CN101830837A - 合成适用作cpla2抑制剂的c-2、c-3取代的n-烷基化吲哚的方法 - Google Patents
合成适用作cpla2抑制剂的c-2、c-3取代的n-烷基化吲哚的方法 Download PDFInfo
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- CN101830837A CN101830837A CN201010200760A CN201010200760A CN101830837A CN 101830837 A CN101830837 A CN 101830837A CN 201010200760 A CN201010200760 A CN 201010200760A CN 201010200760 A CN201010200760 A CN 201010200760A CN 101830837 A CN101830837 A CN 101830837A
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- 239000011630 iodine Substances 0.000 description 1
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- 229910000021 magnesium carbonate Inorganic materials 0.000 description 1
- ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 description 1
- 229960001708 magnesium carbonate Drugs 0.000 description 1
- 238000012423 maintenance Methods 0.000 description 1
- 229910052751 metal Inorganic materials 0.000 description 1
- 239000002184 metal Substances 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- 150000007530 organic bases Chemical class 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 1
- 229910000073 phosphorus hydride Inorganic materials 0.000 description 1
- DJEHXEMURTVAOE-UHFFFAOYSA-M potassium bisulfite Chemical compound [K+].OS([O-])=O DJEHXEMURTVAOE-UHFFFAOYSA-M 0.000 description 1
- 229910000027 potassium carbonate Inorganic materials 0.000 description 1
- 235000011181 potassium carbonates Nutrition 0.000 description 1
- 235000010259 potassium hydrogen sulphite Nutrition 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 239000002244 precipitate Substances 0.000 description 1
- 238000012545 processing Methods 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 239000012264 purified product Substances 0.000 description 1
- 230000035484 reaction time Effects 0.000 description 1
- 239000013049 sediment Substances 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- 235000017550 sodium carbonate Nutrition 0.000 description 1
- 229910000029 sodium carbonate Inorganic materials 0.000 description 1
- 229940001584 sodium metabisulfite Drugs 0.000 description 1
- 235000010262 sodium metabisulphite Nutrition 0.000 description 1
- 238000009331 sowing Methods 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- YBBRCQOCSYXUOC-UHFFFAOYSA-N sulfuryl dichloride Chemical compound ClS(Cl)(=O)=O YBBRCQOCSYXUOC-UHFFFAOYSA-N 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 238000010189 synthetic method Methods 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
- 230000007704 transition Effects 0.000 description 1
- ITMCEJHCFYSIIV-UHFFFAOYSA-N triflic acid Chemical compound OS(=O)(=O)C(F)(F)F ITMCEJHCFYSIIV-UHFFFAOYSA-N 0.000 description 1
- 125000004044 trifluoroacetyl group Chemical group FC(C(=O)*)(F)F 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/14—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of rings other than six-membered aromatic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C303/00—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
- C07C303/36—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of amides of sulfonic acids
- C07C303/38—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of amides of sulfonic acids by reaction of ammonia or amines with sulfonic acids, or with esters, anhydrides, or halides thereof
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C303/00—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
- C07C303/36—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of amides of sulfonic acids
- C07C303/40—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of amides of sulfonic acids by reactions not involving the formation of sulfonamide groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
- C07C311/12—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings
- C07C311/13—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings the carbon skeleton containing six-membered aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Indole Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US60312404P | 2004-08-19 | 2004-08-19 | |
| US60/603,124 | 2004-08-19 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2005800280209A Division CN101006048B (zh) | 2004-08-19 | 2005-08-18 | 合成适用作cpla2抑制剂的c-2、c-3取代的n-烷基化吲哚的方法 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101830837A true CN101830837A (zh) | 2010-09-15 |
Family
ID=35219553
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201010200760A Pending CN101830837A (zh) | 2004-08-19 | 2005-08-18 | 合成适用作cpla2抑制剂的c-2、c-3取代的n-烷基化吲哚的方法 |
| CN2005800280209A Expired - Fee Related CN101006048B (zh) | 2004-08-19 | 2005-08-18 | 合成适用作cpla2抑制剂的c-2、c-3取代的n-烷基化吲哚的方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2005800280209A Expired - Fee Related CN101006048B (zh) | 2004-08-19 | 2005-08-18 | 合成适用作cpla2抑制剂的c-2、c-3取代的n-烷基化吲哚的方法 |
Country Status (24)
| Country | Link |
|---|---|
| US (3) | US7582772B2 (enExample) |
| EP (1) | EP1778629B1 (enExample) |
| JP (1) | JP2008510707A (enExample) |
| KR (1) | KR20070043036A (enExample) |
| CN (2) | CN101830837A (enExample) |
| AR (1) | AR053410A1 (enExample) |
| AT (1) | ATE517084T1 (enExample) |
| AU (1) | AU2005277392A1 (enExample) |
| BR (1) | BRPI0514431A (enExample) |
| CA (1) | CA2576008A1 (enExample) |
| CR (1) | CR8936A (enExample) |
| EC (1) | ECSP077244A (enExample) |
| GT (1) | GT200500224A (enExample) |
| HN (1) | HN2005000474A (enExample) |
| IL (1) | IL181364A0 (enExample) |
| MX (1) | MX2007002042A (enExample) |
| NO (1) | NO20071253L (enExample) |
| PE (1) | PE20060628A1 (enExample) |
| RU (1) | RU2401829C2 (enExample) |
| SG (1) | SG155214A1 (enExample) |
| SV (1) | SV2006002200A (enExample) |
| TW (1) | TW200609214A (enExample) |
| UA (1) | UA85428C2 (enExample) |
| WO (1) | WO2006023611A1 (enExample) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7713964B2 (en) * | 2001-12-03 | 2010-05-11 | Wyeth Llc | Methods for treating asthmatic conditions |
| US7605156B2 (en) * | 2001-12-03 | 2009-10-20 | Wyeth | Methods for the use of inhibitors of cytosolic phospholipase A2 |
| US7342119B2 (en) * | 2003-09-30 | 2008-03-11 | Wyeth Holdings Corporation | Process for the synthesis of a CPLA2 inhibitor |
| HN2004000536A (es) | 2003-12-16 | 2009-02-18 | Wyeth Corp | Un procediemiento de sintesis para la alquilacion reductiva de la posicon c-3 de indoles |
| TW200718687A (en) | 2005-05-27 | 2007-05-16 | Wyeth Corp | Inhibitors of cytosolic phospholipase A2 |
| WO2008055148A2 (en) * | 2006-10-31 | 2008-05-08 | Wyeth | Semi-solid formulations of phospholipase enzyme inhibitors |
| BRPI0717943A2 (pt) * | 2006-10-31 | 2013-10-29 | Wyeth Corp | Composição farmacêutica; forma de dosagem farmacêutica; processo para a preparação de uma composição farmacêutica; e produto preparado pelo processo |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH02115157A (ja) * | 1988-10-24 | 1990-04-27 | Hokko Chem Ind Co Ltd | スルホニルグリシン誘導体および除草剤 |
| UA81596C2 (en) * | 1999-12-09 | 2008-01-25 | Авентис Кропсаенс Гмбх | Nitro-sulfobenzamides |
| US6984735B2 (en) | 2001-12-03 | 2006-01-10 | Wyeth | Process for making an aldehyde |
| US7713964B2 (en) | 2001-12-03 | 2010-05-11 | Wyeth Llc | Methods for treating asthmatic conditions |
| AU2002351182B2 (en) * | 2001-12-03 | 2009-01-15 | Novartis Ag | Inhibitors of cytosolic phospholipase A2 |
| US7605156B2 (en) | 2001-12-03 | 2009-10-20 | Wyeth | Methods for the use of inhibitors of cytosolic phospholipase A2 |
| US6635771B2 (en) | 2001-12-03 | 2003-10-21 | Wyeth | N-benzhydryl indole compounds |
| US6797708B2 (en) | 2001-12-03 | 2004-09-28 | Wyeth | Inhibitors of cytosolic phospholipase A2 |
| US7101875B2 (en) | 2001-12-03 | 2006-09-05 | Wyeth | Methods for treating arthritic disorders |
| TW200510305A (en) | 2003-07-25 | 2005-03-16 | Wyeth Corp | Process for the preparation of CPLA2 inhibitors |
| CN1829684A (zh) | 2003-07-29 | 2006-09-06 | 西巴特殊化学制品控股公司 | 3-芳基-2-氰基-3-羟基-丙烯酸衍生物 |
| US7582771B2 (en) | 2003-09-03 | 2009-09-01 | Wyeth | Process for the synthesis of cPLA2 inhibitors |
| US7342119B2 (en) | 2003-09-30 | 2008-03-11 | Wyeth Holdings Corporation | Process for the synthesis of a CPLA2 inhibitor |
| HN2004000536A (es) | 2003-12-16 | 2009-02-18 | Wyeth Corp | Un procediemiento de sintesis para la alquilacion reductiva de la posicon c-3 de indoles |
-
2005
- 2005-08-16 AR ARP050103452A patent/AR053410A1/es unknown
- 2005-08-18 GT GT200500224A patent/GT200500224A/es unknown
- 2005-08-18 SV SV2005002200A patent/SV2006002200A/es unknown
- 2005-08-18 SG SG200905383-6A patent/SG155214A1/en unknown
- 2005-08-18 RU RU2007105231/04A patent/RU2401829C2/ru not_active IP Right Cessation
- 2005-08-18 CA CA002576008A patent/CA2576008A1/en not_active Abandoned
- 2005-08-18 KR KR1020077005610A patent/KR20070043036A/ko not_active Ceased
- 2005-08-18 UA UAA200701724A patent/UA85428C2/ru unknown
- 2005-08-18 EP EP05788529A patent/EP1778629B1/en not_active Expired - Lifetime
- 2005-08-18 AU AU2005277392A patent/AU2005277392A1/en not_active Abandoned
- 2005-08-18 BR BRPI0514431-0A patent/BRPI0514431A/pt not_active IP Right Cessation
- 2005-08-18 PE PE2005000959A patent/PE20060628A1/es not_active Application Discontinuation
- 2005-08-18 AT AT05788529T patent/ATE517084T1/de not_active IP Right Cessation
- 2005-08-18 JP JP2007527996A patent/JP2008510707A/ja not_active Ceased
- 2005-08-18 CN CN201010200760A patent/CN101830837A/zh active Pending
- 2005-08-18 MX MX2007002042A patent/MX2007002042A/es not_active Application Discontinuation
- 2005-08-18 WO PCT/US2005/029338 patent/WO2006023611A1/en not_active Ceased
- 2005-08-18 TW TW094128146A patent/TW200609214A/zh unknown
- 2005-08-18 US US11/207,072 patent/US7582772B2/en not_active Expired - Fee Related
- 2005-08-18 CN CN2005800280209A patent/CN101006048B/zh not_active Expired - Fee Related
- 2005-08-24 HN HN2005000474A patent/HN2005000474A/es unknown
-
2007
- 2007-02-13 EC EC2007007244A patent/ECSP077244A/es unknown
- 2007-02-15 IL IL181364A patent/IL181364A0/en unknown
- 2007-02-19 CR CR8936A patent/CR8936A/es not_active Application Discontinuation
- 2007-03-07 NO NO20071253A patent/NO20071253L/no not_active Application Discontinuation
-
2009
- 2009-08-18 US US12/542,914 patent/US7842837B2/en not_active Expired - Fee Related
-
2010
- 2010-11-11 US US12/943,958 patent/US8034960B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| RU2401829C2 (ru) | 2010-10-20 |
| GT200500224A (es) | 2006-03-21 |
| HN2005000474A (es) | 2009-04-07 |
| EP1778629B1 (en) | 2011-07-20 |
| US20060041005A1 (en) | 2006-02-23 |
| WO2006023611A1 (en) | 2006-03-02 |
| IL181364A0 (en) | 2007-07-04 |
| PE20060628A1 (es) | 2006-08-14 |
| BRPI0514431A (pt) | 2008-06-10 |
| EP1778629A1 (en) | 2007-05-02 |
| AU2005277392A1 (en) | 2006-03-02 |
| JP2008510707A (ja) | 2008-04-10 |
| MX2007002042A (es) | 2007-03-29 |
| RU2007105231A (ru) | 2008-09-27 |
| UA85428C2 (ru) | 2009-01-26 |
| ATE517084T1 (de) | 2011-08-15 |
| SV2006002200A (es) | 2006-05-09 |
| CA2576008A1 (en) | 2006-03-02 |
| AR053410A1 (es) | 2007-05-09 |
| CR8936A (es) | 2007-04-26 |
| US8034960B2 (en) | 2011-10-11 |
| US7582772B2 (en) | 2009-09-01 |
| TW200609214A (en) | 2006-03-16 |
| NO20071253L (no) | 2007-05-15 |
| ECSP077244A (es) | 2007-03-29 |
| US7842837B2 (en) | 2010-11-30 |
| US20110054189A1 (en) | 2011-03-03 |
| US20090306428A1 (en) | 2009-12-10 |
| CN101006048A (zh) | 2007-07-25 |
| SG155214A1 (en) | 2009-09-30 |
| KR20070043036A (ko) | 2007-04-24 |
| CN101006048B (zh) | 2011-07-06 |
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