)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US96824978A 1978-12-11 1978-12-11

Publications (2)

Publication Number Publication Date
RO85073A RO85073A (ro) 1984-09-24
RO85073B true RO85073B (ro) 1984-10-30

Family

ID=25513965

Family Applications (4)

Application Number Title Priority Date Filing Date
RO7999486A RO80264A (ro) 1978-12-11 1979-12-08 Procedeu pentru prepararea unui derivat de alanilprolina
RO108580A RO85073B (ro) 1978-12-11 1979-12-08 Procedeu pentru prepararea unor derivati de aminoacizi
RO108578A RO85071B (ro) 1978-12-11 1979-12-08 Procedeu pentru prepararea unui derivat de alanilprolina
RO108579A RO85072B (ro) 1978-12-11 1979-12-08 Procedeu pentru prepararea n-(1-carboxi-3-fenilpropil)-l-alanil-l-prolinei

Family Applications Before (1)

Application Number Title Priority Date Filing Date
RO7999486A RO80264A (ro) 1978-12-11 1979-12-08 Procedeu pentru prepararea unui derivat de alanilprolina

Family Applications After (2)

Application Number Title Priority Date Filing Date
RO108578A RO85071B (ro) 1978-12-11 1979-12-08 Procedeu pentru prepararea unui derivat de alanilprolina
RO108579A RO85072B (ro) 1978-12-11 1979-12-08 Procedeu pentru prepararea n-(1-carboxi-3-fenilpropil)-l-alanil-l-prolinei

Country Status (33)

Country Link
US (2) US4374829A (ro)
EP (1) EP0012401B1 (ro)
JP (3) JPS5581845A (ro)
KR (3) KR850000847B1 (ro)
AR (1) AR231971A1 (ro)
AU (1) AU530380B2 (ro)
BG (6) BG39467A3 (ro)
CA (4) CA1302005C (ro)
CS (1) CS237311B2 (ro)
DD (1) DD148770A5 (ro)
DE (2) DE19375005I2 (ro)
DK (1) DK165455C (ro)
EG (1) EG14182A (ro)
ES (2) ES8101540A1 (ro)
FI (1) FI68405C (ro)
GR (1) GR72251B (ro)
HK (1) HK27487A (ro)
HU (1) HU182902B (ro)
IE (1) IE48922B1 (ro)
IL (1) IL58849A (ro)
LU (1) LU90173I2 (ro)
MA (1) MA18664A1 (ro)
NL (4) NL930006I2 (ro)
NO (3) NO151622C (ro)
NZ (1) NZ192312A (ro)
PH (1) PH24268A (ro)
PL (2) PL126126B1 (ro)
PT (1) PT70542A (ro)
RO (4) RO80264A (ro)
SU (1) SU1287756A3 (ro)
YU (3) YU42655B (ro)
ZA (1) ZA796688B (ro)
ZW (1) ZW24479A1 (ro)

Families Citing this family (399)

* Cited by examiner, † Cited by third party
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