NZ630199A - Process and intermediates for preparing integrase inhibitors - Google Patents
Process and intermediates for preparing integrase inhibitorsInfo
- Publication number
- NZ630199A NZ630199A NZ630199A NZ63019913A NZ630199A NZ 630199 A NZ630199 A NZ 630199A NZ 630199 A NZ630199 A NZ 630199A NZ 63019913 A NZ63019913 A NZ 63019913A NZ 630199 A NZ630199 A NZ 630199A
- Authority
- NZ
- New Zealand
- Prior art keywords
- intermediates
- chloro
- integrase inhibitors
- compounds
- dimethoxyphenyl
- Prior art date
Links
- 239000000543 intermediate Substances 0.000 title abstract 3
- 229940124524 integrase inhibitor Drugs 0.000 title 1
- 239000002850 integrase inhibitor Substances 0.000 title 1
- RLCJXIYWSSMZDH-UHFFFAOYSA-N 1-[5-[(3-chloro-2-fluorophenyl)methyl]-2,4-dimethoxyphenyl]ethanone Chemical compound COC1=CC(OC)=C(C(C)=O)C=C1CC1=CC=CC(Cl)=C1F RLCJXIYWSSMZDH-UHFFFAOYSA-N 0.000 abstract 2
- FKHOOEDRXRLSTH-UHFFFAOYSA-N 1-chloro-3-[(2,4-dimethoxyphenyl)methyl]-2-fluorobenzene Chemical compound COC1=CC(OC)=CC=C1CC1=CC=CC(Cl)=C1F FKHOOEDRXRLSTH-UHFFFAOYSA-N 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- ZTWBZORDUMKEDE-UHFFFAOYSA-N ethyl 3-[5-[(3-chloro-2-fluorophenyl)methyl]-2,4-dimethoxyphenyl]-3-oxopropanoate Chemical compound C1=C(OC)C(C(=O)CC(=O)OCC)=CC(CC=2C(=C(Cl)C=CC=2)F)=C1OC ZTWBZORDUMKEDE-UHFFFAOYSA-N 0.000 abstract 2
- YZMVLKJJJCMVGX-UHFFFAOYSA-N 1,2,3,4-tetrahydroquinoline-2,4-dione Chemical class C1=CC=C2NC(=O)CC(=O)C2=C1 YZMVLKJJJCMVGX-UHFFFAOYSA-N 0.000 abstract 1
- 102100034343 Integrase Human genes 0.000 abstract 1
- 108010061833 Integrases Proteins 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C43/00—Ethers; Compounds having groups, groups or groups
- C07C43/02—Ethers
- C07C43/20—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring
- C07C43/225—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring containing halogen
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C43/00—Ethers; Compounds having groups, groups or groups
- C07C43/02—Ethers
- C07C43/257—Ethers having an ether-oxygen atom bound to carbon atoms both belonging to six-membered aromatic rings
- C07C43/29—Ethers having an ether-oxygen atom bound to carbon atoms both belonging to six-membered aromatic rings containing halogen
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
- C07C45/27—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by oxidation
- C07C45/30—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by oxidation with halogen containing compounds, e.g. hypohalogenation
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
- C07C45/45—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by condensation
- C07C45/46—Friedel-Crafts reactions
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C49/00—Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
- C07C49/76—Ketones containing a keto group bound to a six-membered aromatic ring
- C07C49/84—Ketones containing a keto group bound to a six-membered aromatic ring containing ether groups, groups, groups, or groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C67/00—Preparation of carboxylic acid esters
- C07C67/12—Preparation of carboxylic acid esters from asymmetrical anhydrides
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C67/00—Preparation of carboxylic acid esters
- C07C67/30—Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group
- C07C67/333—Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by isomerisation; by change of size of the carbon skeleton
- C07C67/343—Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
- C07D215/54—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
- C07D215/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3 with oxygen atoms in position 4
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Quinoline Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261679475P | 2012-08-03 | 2012-08-03 | |
| PCT/US2013/053295 WO2014022707A1 (en) | 2012-08-03 | 2013-08-01 | Process and intermediates for preparing integrase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| NZ630199A true NZ630199A (en) | 2016-12-23 |
Family
ID=48980354
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NZ630199A NZ630199A (en) | 2012-08-03 | 2013-08-01 | Process and intermediates for preparing integrase inhibitors |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US8877931B2 (instruction) |
| EP (1) | EP2880017B1 (instruction) |
| JP (1) | JP6147856B2 (instruction) |
| KR (1) | KR20150040340A (instruction) |
| CN (1) | CN104520275B (instruction) |
| AU (1) | AU2013296289B2 (instruction) |
| BR (1) | BR112015002275A2 (instruction) |
| CA (1) | CA2878699C (instruction) |
| EA (1) | EA026089B1 (instruction) |
| ES (1) | ES2608860T3 (instruction) |
| IL (1) | IL236618A (instruction) |
| IN (1) | IN2015DN01688A (instruction) |
| MX (1) | MX337094B (instruction) |
| NZ (1) | NZ630199A (instruction) |
| PT (1) | PT2880017T (instruction) |
| SG (1) | SG11201500812QA (instruction) |
| WO (1) | WO2014022707A1 (instruction) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR122015029881B1 (pt) | 2012-12-21 | 2022-04-26 | Gilead Sciences, Inc | Compostos carbamoilpiridona policíclicos, composição farmacêutica que os compreende e seu uso farmacêutico |
| SI3019503T1 (sl) | 2013-07-12 | 2017-11-30 | Gilead Sciences, Inc. | Policiklične karbamoilpiridonske spojine in njihova uporaba za zdravljenje HIV infekcij |
| NO2865735T3 (instruction) | 2013-07-12 | 2018-07-21 | ||
| NO2717902T3 (instruction) | 2014-06-20 | 2018-06-23 | ||
| TWI677489B (zh) | 2014-06-20 | 2019-11-21 | 美商基利科學股份有限公司 | 多環型胺甲醯基吡啶酮化合物之合成 |
| TW201613936A (en) | 2014-06-20 | 2016-04-16 | Gilead Sciences Inc | Crystalline forms of(2R,5S,13aR)-8-hydroxy-7,9-dioxo-n-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide |
| TWI695003B (zh) | 2014-12-23 | 2020-06-01 | 美商基利科學股份有限公司 | 多環胺甲醯基吡啶酮化合物及其醫藥用途 |
| EP3277691B1 (en) | 2015-04-02 | 2019-01-30 | Gilead Sciences, Inc. | Polycyclic-carbamoylpyridone compounds and their pharmaceutical use |
| CA3160068A1 (en) * | 2019-09-24 | 2021-04-01 | Asymchem Laboratories (Tianjin) Co., Ltd. | Continuous preparation method for benzylzinc halide and derivative thereof |
| CN112661698A (zh) * | 2021-01-14 | 2021-04-16 | 浙江海森药业股份有限公司 | 一种艾维雷韦的制备方法 |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE9904108D0 (sv) * | 1999-11-15 | 1999-11-15 | New Pharma Research Ab | Nya föreningar |
| KR100603163B1 (ko) | 2000-12-14 | 2006-07-24 | 더 프록터 앤드 갬블 캄파니 | 퀴놀론 및 나프티리딘 제조에서의 폐환 공정 단계 |
| TW200300349A (en) | 2001-11-19 | 2003-06-01 | Sankyo Co | A 4-oxoqinoline derivative |
| EP1510510A1 (en) | 2002-05-31 | 2005-03-02 | Banyu Pharmaceutical Co., Ltd. | Method of substituent introduction through halogen-metal exchange reaction |
| US6803469B2 (en) | 2002-08-05 | 2004-10-12 | The Procter & Gamble Company | Process for preparing quinolone antibiotic intermediates |
| TW200409759A (en) | 2002-09-25 | 2004-06-16 | Wyeth Corp | Substituted 4-(indazol-3-yl)phenols |
| TWI248928B (en) * | 2002-11-20 | 2006-02-11 | Japan Tobacco Inc | 4-oxoquinoline compound and use thereof as HIV integrase inhibitor |
| EP1582524B1 (en) | 2004-04-02 | 2008-08-13 | Ludwig Maximilians Universität | Method of preparing organomagnesium compounds |
| EP1582523A1 (en) | 2004-04-02 | 2005-10-05 | Ludwig-Maximilians-Universität München | Method of preparing organomagnesium compounds |
| MY134672A (en) | 2004-05-20 | 2007-12-31 | Japan Tobacco Inc | Stable crystal of 4-oxoquinoline compound |
| US7531554B2 (en) | 2004-05-20 | 2009-05-12 | Japan Tobacco Inc. | 4-oxoquinoline compound and use thereof as HIV integrase inhibitor |
| JP4629104B2 (ja) | 2004-05-21 | 2011-02-09 | 日本たばこ産業株式会社 | ４−オキソキノリン誘導体および抗ｈｉｖ剤を含む併用剤 |
| WO2007063869A1 (ja) | 2005-11-30 | 2007-06-07 | Japan Tobacco Inc. | 高純度キノロン化合物の製造方法 |
| US20090233964A1 (en) | 2005-12-30 | 2009-09-17 | Gilead Sciences, Inc. | Methods for improving the pharmacokinetics of hiv integrase inhibitors |
| IN2014CN00532A (instruction) | 2006-03-06 | 2015-04-03 | Japan Tobacco Inc | |
| KR101023635B1 (ko) | 2006-03-06 | 2011-03-22 | 니뽄 다바코 산교 가부시키가이샤 | 4-옥소퀴놀린 화합물 제조 방법 |
| TW200811153A (en) | 2006-06-23 | 2008-03-01 | Japan Tobacco Inc | 6-(heterocyclyl-substituted benzyl)-4-oxoquinoline compound and use thereof as HIV integrase inhibitor |
| AP3004A (en) | 2006-09-12 | 2014-10-31 | Gilead Sciences Inc | Process and intermediates for preparing integrase inhibitors |
| NZ582086A (en) | 2007-06-29 | 2012-07-27 | Gilead Sciences Inc | Therapeutic compositions and the use thereof |
| AU2008270634B2 (en) | 2007-06-29 | 2014-01-16 | Gilead Sciences, Inc. | Therapeutic compositions and the use thereof |
| AR068403A1 (es) | 2007-09-11 | 2009-11-18 | Gilead Sciences Inc | Proceso e intermediarios para la preparacion de inhibidores de integrasa |
-
2013
- 2013-08-01 CN CN201380041287.6A patent/CN104520275B/zh not_active Expired - Fee Related
- 2013-08-01 MX MX2015001506A patent/MX337094B/es active IP Right Grant
- 2013-08-01 IN IN1688DEN2015 patent/IN2015DN01688A/en unknown
- 2013-08-01 WO PCT/US2013/053295 patent/WO2014022707A1/en active Application Filing
- 2013-08-01 US US13/956,905 patent/US8877931B2/en active Active
- 2013-08-01 JP JP2015525605A patent/JP6147856B2/ja not_active Expired - Fee Related
- 2013-08-01 EP EP13748229.5A patent/EP2880017B1/en active Active
- 2013-08-01 EA EA201590018A patent/EA026089B1/ru not_active IP Right Cessation
- 2013-08-01 BR BR112015002275A patent/BR112015002275A2/pt not_active IP Right Cessation
- 2013-08-01 KR KR20157005620A patent/KR20150040340A/ko not_active Abandoned
- 2013-08-01 NZ NZ630199A patent/NZ630199A/en not_active IP Right Cessation
- 2013-08-01 PT PT137482295T patent/PT2880017T/pt unknown
- 2013-08-01 ES ES13748229.5T patent/ES2608860T3/es active Active
- 2013-08-01 SG SG11201500812QA patent/SG11201500812QA/en unknown
- 2013-08-01 AU AU2013296289A patent/AU2013296289B2/en not_active Ceased
- 2013-08-01 CA CA2878699A patent/CA2878699C/en not_active Expired - Fee Related
-
2015
- 2015-01-11 IL IL236618A patent/IL236618A/en not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| AU2013296289A1 (en) | 2015-02-19 |
| ES2608860T3 (es) | 2017-04-17 |
| AU2013296289B2 (en) | 2017-10-05 |
| JP6147856B2 (ja) | 2017-06-14 |
| PT2880017T (pt) | 2016-12-14 |
| IN2015DN01688A (instruction) | 2015-07-03 |
| KR20150040340A (ko) | 2015-04-14 |
| EA201590018A1 (ru) | 2015-05-29 |
| CN104520275A (zh) | 2015-04-15 |
| EA026089B1 (ru) | 2017-02-28 |
| MX2015001506A (es) | 2015-04-08 |
| US20140039194A1 (en) | 2014-02-06 |
| HK1209415A1 (en) | 2016-04-01 |
| IL236618A0 (en) | 2015-02-26 |
| US8877931B2 (en) | 2014-11-04 |
| EP2880017B1 (en) | 2016-10-05 |
| MX337094B (es) | 2016-02-10 |
| WO2014022707A1 (en) | 2014-02-06 |
| JP2015524822A (ja) | 2015-08-27 |
| HK1209748A1 (en) | 2016-04-08 |
| CA2878699A1 (en) | 2014-02-06 |
| CA2878699C (en) | 2018-09-11 |
| IL236618A (en) | 2017-04-30 |
| SG11201500812QA (en) | 2015-04-29 |
| BR112015002275A2 (pt) | 2017-07-04 |
| CN104520275B (zh) | 2016-11-02 |
| EP2880017A1 (en) | 2015-06-10 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PSEA | Patent sealed | ||
| RENW | Renewal (renewal fees accepted) |
Free format text: PATENT RENEWED FOR 1 YEAR UNTIL 01 AUG 2018 BY DAVIES COLLISON CAVE PTY LTD Effective date: 20170717 |
|
| RENW | Renewal (renewal fees accepted) |
Free format text: PATENT RENEWED FOR 1 YEAR UNTIL 01 AUG 2019 BY COMPUTER PACKAGES INC Effective date: 20180718 |
|
| LAPS | Patent lapsed |