KR870007200A - Process for preparing peptidyl aminodiol - Google Patents

Process for preparing peptidyl aminodiol Download PDF

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Publication number
KR870007200A
KR870007200A KR1019860004143A KR860004143A KR870007200A KR 870007200 A KR870007200 A KR 870007200A KR 1019860004143 A KR1019860004143 A KR 1019860004143A KR 860004143 A KR860004143 A KR 860004143A KR 870007200 A KR870007200 A KR 870007200A
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South Korea
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hydrogen
methyl
lower alkyl
compound
benzyl
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KR1019860004143A
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Korean (ko)
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KR910000405B1 (en
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리차드 룰리 제이
하워드 로젠버그 소울
제이콥 플래트너 존
케이엘 풍 안토니
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애보트 래보러토리스
조셉 엠·버니크
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Priority claimed from US06/818,714 external-priority patent/US4680284A/en
Application filed by 애보트 래보러토리스, 조셉 엠·버니크 filed Critical 애보트 래보러토리스
Publication of KR870007200A publication Critical patent/KR870007200A/en
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Publication of KR910000405B1 publication Critical patent/KR910000405B1/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • General Health & Medical Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

내용 없음No content

Description

펩티딜 아미노디올의 제조방법Process for preparing peptidyl aminodiol

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음Since this is an open matter, no full text was included.

Claims (11)

하기 일반식의 펩티딜 아미노디올 및 약제학적으로 무독한 이의 염.Peptidyl aminodiol of the general formula and pharmaceutically toxic salts thereof. 상기식에서,In the above formula, R10 R 10 is 이며And A는 수소 또는 N-보호기이고,A is hydrogen or an N-protecting group, W는 0 또는 1이며,W is 0 or 1, B는 수소, 히드록시, NH, N-알킬, 저급알킬 또는 아릴알킬이고, 단, W가 1인경우, B는 NH이며,B is hydrogen, hydroxy, NH, N-alkyl, lower alkyl or arylalkyl, provided that when W is 1, B is NH, W가 0인 경우, B는 수소, 히드록시, 저급 알킬 또는 아릴알킬이고,When W is 0, B is hydrogen, hydroxy, lower alkyl or arylalkyl, R1은 저급알킬이거나, 친지방성 또는 방향족 또는 친수성 아미노산 측쇄이며,R 1 is lower alkyl, lipophilic or aromatic or hydrophilic amino acid side chain, m은 1내지 3이고,m is 1 to 3, n은 1내지 3이며,n is 1 to 3, p는 1내지 3이고,p is 1 to 3, q는 1내지 3이며,q is 1 to 3, s는 1내지 3이고,s is 1 to 3, t는 0내지 2이며,t is 0 to 2, R2는 수소 또는 저급 알킬이고,R 2 is hydrogen or lower alkyl, R3및 R4는 서로 무관하게 저급 알킬이거나 친지방성 또는 방향족 아미노산 측쇄이며,R 3 and R 4 , independently of one another, are lower alkyl or lipophilic or aromatic amino acid side chains, R5및 R7은 서로 무관하게 수소 또는 저급알킬이고,R 5 and R 7 are independently of each other hydrogen or lower alkyl, R6는 수소, 저급 알킬, 비닐, 아릴알킬 또는R 6 is hydrogen, lower alkyl, vinyl, arylalkyl or 이며, Is, R8은 수소 또는 저급 알킬이고,R 8 is hydrogen or lower alkyl, X는 산소, NH 또는 황이며,X is oxygen, NH or sulfur, R9는 수소, 저급 알킬 또는 알카노일이거나, XR9는 함께 저급알킬 술포닐, N3또는 Cl일 수 있다.R 9 may be hydrogen, lower alkyl or alkanoyl, or XR 9 together may be lower alkyl sulfonyl, N 3 or Cl. 제1항에 있어서, R10이며, R7은 수소이고, R6인 화합물.The compound of claim 1, wherein R 10 is R 7 is hydrogen and R 6 is Phosphorus compounds. 제2항에 있어서, W가 1이고, B는 NH이며, R1은 벤질, 4-메톡시벤질 또는 이소부틸이고, R2는 수소이며, R3은 저급알킬, (4-이미다졸)메틸 또는 (3-피라졸일)메틸이고, R4는 저급알킬 또는 시클로알킬메틸이며, R5가 수소인 화합물.The compound of claim 2, wherein W is 1, B is NH, R 1 is benzyl, 4-methoxybenzyl or isobutyl, R 2 is hydrogen, R 3 is lower alkyl, (4-imidazole) methyl Or (3-pyrazolyl) methyl, R 4 is loweralkyl or cycloalkylmethyl, and R 5 is hydrogen. 제1항에 있어서, R10이며, R6은 수소, 저급 알킬, 비닐 또는 아릴알킬인 화합물.The compound of claim 1, wherein R 10 is And R 6 is hydrogen, lower alkyl, vinyl or arylalkyl. 제4항에 있어서, A가 t-부틸옥시카보닐. t-부틸아세틸 또는 에톡시카보닐이며, W는 1이고, B는 NH이며, R1은 벤질, 시클로헥실메틸, (4-메톡시)벤질 ; (1-나프틸)메틸 또는 이소부틸이고, R2는 수소 또는 메틸이며, R3는 메틸, (4-이미다졸일)메틸, 벤질, (3-피라졸일)메틸, (메틸 메캅토)메틸 또는 이소부틸이고, R4는 이소부틸 또는 시클로헥실메틸이며, R5는 수소 또는 이소펜틸이며, R6는 수소, 저급 알킬, 비닐 또는 벤질이고, R7이 수소 또는 에틸인 화합물.The method of claim 4, wherein A is t-butyloxycarbonyl. t-butylacetyl or ethoxycarbonyl, W is 1, B is NH, R 1 is benzyl, cyclohexylmethyl, (4-methoxy) benzyl; (1-naphthyl) methyl or isobutyl, R 2 is hydrogen or methyl, R 3 is methyl, (4-imidazolyl) methyl, benzyl, (3-pyrazolyl) methyl, (methyl mecapto) methyl Or isobutyl, R 4 is isobutyl or cyclohexylmethyl, R 5 is hydrogen or isopentyl, R 6 is hydrogen, lower alkyl, vinyl or benzyl, and R 7 is hydrogen or ethyl. 제5항에 있어서, A가 에톡시카보닐이고, R1은(4-메톡시)벤질이며, R2는 수소이고, R3은(4-이미다졸일)메틸이며, R4는 시클로헥실메틸이고, R5및 R7은 수소이며, R6이 이부틸인 화합물.The compound of claim 5, wherein A is ethoxycarbonyl, R 1 is (4-methoxy) benzyl, R 2 is hydrogen, R 3 is (4-imidazolyl) methyl, and R 4 is cyclohexyl Methyl, R 5 and R 7 are hydrogen, and R 6 is ibutyl. 제5항에 있어서, A가 에톡시카보닐이며, R1은 벤질이고, R2,R5및 R7은 수소이며, R3는 (4-이미다졸일)메틸이고, R4는 시클로헥실메틸이며, R6이 이소부틸인 화합물.The compound of claim 5, wherein A is ethoxycarbonyl, R 1 is benzyl, R 2 , R 5 and R 7 are hydrogen, R 3 is (4-imidazolyl) methyl, and R 4 is cyclohexyl Methyl and R 6 is isobutyl. 제5항에 있어서, A가 에톡시카보닐이며, R1은 벤질이고, R2, R5및 R7은 수소이며, R3및 R6은 이소부틸이고, R4가 시콜로헥실메틸인 화합물.6. A compound according to claim 5, wherein A is ethoxycarbonyl, R 1 is benzyl, R 2 , R 5 and R 7 are hydrogen, R 3 and R 6 are isobutyl and R 4 is cyclohexylmethyl compound. 제1항에 있어서, R10The compound of claim 1, wherein R 10 is 이며, R4는 시클로헥실메틸이고, R5및 R7은 수소이며, R6가 저급 알킬인 화합물.R 4 is cyclohexylmethyl, R 5 and R 7 are hydrogen, and R 6 is lower alkyl. 제9항에 있어서, R10 The compound of claim 9, wherein R 10 is 이며, A는 에톡시카보닐이고, n은 1이며 m이 2인 화합물.And A is ethoxycarbonyl, n is 1 and m is 2. 제9항에 있어서, R10 The compound of claim 9, wherein R 10 is 이며, A는 수소이고, R1이 메틸인 화합물.And A is hydrogen and R 1 is methyl. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019860004143A 1986-01-16 1986-05-27 Peptidyl aminodiol KR910000405B1 (en)

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
US81873486A 1986-01-16 1986-01-16
US81871586A 1986-01-16 1986-01-16
US818734 1986-01-16
US818714~5 1986-01-16
US817,715 1986-01-16
US818,734 1986-01-16
US06/818,714 US4680284A (en) 1985-01-23 1986-01-16 Modified phenylalanine peptidylaminodiols
US819,714 1986-01-16

Publications (2)

Publication Number Publication Date
KR870007200A true KR870007200A (en) 1987-08-17
KR910000405B1 KR910000405B1 (en) 1991-01-25

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KR1019860004143A KR910000405B1 (en) 1986-01-16 1986-05-27 Peptidyl aminodiol

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KR (1) KR910000405B1 (en)
GR (1) GR860286B (en)

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GR860286B (en) 1986-06-02
KR910000405B1 (en) 1991-01-25

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