JP2017533203A - 半合成法 - Google Patents
半合成法 Download PDFInfo
- Publication number
- JP2017533203A JP2017533203A JP2017521573A JP2017521573A JP2017533203A JP 2017533203 A JP2017533203 A JP 2017533203A JP 2017521573 A JP2017521573 A JP 2017521573A JP 2017521573 A JP2017521573 A JP 2017521573A JP 2017533203 A JP2017533203 A JP 2017533203A
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- hydrogen
- alkoxy
- alkylene
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 0 CN(C)[C@@](C(CC(Cc(c(*)cc(*)c1O)c1C1=O)C1=C1O)[C@]11O)C(O)=C(C(N)=O)C1=O Chemical compound CN(C)[C@@](C(CC(Cc(c(*)cc(*)c1O)c1C1=O)C1=C1O)[C@]11O)C(O)=C(C(N)=O)C1=O 0.000 description 3
- RDRDQBHUDBIVHT-YCTKZLFKSA-N CN(C)[C@@H](C1CC2Cc(cc3)c4c(O)c3N)C(O)=C(C(N)=O)C3=[O][C@]13C(O)=C2C4=O Chemical compound CN(C)[C@@H](C1CC2Cc(cc3)c4c(O)c3N)C(O)=C(C(N)=O)C3=[O][C@]13C(O)=C2C4=O RDRDQBHUDBIVHT-YCTKZLFKSA-N 0.000 description 2
- JTYKBLZOTIKGLU-OJBBSUIXSA-N CN(C)[C@@H](C(CC(Cc(c(C1=O)c(c([N+]([O-])=O)c2)O)c2F)C1=C1O)[C@]11O)C(O)=C(C(N)=O)C1=N Chemical compound CN(C)[C@@H](C(CC(Cc(c(C1=O)c(c([N+]([O-])=O)c2)O)c2F)C1=C1O)[C@]11O)C(O)=C(C(N)=O)C1=N JTYKBLZOTIKGLU-OJBBSUIXSA-N 0.000 description 1
- ABOKOYYYGCIPIK-KWLNVPAYSA-N CN(C)[C@@H](C(CC(Cc(c(C1=O)c2O)ccc2N)C1=C1O)[C@]11O)C(O)=C(C(N)=O)C1=N Chemical compound CN(C)[C@@H](C(CC(Cc(c(C1=O)c2O)ccc2N)C1=C1O)[C@]11O)C(O)=C(C(N)=O)C1=N ABOKOYYYGCIPIK-KWLNVPAYSA-N 0.000 description 1
- HLFSMUUOKPBTSM-UDHQDRSKSA-N CN(C)[C@@H](C(CC(Cc(c(F)cc(NC(CN1CCCC1)=O)c1O)c1C1=O)C1=C1O)[C@]11O)C(O)=C(C(N)=O)C1=O Chemical compound CN(C)[C@@H](C(CC(Cc(c(F)cc(NC(CN1CCCC1)=O)c1O)c1C1=O)C1=C1O)[C@]11O)C(O)=C(C(N)=O)C1=O HLFSMUUOKPBTSM-UDHQDRSKSA-N 0.000 description 1
- ZKTYHFZIDPAQIY-IWPHMJMQSA-N CN(C)[C@@H](C1CC2Cc(c3c(c(N)c4)O)c4F)C(O)=C(C(N)=O)C4=[O][C@]14C(O)=C2C3=O Chemical compound CN(C)[C@@H](C1CC2Cc(c3c(c(N)c4)O)c4F)C(O)=C(C(N)=O)C4=[O][C@]14C(O)=C2C3=O ZKTYHFZIDPAQIY-IWPHMJMQSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C231/00—Preparation of carboxylic acid amides
- C07C231/12—Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic 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
- C07D295/04—Heterocyclic 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
- C07D295/14—Heterocyclic 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
- C07D295/145—Heterocyclic 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 attached to the same carbon chain, which is not interrupted by carbocyclic rings
- C07D295/15—Heterocyclic 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 attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
- C07C237/24—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton
- C07C237/26—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton of a ring being part of a condensed ring system formed by at least four rings, e.g. tetracycline
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C245/00—Compounds containing chains of at least two nitrogen atoms with at least one nitrogen-to-nitrogen multiple bond
- C07C245/20—Diazonium compounds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/06—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2603/00—Systems containing at least three condensed rings
- C07C2603/02—Ortho- or ortho- and peri-condensed systems
- C07C2603/40—Ortho- or ortho- and peri-condensed systems containing four condensed rings
- C07C2603/42—Ortho- or ortho- and peri-condensed systems containing four condensed rings containing only six-membered rings
- C07C2603/44—Naphthacenes; Hydrogenated naphthacenes
- C07C2603/46—1,4,4a,5,5a,6,11,12a- Octahydronaphthacenes, e.g. tetracyclines
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Communicable Diseases (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Oncology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Hydrogenated Pyridines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462067697P | 2014-10-23 | 2014-10-23 | |
| US62/067,697 | 2014-10-23 | ||
| PCT/US2015/057167 WO2016065290A1 (en) | 2014-10-23 | 2015-10-23 | Semi-synthesis procedures |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2017533203A true JP2017533203A (ja) | 2017-11-09 |
| JP2017533203A5 JP2017533203A5 (enExample) | 2018-11-29 |
Family
ID=54478255
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017521573A Pending JP2017533203A (ja) | 2014-10-23 | 2015-10-23 | 半合成法 |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US10087157B2 (enExample) |
| EP (1) | EP3209642A1 (enExample) |
| JP (1) | JP2017533203A (enExample) |
| CN (1) | CN107108472B (enExample) |
| AU (1) | AU2015335661A1 (enExample) |
| CA (1) | CA2964957A1 (enExample) |
| EA (1) | EA201790897A1 (enExample) |
| MA (1) | MA40836A (enExample) |
| MX (1) | MX369167B (enExample) |
| WO (1) | WO2016065290A1 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112015004523B1 (pt) | 2012-08-31 | 2020-08-04 | Tetraphase Pharmaceuticals, Inc | Compostos de tetraciclina, composições farmacêuticas e seus usos |
| MA40836A (fr) | 2014-10-23 | 2017-08-29 | Tetraphase Pharmaceuticals Inc | Procédures de semi-synthèse |
| WO2017097891A1 (en) | 2015-12-10 | 2017-06-15 | Sandoz Ag | Crystalline eravacycline |
| CN107759503A (zh) * | 2016-08-16 | 2018-03-06 | 四川科伦博泰生物医药股份有限公司 | 一种四环素衍生物及其用途 |
| ES2978198T3 (es) * | 2016-10-19 | 2024-09-06 | Tetraphase Pharmaceuticals Inc | Formas cristalinas de eravaciclina |
| CN111362829B (zh) * | 2018-12-26 | 2021-11-30 | 浙江昌海制药有限公司 | 一种米诺环素二对氯苯磺酸盐晶型及其制备方法和应用 |
| CN109734668B (zh) * | 2019-03-08 | 2020-06-23 | 杭州华樾新材料有限公司 | 四氟硼酸盐离子液体的合成方法 |
| CN110156624B (zh) * | 2019-05-29 | 2022-03-08 | 河北冀衡药业股份有限公司 | 一种米诺环素及其衍生物的合成方法 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2011530534A (ja) * | 2008-08-08 | 2011-12-22 | テトラフェース ファーマシューティカルズ，インコーポレイテッド | Ｃ７−フルオロ置換テトラサイクリン化合物 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB935384A (en) | 1959-03-30 | 1963-08-28 | Pfizer & Co C | Tetracycline derivatives and preparation thereof |
| US3239499A (en) | 1961-05-19 | 1966-03-08 | Pfizer & Co C | Tetracycline derivative |
| RU2300380C2 (ru) * | 2001-10-05 | 2007-06-10 | Тетрадженекс Фармасьютикалс, Инк. | Производные тетрациклина и способы их применения |
| WO2010126607A2 (en) | 2009-04-30 | 2010-11-04 | President And Fellows Of Harvard College | Synthesis of tetracyclines and intermediates thereto |
| JP5944825B2 (ja) * | 2009-08-28 | 2016-07-05 | テトラフェース ファーマシューティカルズ，インコーポレイテッド | テトラサイクリン化合物 |
| JP5820462B2 (ja) * | 2010-03-31 | 2015-11-24 | テトラフェース ファーマシューティカルズ，インコーポレイテッド | 多環式テトラサイクリン化合物 |
| WO2012047907A1 (en) | 2010-10-04 | 2012-04-12 | President And Fellows Of Harvard College | Synthesis of c5-substituted tetracyclines, uses thereof, and intermediates thereto |
| MA40836A (fr) | 2014-10-23 | 2017-08-29 | Tetraphase Pharmaceuticals Inc | Procédures de semi-synthèse |
-
2015
- 2015-10-22 MA MA040836A patent/MA40836A/fr unknown
- 2015-10-23 US US15/521,162 patent/US10087157B2/en not_active Expired - Fee Related
- 2015-10-23 WO PCT/US2015/057167 patent/WO2016065290A1/en not_active Ceased
- 2015-10-23 CN CN201580070869.6A patent/CN107108472B/zh not_active Expired - Fee Related
- 2015-10-23 EP EP15791440.9A patent/EP3209642A1/en not_active Withdrawn
- 2015-10-23 JP JP2017521573A patent/JP2017533203A/ja active Pending
- 2015-10-23 AU AU2015335661A patent/AU2015335661A1/en not_active Abandoned
- 2015-10-23 MX MX2017005223A patent/MX369167B/es active IP Right Grant
- 2015-10-23 CA CA2964957A patent/CA2964957A1/en not_active Abandoned
- 2015-10-23 EA EA201790897A patent/EA201790897A1/ru unknown
-
2018
- 2018-08-09 US US16/059,857 patent/US10618879B2/en not_active Expired - Fee Related
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2011530534A (ja) * | 2008-08-08 | 2011-12-22 | テトラフェース ファーマシューティカルズ，インコーポレイテッド | Ｃ７−フルオロ置換テトラサイクリン化合物 |
Non-Patent Citations (3)
| Title |
|---|
| HLAVKA, JOSEPH J.; KRAZINSKI, H.; BOOTHE, J. H.: "6-Deoxytetracyclines. IV. Photochemical displacement of a diazonium group", JOURNAL OF ORGANIC CHEMISTRY, vol. 27, JPN6019029821, 1962, pages 3674 - 5, ISSN: 0004240910 * |
| JORGE HEREDIA-MOYA, KENNETH L. KIRK: "Photochemical Schiemann Reaction in Ionic Liquids", JOURNAL OF FLUORINE CHEMISTRY, vol. 128（6）, JPN6019029826, 2007, pages 674 - 678, ISSN: 0004240912 * |
| TAKERU FURUYA, JOHANNES E. M. N. KLEIN, TOBIAS RITTER: "Carbon-Fluorine Bond Formation for the Synthesis of Aryl Fluorides", SYNTHESIS, vol. 11, JPN6019029823, 2010, pages 1804 - 1821, ISSN: 0004240911 * |
Also Published As
| Publication number | Publication date |
|---|---|
| MA40836A (fr) | 2017-08-29 |
| US10618879B2 (en) | 2020-04-14 |
| US20170334872A1 (en) | 2017-11-23 |
| CN107108472A (zh) | 2017-08-29 |
| EP3209642A1 (en) | 2017-08-30 |
| AU2015335661A1 (en) | 2017-05-04 |
| US10087157B2 (en) | 2018-10-02 |
| MX369167B (es) | 2019-10-30 |
| US20190210988A1 (en) | 2019-07-11 |
| WO2016065290A1 (en) | 2016-04-28 |
| EA201790897A1 (ru) | 2017-08-31 |
| MX2017005223A (es) | 2017-06-21 |
| CN107108472B (zh) | 2020-03-13 |
| CA2964957A1 (en) | 2016-04-28 |
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