KR860009012A - 벤조티아진 디옥사이드 유도체의 제조방법 - Google Patents

벤조티아진 디옥사이드 유도체의 제조방법 Download PDF

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KR860009012A
KR860009012A KR1019860004181A KR860004181A KR860009012A KR 860009012 A KR860009012 A KR 860009012A KR 1019860004181 A KR1019860004181 A KR 1019860004181A KR 860004181 A KR860004181 A KR 860004181A KR 860009012 A KR860009012 A KR 860009012A
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methyl
ethyl
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amino
methylpyridinium
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죠지 롬바르디노 죠세프
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화이자 인코포레이티드
알렌 제이. 스피겔
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    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
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    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
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    • C07D213/16Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom containing only hydrogen and carbon atoms in addition to the ring nitrogen atom containing only one pyridine ring
    • C07D213/20Quaternary compounds thereof
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
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    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/155Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms 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 the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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Abstract

내용 없음

Description

벤조티아진 디옥사이드 유도체의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

  1. 일반식(Ⅱ)의 옥시캄 화합물을 일반식(Ⅲ) 또는 (Ⅲ')의 아실할라이드 화합물 또는 그의 하이드로클로라이드 산부가염과 반응시킴을 특징으로 하여 일반식(Ⅰ) 또는 (Ⅰ')의 화합물 또는 그의 약제학적으로 허용되는 산부가염을 제조하는 방법.
    상기식에서, R은 2-피리딜, 6-메틸-2-피리딜, 6-플루오로-2-피리딜, 6-클로로-2-피리딜, 5-메틸-3-이속사졸릴 또는 2-티아졸릴이고; Y는 각 알킬부위에 3개까지의 탄소원자를 갖는 N, N-디알킬아미노이거나, N-메틸-N-벤질아미노, N-에틸-N-벤질아미노, N-메틸-N-(β-페닐에틸)아미노 또는 N-에틸-N-(β-페닐에틸)아미노이거나, 또는 각각 사이클로알킬 부위에 6개까지의 탄소원자를 갖는 N-메틸-N-사이클로알킬아미노 또는 N-에틸-N-사이클로알킬아미노이거나, 또는 N-메틸-N-페닐아미노, N-에틸-N-페닐아미노, N-메틸-N-(p-클롤로페닐)아미노, N-에틸-N-(p-클롤로페닐)아미노, N-메틸-N-(N', N'-디메킬카바밀메틸)아미노, N-메틸-N-(N, N'-디메킬카바밀메틸)아미노,피롤리디노, 피페리디노, 2-메틸피페리미노, 2-에틸피레리미노, 호모페리디노, 1-아자-사이클로옥틸, N-메틸피페라지노, 모르폴리노 또는 티오모르폴리노이고; Z는 피리디늄, 2-메틸피리디늄, 3-메틸피리디늄,4-메틸피리디늄, 2,6디메틸피리디늄, 2,4,6-트리메틸피리디늄, 3-에틸피리디늄, 4-에틸피리디늄, 3-에틸-4-메틸피리디늄, 4-에틸-2-메틸피리디늄 또는 5-에틸-2-메틸피리디늄이고; A는 약리학적으로 혀용되는 음이온이고; X는 염소 또는 브롬이다.
  2. 제1항에 있어서, 모화합물인 옥시캄 출발물질에 대하여 적어도 등가몰량의 아실할라이드를 사용하는 방법.
  3. 제1항에 있어서, 적어도 등가량의 적절한 표준염기의 존재하에 거의 무수상태의 조건하에 반응불활성 유기용매중에서 반응을 수행하는 방법.
  4. 제3항에 있어서, 약 0 내지 약 50℃의 온도하에서 약 30분 내지 약 125시간동안 반응을 수행하는 방법.
  5. 제3항에 있어서, 용매가 할로겐화 저급탄화수소이고, 표준염기가 3급 아민인 방법.
  6. 제1항에 있어서, 제조된 화합물이 2-메틸-4-[4-(모르폴리노메틸)-벤조일옥시]-N-(2-피리디닐)-2H-1,2-벤조티아진-3-카복스아미드-1,1-디옥사이드인 방법.
  7. 제1항에 있어서, 제조된 화합물이 2-메틸-4-[4-(피페리디노메틸)-벤조일옥시]-N-(2-피리디닐)-2H-1,2-벤조티아진-3-카복스아미드-1,1-디옥사이드인 방법.
  8. 제1항에 있어서, 제조된 화합물이 2-메틸-N-(6-메틸-2-피리디닐)-4-[피페리디노메틸)벤조일옥시]-N-(2-피리디닐)-2H-1,2-벤조티아진-3-카복스아미드-1,1-디옥사이드인 방법.
  9. 제1항에 있어서, 제조된 화합물이 2-메틸-4-[4-(메틸피레라지노메틸)벤조일옥시]-N-(2-피리디닐)-2H-1,2-벤조티아진-3-카복스아미드-1,1-디옥사이드인 방법.
  10. 제1항에 있어서, 제조된 화합물이 2-메틸-4-[4-(피리디늄메틸)벤조일옥시]-N-(2-피리디닐)-2H-1,2-벤조티아진-3-카복스아미드-1,1-디옥사이드 클로라이드인 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019860004181A 1985-05-29 1986-05-28 벤조티아진 디옥사이드 유도체의 제조방법 KR870000913B1 (ko)

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US06/738,805 US4623486A (en) 1985-05-29 1985-05-29 [4-substituted benzoyloxy]-N-substituted-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxides having anti-arthritic activity
US738,805 1985-05-29
US738805 1985-05-29

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JP (1) JPS61277683A (ko)
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GR861389B (en) 1986-09-17
IL78912A (en) 1990-07-12
ZA863986B (en) 1988-01-27
DK249086A (da) 1986-11-30
HU200178B (en) 1990-04-28
DE3673710D1 (de) 1990-10-04
ATE56010T1 (de) 1990-09-15
JPS61277683A (ja) 1986-12-08
EP0208404A2 (en) 1987-01-14
DD247451A5 (de) 1987-07-08
CA1270485A (en) 1990-06-19
YU90686A (en) 1987-10-31
ES8707211A1 (es) 1987-07-16
US4623486A (en) 1986-11-18
FI86065B (fi) 1992-03-31
HU199839B (en) 1990-03-28
EP0208404B1 (en) 1990-08-29
KR870000913B1 (ko) 1987-05-06
JPH0575754B2 (ko) 1993-10-21
ES555374A0 (es) 1987-07-16
PH23146A (en) 1989-05-11
EP0208404A3 (en) 1987-04-15
YU44576B (en) 1990-10-31
CN1004628B (zh) 1989-06-28
FI862252A0 (fi) 1986-05-28
EG17811A (en) 1990-08-30
PT82649A (en) 1986-06-01
HUT43597A (en) 1987-11-30
NO862124L (no) 1986-12-01
SU1538896A3 (ru) 1990-01-23
PT82649B (pt) 1988-08-17
FI862252A (fi) 1986-11-30
NZ216310A (en) 1988-10-28
CN86103603A (zh) 1987-01-21
SU1531855A3 (ru) 1989-12-23
FI86065C (fi) 1992-07-10
PL147843B1 (en) 1989-08-31
AU557396B1 (en) 1986-12-18
NO165240C (no) 1991-01-16
DK249086D0 (da) 1986-05-28
NO165240B (no) 1990-10-08

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