KR840000569A - 치환된 티아졸로[3,2-a]피리미딘의 제조방법 - Google Patents
치환된 티아졸로[3,2-a]피리미딘의 제조방법 Download PDFInfo
- Publication number
- KR840000569A KR840000569A KR1019820003145A KR820003145A KR840000569A KR 840000569 A KR840000569 A KR 840000569A KR 1019820003145 A KR1019820003145 A KR 1019820003145A KR 820003145 A KR820003145 A KR 820003145A KR 840000569 A KR840000569 A KR 840000569A
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- KR
- South Korea
- Prior art keywords
- group
- compound
- formula
- alkyl
- general formula
- Prior art date
Links
- CDUYCVWBLGEWSY-UHFFFAOYSA-N 5h-[1,3]thiazolo[3,2-a]pyrimidine Chemical class C1C=CN=C2SC=CN12 CDUYCVWBLGEWSY-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 14
- 150000003839 salts Chemical class 0.000 claims 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 125000004423 acyloxy group Chemical group 0.000 claims 3
- 125000002485 formyl group Chemical class [H]C(*)=O 0.000 claims 3
- 125000005843 halogen group Chemical group 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- -1 nitro, amino, formylamino, Phenyl group Chemical group 0.000 claims 3
- 125000001559 cyclopropyl group Chemical class [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical compound C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- 230000002378 acidificating effect Effects 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 125000005236 alkanoylamino group Chemical group 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 150000001450 anions Chemical class 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 235000010290 biphenyl Nutrition 0.000 claims 1
- 239000004305 biphenyl Substances 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biochemistry (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Molecular Biology (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
내용 없음
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (27)
- (a) 일반식 (Ⅱ)의 화합물 또는 그 염을 일반식 (Ⅲ)의 알데히드와 반응시락 A가 하나의 결합인 일반식 (Ⅰ)의 화합물을 수득하거나, 또는
- (b) 일반식 (Ⅳ)의 화합물을 일반식 (Ⅲ)의 알데히드와 반응시켜 A가 하나의 결합인 일반식 (Ⅰ)의 화합물을 수득하거나, 또는
- (c) 일반식 (Ⅴ)의 화합물을 일반식 (Ⅵ)의 화합물 또는 일반식 (Ⅶ)의 화합물과 반응시락 각각의 경우에 A가 하나의 결합인 일반식 (Ⅰ)의 화합물을 수득하거나, 또는
- (d) 일반식 (Ⅷ)의 화합물을 시클로프로판화시켜 A가 -CH2- 그룹인 일반식 (Ⅰ)의 화합물을 수득하고 ;
- 필요한 경우, 일반식 (Ⅰ)의 화합물을 일반식 (Ⅰ)의 다른 화합물로 전환시키고 및/또는 필요한 경우, 일반식 (Ⅰ)의 화합물을 그의 약제학적으로 허용되는 염으로 전환시키고 및/또는 필요한 경우, 염을 유리 화합물로 전환시키고 및/또는 필요한 경우, 이성체 혼합물을 단독 이성체로 분리시킴을 포함하여 일반식 (Ⅰ)의 화합물 및 그 약제학적으로 허용되는 염을 제조하는 방법.
-
-
- 상기식에서
- A는 하나의 결합을 완성하여 α- 및 β-탄소원자 사이에 이중 결합을 제공하거나 또는 -CH2- 그룹을 나타내어 α- 및 β-탄소원자를 포함하는 시클로프로판 고리를 제공하고,
- R1및 R2는 각각 독립적으로
- a) 수소 또는 할로겐원자 ;
- b) C1-C4알킬, 시아노 또는 트리플루오로메틸 ;
- c) 티에닐, 피리딜, 바이페닐 또는 나프틸 ;
- d) 치환되지 않았거나 할로겐, C1-C4알킬, 하이드록시, C1-C4알콕시 포트밀옥시, C2-C8알카노일옥시, 트리플루오로메틸, 니트로, 아미노, 포르밀아미노, C2-C8알카노일아미노 중에서 선택된 1 내지 3개의 치환체로 치환된 페닐그룹 ;
- e) 산소원자들이 페닐고리의 두 개의 인접한 탄소원자들과 연결되어 있는 하나 또는 2개의 C1-C4알킬렌 디옥시그룹으로 치환된 페닐그룹 ;
- f) 각각의 R' 및 R"가 독립적으로 수소원자 또는 C1-C4알킬그룹을 나타내는그룹을 나타내고,
- R3는
- a') 수소 또는 할로겐원자 ;
- b') C1-C4알킬 ;
- c') 하이록시, 포르밀옥시 또는 C2-C8알카노일옥시 ;
- d') C1-C4알콕시 또는 C3-C4알케닐옥시를 나타내고,
- R4는
- a") 치환되지 않았거나 또는 C1-C4알킬로 치환된 피리딜 그룹 ;
- b") R5가 수소원자 또는 C1-C4알킬그룹을 나타내는그룹 ;
- c") 일반식의 그룹(여기서, 각각의 R6, R7및 R8이 독립적으로 수소 또는 할로겐원자 ; 하이드록시그룹 ; 치환되지 않았거나 C1-C4디알킬아미노 그룹으로 치환된 C1-C6알콕시 그룹 ; C1-C4알킬그룹 ; 포르밀옥시 또는 C2-C8알카노일옥시그룹 ; -NO2그룹 또는 R9및 R10이 각각 독립적으로 수소원자, C1-C|4알킬그룹, 포르밀 또는 C2-C8알카노일그룹인그룹을 나타낸다.)
- d") 치환되지 않았거나 C1-C4알킬로 치환된 티아졸릴 그룹을 나타내고, Q는 아릴 또는 C1-C6알킬일 수 있으며, Y(-)는 산성 음이온을 나타내고, R11은 C1-C4알킬이다.
- ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB81.21979 | 1981-07-15 | ||
| GB8121979 | 1981-07-15 | ||
| GB8201621 | 1982-01-20 | ||
| GB82.01621 | 1982-01-20 | ||
| GB8212430 | 1982-04-29 | ||
| GB82.12430 | 1982-04-29 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR840000569A true KR840000569A (ko) | 1984-02-25 |
| KR880002301B1 KR880002301B1 (ko) | 1988-10-22 |
Family
ID=27261230
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR8203145A KR880002301B1 (ko) | 1981-07-15 | 1982-07-15 | 치환된 티아졸로[3,2-a]피리미딘의 제조방법 |
Country Status (25)
| Country | Link |
|---|---|
| US (2) | US4444773A (ko) |
| KR (1) | KR880002301B1 (ko) |
| AT (1) | AT384614B (ko) |
| AU (1) | AU551718B2 (ko) |
| CA (1) | CA1208635A (ko) |
| CH (1) | CH653036A5 (ko) |
| DE (1) | DE3226516A1 (ko) |
| DK (1) | DK156222C (ko) |
| ES (2) | ES513808A0 (ko) |
| FI (1) | FI71940C (ko) |
| FR (1) | FR2509734B1 (ko) |
| GB (1) | GB2103608B (ko) |
| GR (1) | GR76208B (ko) |
| HU (1) | HU186951B (ko) |
| IE (1) | IE53426B1 (ko) |
| IL (1) | IL66316A (ko) |
| IT (1) | IT1190914B (ko) |
| LU (1) | LU84262A1 (ko) |
| NL (1) | NL8202706A (ko) |
| NO (1) | NO822441L (ko) |
| NZ (1) | NZ201194A (ko) |
| PT (1) | PT75240B (ko) |
| SE (2) | SE453295B (ko) |
| SU (1) | SU1358786A3 (ko) |
| YU (1) | YU151582A (ko) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NL8202706A (nl) * | 1981-07-15 | 1983-02-01 | Erba Farmitalia | Gesubstitueerde thiazolo3,2-apyrimidinen en werkwijzen ter bereiding ervan. |
| US4537962A (en) * | 1982-02-04 | 1985-08-27 | Farmitalia Carlo Erba, S.P.A. | Substituted 1,3,4-thiadiazolo[3,2-A]pyrimidines and compositions containing them |
| US4546101A (en) * | 1982-09-10 | 1985-10-08 | Fujisawa Pharmaceutical Co., Ltd. | New cephem compounds useful for treating infectious diseases in human being and animals and processes for preparation thereof |
| GB8300728D0 (en) * | 1983-01-12 | 1983-02-16 | Erba Farmitalia | Substituted carboxy-thiazolo / 3 2 - a / pyrimidine derivatives |
| DE10112197A1 (de) * | 2001-03-14 | 2002-09-19 | Gruenenthal Gmbh | Substituierte Pyrazolo- und Thiazolopyrimidine |
| EA018133B1 (ru) * | 2008-01-11 | 2013-05-30 | Гленмарк Фармасьютикалс, С.А. | Конденсированные пиримидиновые производные как модуляторы trpv3 |
| US8119647B2 (en) * | 2008-04-23 | 2012-02-21 | Glenmark Pharmaceuticals S.A. | Fused pyrimidineone compounds as TRPV3 modulators |
| ES2408654T3 (es) * | 2008-07-02 | 2013-06-21 | Avexa Limited | Tiazopirimidinonas y uso de las mismas |
| CN106916168B (zh) * | 2017-03-13 | 2019-08-27 | 牡丹江医学院 | 一种治疗重症胰腺炎的化合物及其制备方法 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3594378A (en) * | 1969-10-24 | 1971-07-20 | Ayerst Mckenna & Harrison | Thiazolopyrimidine derivatives and preparation thereof |
| US3888983A (en) * | 1970-08-14 | 1975-06-10 | Seperic | Derivatives of thiazolino-pyrimidin-6-ones, in inducing analgesia |
| GB2084568A (en) * | 1980-08-16 | 1982-04-15 | Beecham Group Ltd | Imidazothiazole derivatives |
| NL8202706A (nl) * | 1981-07-15 | 1983-02-01 | Erba Farmitalia | Gesubstitueerde thiazolo3,2-apyrimidinen en werkwijzen ter bereiding ervan. |
-
1982
- 1982-07-06 NL NL8202706A patent/NL8202706A/nl not_active Application Discontinuation
- 1982-07-06 AU AU85648/82A patent/AU551718B2/en not_active Ceased
- 1982-07-07 NZ NZ201194A patent/NZ201194A/en unknown
- 1982-07-07 LU LU84262A patent/LU84262A1/xx unknown
- 1982-07-08 AT AT0266182A patent/AT384614B/de not_active IP Right Cessation
- 1982-07-08 ES ES513808A patent/ES513808A0/es active Granted
- 1982-07-12 YU YU01515/82A patent/YU151582A/xx unknown
- 1982-07-12 SE SE8204292A patent/SE453295B/sv not_active IP Right Cessation
- 1982-07-12 IT IT22353/82A patent/IT1190914B/it active
- 1982-07-12 FI FI822468A patent/FI71940C/fi not_active IP Right Cessation
- 1982-07-12 SE SE8204292D patent/SE8204292L/xx not_active Application Discontinuation
- 1982-07-13 CH CH4272/82A patent/CH653036A5/de not_active IP Right Cessation
- 1982-07-13 SU SU823466583A patent/SU1358786A3/ru active
- 1982-07-13 PT PT75240A patent/PT75240B/pt unknown
- 1982-07-14 GB GB08220385A patent/GB2103608B/en not_active Expired
- 1982-07-14 NO NO822441A patent/NO822441L/no unknown
- 1982-07-14 IE IE1692/82A patent/IE53426B1/en unknown
- 1982-07-14 GR GR68755A patent/GR76208B/el unknown
- 1982-07-14 US US06/398,302 patent/US4444773A/en not_active Expired - Fee Related
- 1982-07-14 IL IL66316A patent/IL66316A/xx unknown
- 1982-07-14 HU HU822289A patent/HU186951B/hu not_active IP Right Cessation
- 1982-07-14 DK DK314682A patent/DK156222C/da not_active IP Right Cessation
- 1982-07-14 CA CA000407223A patent/CA1208635A/en not_active Expired
- 1982-07-15 FR FR8212391A patent/FR2509734B1/fr not_active Expired
- 1982-07-15 KR KR8203145A patent/KR880002301B1/ko active
- 1982-07-15 DE DE19823226516 patent/DE3226516A1/de not_active Ceased
-
1983
- 1983-03-16 ES ES520642A patent/ES520642A0/es active Granted
-
1984
- 1984-05-30 US US06/615,346 patent/US4551457A/en not_active Expired - Fee Related
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