KR870700607A - 메발로노락톤의 이미다졸 유도체를 제조하는 방법 - Google Patents

메발로노락톤의 이미다졸 유도체를 제조하는 방법

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KR870700607A
KR870700607A KR1019870700051A KR870700051A KR870700607A KR 870700607 A KR870700607 A KR 870700607A KR 1019870700051 A KR1019870700051 A KR 1019870700051A KR 870700051 A KR870700051 A KR 870700051A KR 870700607 A KR870700607 A KR 870700607A
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butyl
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제임스 리차드 웨어링
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산도즈 파마슈티칼스 코포레이션
예안 크래머
산도즈 리미티드
한즈 루돌프 하우즈
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    • BPERFORMING OPERATIONS; TRANSPORTING
    • B29WORKING OF PLASTICS; WORKING OF SUBSTANCES IN A PLASTIC STATE IN GENERAL
    • B29CSHAPING OR JOINING OF PLASTICS; SHAPING OF MATERIAL IN A PLASTIC STATE, NOT OTHERWISE PROVIDED FOR; AFTER-TREATMENT OF THE SHAPED PRODUCTS, e.g. REPAIRING
    • B29C48/00Extrusion moulding, i.e. expressing the moulding material through a die or nozzle which imparts the desired form; Apparatus therefor
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    • Y10T428/00Stock material or miscellaneous articles
    • Y10T428/29Coated or structually defined flake, particle, cell, strand, strand portion, rod, filament, macroscopic fiber or mass thereof
    • Y10T428/2913Rod, strand, filament or fiber
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    • YGENERAL 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
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    • Y10T428/29Coated or structually defined flake, particle, cell, strand, strand portion, rod, filament, macroscopic fiber or mass thereof
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    • YGENERAL 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
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    • Y10T428/00Stock material or miscellaneous articles
    • Y10T428/29Coated or structually defined flake, particle, cell, strand, strand portion, rod, filament, macroscopic fiber or mass thereof
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Abstract

내용 없음

Description

메발로노락톤의 이미다졸 유도체를 제조하는 방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (4)

  1. a) X가 -(CH2)m- 또는 (E)-CH=CH-이고, R17은 어느 것이거나 R18이며, Z가 일반식(a)의 그룹이고, 여기에서 R13은 수소이며, R14가 R16(이는 C1-3알킬, n-부틸, i-부틸, t-부틸 또는 벤질이다)일 경우, 일반식(XVII)의 화합물을 환원시키거나, b) X가 -(CH2)m- 또는 (E)-CH=CH-이고, Z가 일반식(a)의 그룹이며, 여기에서 R13은 R13a이고, R17은 각각 독립적으로 R18또는 M2 일 경우, 일반식 (IXa)의 화합물을 가수분해시키거나, c) R17이 R18이고, R13이 수소이며, X가 -CH=CH- 또는 -CH2-CH=CH-이고, Z가 4R, 6S 배열을 나타내는 일반식(b)의 그룹이거나, X가 -CH2CH2- 또는 -CH2CH2CH2-이며, Z가 4R, 6R 배열을 나타내는 일반식(b)의 그룹일 경우, 일반식(Va)의 화합물을 탈실릴화시키거나, d) R17이 R18이고, X가 -CH2CH2-, -CH2CH2CH2-, -CH=CH-, -CH=CH-CH2- 또는 -CH2-CH=CH-이며, Z가 일반식(a)의 그룹(여기에서 R14는 R16이다)일 경우, 일반식(XI)의 화합물을 탈실릴화시키거나, e) Z가 일반식(c)의 그룹이고, 여기에서 Q가이며, R14가 R16이고 R17은 어느 것이거나 R18이며, X가 X7일 경우, Q가[즉, Z가 일반식(a)의 그룹이다]인 상응하는 일반식(I)의 화합물을 산화시키거나, f) Z가 에스테르 형태의 일반식(c)의 그룹이며, 여기에서 Q가이고, R17는 어느 것이거나 R18이며, X가 X7일 경우, Q가인 상응하는 일반식(I)의 화합물을 케탈화시키거나, g) 에스테르 또는 락톤 형태의 일반식(I)의 화합물을 가수분해시키거나, h) 유리산 형태의 일반식(I)의 화합물을 에스테르화 또는 락톤화 시키고, 유리카복실 그룹이 생성될 경우, 유리산 형태 또는 염의 형태로 수득된 화합물을 회수시킴을 특징으로 하여 일반식(I)의 화합물 또는 그의 약제학적으로 허용되는 산부가염을 제조하는 방법.
    상기 식에서, R1은 비대칭 탄소원자를 함유하지 않는 C1-6알킬, C3-7사이클로알킬, 아다만틸-1 또는(여기에서 R4, R5및 R6는 후술하는 바와 같다)이며, R2는 비대칭 탄소원자를 함유하지 않는 C1-6알킬, C3-7사이클로알킬, 아다만틸-1 또는(여기에서 R7, R8및 R9는 후술하는 바와 같다)이고, R3는 수소, 비대칭탄소 원자를 함유하지 않는 C1-6알킬, C3-7사이클로알킬, 아다만틸-1, 스티릴 또는(여기에서 R10, R11및 R12는 후술하는 바와 같다)이며, X는 -(CH2)m-, -CH-, -CH=CH-CH-CH2= 또는 -CH2-CH=CH-이고, 여기에서 m은 0, 1, 2 또는 3이며, Z는이고, 여기에서 Q는또는이며, 여기에서 R15는 각각 비대칭 탄소원자를 함유하지 않는 1급 또는 2급 C1-6알킬이고, 두 R15는 동일하거나, 두 R15는 함께 -(CH2)q-(여기에서 q는 2 또는 3이다)이며, R13는 수소 또는 C1-3알킬이고, R14는 수소, R16(이는 생리학적으로 허용되는 에스테르 그룹이다) 또는 M(이는 양이온이다)이며; 단, Z는 (i) X가 -CH=CH- 또는 -CH2-CH=CH-이거나, (ii) R13가 C1-3알킬이거나 (iii) (i) 및 (ii)일 경우에만은 일반식(c)의 그룹이어야 하고; R4, R7및 R10은 각각 독립적으로 수소, C1-3알킬, n-부틸, i-부틸, t-부틸, C1-3알콕시, n-부톡시, i-부톡시, 트리플루오로메틸, 플루오로, 클로로, 브로모, 페닐, 페녹시 또는 벤질옥시이며, R5, R8및 R11은 각각 독립적으로 수소, C1-3알킬, C1-3알콕시, 트리플루오로메틸, 플루오로, 클로로, 브로모, -COOR17, -N(R19)2, 페녹시 또는 벤질옥시이고, 여기에서 R17은 수소, R18(이는 C1-3알킬, n-부틸, i-부틸, t-부틸 또는 벤질이다) 또는 M(M은 상기 정의한 바와 같다)이며, R19은 각각 독립적으로 비대칭 탄소원자를 함유하지 않는 C1-6알킬이고, R6, R9및 R12은 각각 독립적으로 수소, C1-2알킬, C1-2알콕시, 플루오로 또는 클로로이며; 단, 환 A, B 및 C의 각각에 있어서 하나 이하의 치환체가 독립적으로 트리플루오로메틸, 페녹시 및 벤질옥시이어야 하고, X8은 (i) -CH=CH- 또는 CH2CH=CH-이거나 (ii) -CH2CH2- 또는 -CH2CH2CH2-이며, X9은 (i) -CH2CH2- 또는 -CH2CH2CH2-이거나, (ii) -CH=CH-, -CH=CH-CH2- 또는 -CH2-CH=CH-이고, ImA는 R17이 각각 독립적으로 R18일 경우 일반식의 그룹(여기에서 R1, R2및 R3는 상기 정의한 바와 같다)이며, R'16는 C1-3알킬, n-부틸, i-부틸, t-부틸 또는 벤질이고, R13a는 C1-3알킬이며, M2 는 나트륨 또는 칼륨이고, R22는 C1-3알킬이며; 단, (1) Z가일 경우에, 화합물은 유리염기 형태이며, (i) R14가 R16이고, R17이 각각 독립적으로 R18이거나, (ii) R14가 M이며 R17이 각각 독립적으로 R18또는 M이고, (2) (i) R14또는 하나이상의 R17이 M이거나, (ii) R14및 하나 이상의 R17이 M일 경우, 화합물은 유리산 형태이어야 한다.
  2. 제1항에 있어서, M이 각각 독립적으로 약제학적으로 허용되는 양이온인 방법.
  3. 제2항에 있어서, a) R1이 비대칭 탄소원자를 함유하지 않는 C1-6알킬, C3-7사이클로알킬 또는 아다민틸-1이고, R2인 화합물, b) Z가a)의 화합물, c) R1이 비대칭 탄소원자를 함유하지 않는 C1-6알킬이며, R3가 비대칭 탄소원자를 함유하지 않는 C1-6알킬, 사이클로헥실 또는이고, R7이 수소, C1-3알킬, 플루오로, 클로로 또는 브로모이며, R8이 수소, C1-2알킬, 플루오로 또는 클로로이고, R9이 수소, 또는 메틸이며, R13이 수소 또는 메틸이고, R14이 수소, C1-3알킬, n-부틸, i-부틸, t-부틸, 벤질 또는 M이며, X가 -CH2CH2- 또는 -CH=CH-인 b)의 화합물, d) R1이 C1-3알킬, n-부틸 또는 i-부틸이고, R3이며, R13가 수소이고, R14가 수소, C1-3알킬 또는 M이며, X가 (E)-CH=CH-인 c)의 화합물, e) R10이 수소, C1-3알킬, C1-2알콕시, 트리플루오로메틸, 플루오로, 클로로, 브로모 또는 페닐이고, R11이 수소, C1-2알킬, 플루오로, 클로로, 브로모, -COOR'17(여기에서 R'17는 수소, C1-3알킬 또는 M이다) 또는 -N(R'19)2(여기에서 R'19는 각각 독립적으로 C1-2알킬이다)이며, R12는 수소 또는 메틸이고, R14는 수소, C1-2알킬 또는 M인 d)의 화합물, f) R1이 C1-3알킬이고, R7이 수소, 메틸 또는 플루오로이며, R8이 수소 또는 메틸이고, R10이 수소, 메틸 또는 플루오로이며, R11이 수소 또는 메틸인 일반식 e)의 화합물,
    g) R9이 수소이고, R12가 수소인 f)의 화합물, h) R14가 약제학적으로 허용되는 양이온인 g)의 화합물, i) 일반식의 그룹의 3- 및 5-위치에 있는 하이드록시 그룹이 에리트로 배열을 나타내는 h)의 화합물, j) Z가인 a)의 화합물,k) Z가인 a)의 화합물, l) R1이 이고, R2가 비대칭 탄소원자를 함유하지 않는 C1-6알킬, C3-7사이클로알킬 또는 아다만틸-1인 화합물, m) Z가인 l)의 화합물, n) R1이고, R2인 화합물, o) R1이 비대칭 탄소원자를 함유하지 않는 C1-6알킬 C3-7사이클로 알킬 또는 아다만틸-1이고, R2가 비대칭 탄소원자를 함유하지 않는 C1-6알킬, C3-7사이클로 알킬 또는 아다만틸-1인 화합물로 이루어진 그룹중에서 선택되는 화합물을 제조하는 방법.
  4. 제1항에 있어서, 다음 a) 내지 l)로 이루어진 그룹중에서 선택되는 화합물을 제조하는 방법.
    상기 식에서 M은 약제학적으로 허용되는 양이온이다.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019870700051A 1985-05-22 1986-05-16 메발로노락톡의 이미다졸 유도체를 제조하는 방법 KR910003428B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US06/736,679 US4668794A (en) 1985-05-22 1985-05-22 Intermediate imidazole acrolein analogs
US736679 1985-05-22
PCT/EP1986/000297 WO1986007054A1 (en) 1985-05-22 1986-05-16 Imidazole analogs of mevalonolactone and derivatives thereof

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IL78858A (en) 1991-03-10
PT82623A (en) 1986-06-01
EP0235164A1 (en) 1987-09-09
DK33287D0 (da) 1987-01-21
KR910003428B1 (ko) 1991-05-31
PL149929B1 (en) 1990-04-30
FI865162A0 (fi) 1986-12-17
PT82623B (pt) 1988-08-17
GR861319B (en) 1986-09-19
PH25768A (en) 1991-10-18
NZ216234A (en) 1990-01-29
JPS62502894A (ja) 1987-11-19
DE3673003D1 (de) 1990-08-30
ES555199A0 (es) 1987-07-16
ES8707191A1 (es) 1987-07-16
FI865162A (fi) 1986-12-17
AU594064B2 (en) 1990-03-01
EP0235164B1 (en) 1990-07-25
WO1986007054A1 (en) 1986-12-04
HUT41743A (en) 1987-05-28
IL78858A0 (en) 1986-09-30
US4668794A (en) 1987-05-26
DK33287A (da) 1987-01-21
AU5960686A (en) 1986-12-24
ZA863840B (en) 1987-12-30

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