WO2019105324A1 - 一种水杨胺醋酸盐的制备方法 - Google Patents
一种水杨胺醋酸盐的制备方法 Download PDFInfo
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- WO2019105324A1 WO2019105324A1 PCT/CN2018/117458 CN2018117458W WO2019105324A1 WO 2019105324 A1 WO2019105324 A1 WO 2019105324A1 CN 2018117458 W CN2018117458 W CN 2018117458W WO 2019105324 A1 WO2019105324 A1 WO 2019105324A1
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- acid
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- acetate
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C213/00—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
- C07C213/08—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions not involving the formation of amino groups, hydroxy groups or etherified or esterified hydroxy groups
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C231/00—Preparation of carboxylic acid amides
- C07C231/10—Preparation of carboxylic acid amides from compounds not provided for in groups C07C231/02 - C07C231/08
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C53/00—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
- C07C53/08—Acetic acid
- C07C53/10—Salts thereof
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C209/00—Preparation of compounds containing amino groups bound to a carbon skeleton
- C07C209/04—Preparation of compounds containing amino groups bound to a carbon skeleton by substitution of functional groups by amino groups
- C07C209/22—Preparation of compounds containing amino groups bound to a carbon skeleton by substitution of functional groups by amino groups by substitution of other functional groups
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C209/00—Preparation of compounds containing amino groups bound to a carbon skeleton
- C07C209/54—Preparation of compounds containing amino groups bound to a carbon skeleton by rearrangement reactions
- C07C209/58—Preparation of compounds containing amino groups bound to a carbon skeleton by rearrangement reactions from or via amides
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C209/00—Preparation of compounds containing amino groups bound to a carbon skeleton
- C07C209/62—Preparation of compounds containing amino groups bound to a carbon skeleton by cleaving carbon-to-nitrogen, sulfur-to-nitrogen, or phosphorus-to-nitrogen bonds, e.g. hydrolysis of amides, N-dealkylation of amines or quaternary ammonium compounds
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C211/00—Compounds containing amino groups bound to a carbon skeleton
- C07C211/01—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms
- C07C211/26—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring
- C07C211/27—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring having amino groups linked to the six-membered aromatic ring by saturated carbon chains
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C213/00—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
- C07C213/02—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions involving the formation of amino groups from compounds containing hydroxy groups or etherified or esterified hydroxy groups
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
- C07C215/46—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
- C07C215/48—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by hydroxy groups
- C07C215/50—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by hydroxy groups with amino groups and the six-membered aromatic ring, or the condensed ring system containing that ring, bound to the same carbon atom of the carbon chain
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C269/00—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
- C07C269/04—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups from amines with formation of carbamate groups
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
- C07C51/41—Preparation of salts of carboxylic acids
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
- C07C235/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
- C07C235/32—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
- C07C235/34—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
Abstract
Description
Claims (10)
- 如权利要求1所述的制备方法,其特征在于,步骤(1)中氨基保护的反应温度为0-50℃。
- 如权利要求1所述的制备方法,其特征在于,步骤(1)中氨基保护的反应时间为3-18小时。
- 如权利要求1所述的制备方法,其特征在于,步骤(1)中氨基甲酸叔丁酯与水杨醛的当量比为1.0-3.0:1。
- 如权利要求1所述的制备方法,其特征在于,步骤(1)的反应溶剂选自四氢呋喃、2-甲基四氢呋喃、乙腈或1,4-二氧六环。
- 如权利要求1所述的制备方法,其特征在于,步骤(2)中水解使用的酸选自盐酸、三氟乙酸、氢溴酸或硫酸。
- 如权利要求1所述的制备方法,其特征在于,步骤(2)中的酸水解在醇 类有机溶剂存在下进行。
- 如权利要求7所述的制备方法,其特征在于,所述醇类有机溶剂为C1-4的脂肪醇;优选自甲醇、乙醇、或正丁醇。
- 如权利要求1所述的制备方法,其特征在于,步骤(2)中与醋酸的反应温度为室温至醋酸溶液的回流温度。
- 如权利要求1所述的制备方法,其特征在于,步骤(2)中与醋酸的反应时间为10-24小时。
Priority Applications (8)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US16/768,570 US11512044B2 (en) | 2017-11-28 | 2018-11-26 | Method for preparing salicylamine acetate |
EP18884479.9A EP3719002B8 (en) | 2017-11-28 | 2018-11-26 | Method for preparing salicylamine acetate |
MX2020005544A MX2020005544A (es) | 2017-11-28 | 2018-11-26 | Metodo para preparar acetato de salicilamina. |
CA3083618A CA3083618A1 (en) | 2017-11-28 | 2018-11-26 | Method for preparing salicylamine acetate |
AU2018377588A AU2018377588A1 (en) | 2017-11-28 | 2018-11-26 | Method for preparing salicylamine acetate |
BR112020010618-6A BR112020010618B1 (pt) | 2017-11-28 | 2018-11-26 | Método para preparar acetato de salicilamina |
JP2020545847A JP7454498B2 (ja) | 2017-11-28 | 2018-11-26 | サリチルアミド酢酸塩の製造方法 |
KR1020207018651A KR20200103693A (ko) | 2017-11-28 | 2018-11-26 | 살리실아민 아세테이트를 제조하기 위한 방법 |
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CN201711221319.7 | 2017-11-28 | ||
CN201711221319.7A CN109836341B (zh) | 2017-11-28 | 2017-11-28 | 一种水杨胺醋酸盐的制备方法 |
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WO2019105324A1 true WO2019105324A1 (zh) | 2019-06-06 |
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PCT/CN2018/117458 WO2019105324A1 (zh) | 2017-11-28 | 2018-11-26 | 一种水杨胺醋酸盐的制备方法 |
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US (1) | US11512044B2 (zh) |
EP (1) | EP3719002B8 (zh) |
JP (1) | JP7454498B2 (zh) |
KR (1) | KR20200103693A (zh) |
CN (1) | CN109836341B (zh) |
AU (1) | AU2018377588A1 (zh) |
BR (1) | BR112020010618B1 (zh) |
CA (1) | CA3083618A1 (zh) |
MX (1) | MX2020005544A (zh) |
WO (1) | WO2019105324A1 (zh) |
Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
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JPS55162747A (en) * | 1979-06-07 | 1980-12-18 | Ono Pharmaceut Co Ltd | 2-aminomethylphenol derivative and its preparation |
WO2012104305A1 (en) * | 2011-02-01 | 2012-08-09 | Evolva Sa | Antimicrobial 4-oxoquinolizines |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
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US6117880A (en) * | 1997-10-30 | 2000-09-12 | Merck & Co., Inc. | Somatostatin agonists |
CN101774927A (zh) * | 2010-02-01 | 2010-07-14 | 重庆市春瑞医药化工有限公司 | 一种二苄基乙二胺及其醋酸盐的制备方法 |
PL2731597T3 (pl) | 2011-07-12 | 2024-04-29 | Vanderbilt University | Sposoby leczenia stanu zapalnego i nadciśnienia tętniczego za pomocą wychwytywaczy gamma-ketoaldehydowych |
CN102675143A (zh) * | 2012-06-05 | 2012-09-19 | 自贡鸿鹤化工股份有限公司 | 乙水杨胺的合成方法 |
CN106496182B (zh) * | 2016-09-09 | 2019-07-05 | 复旦大学 | 一种阿托伐他汀测链中间体的制备方法 |
-
2017
- 2017-11-28 CN CN201711221319.7A patent/CN109836341B/zh active Active
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2018
- 2018-11-26 US US16/768,570 patent/US11512044B2/en active Active
- 2018-11-26 CA CA3083618A patent/CA3083618A1/en active Pending
- 2018-11-26 MX MX2020005544A patent/MX2020005544A/es unknown
- 2018-11-26 AU AU2018377588A patent/AU2018377588A1/en active Pending
- 2018-11-26 BR BR112020010618-6A patent/BR112020010618B1/pt active IP Right Grant
- 2018-11-26 KR KR1020207018651A patent/KR20200103693A/ko not_active Application Discontinuation
- 2018-11-26 JP JP2020545847A patent/JP7454498B2/ja active Active
- 2018-11-26 WO PCT/CN2018/117458 patent/WO2019105324A1/zh unknown
- 2018-11-26 EP EP18884479.9A patent/EP3719002B8/en active Active
Patent Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS55162747A (en) * | 1979-06-07 | 1980-12-18 | Ono Pharmaceut Co Ltd | 2-aminomethylphenol derivative and its preparation |
WO2012104305A1 (en) * | 2011-02-01 | 2012-08-09 | Evolva Sa | Antimicrobial 4-oxoquinolizines |
Non-Patent Citations (3)
Title |
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MESTICHELLI, P. ET AL.: "Concise Copper-Catalyzed Synthesis of Tricyclic Biaryl Ether- Linked Aza-Heterocyclic Ring Systems", ORGANIC LETTERS, vol. 15, no. 21, 17 October 2013 (2013-10-17) - 31 December 2013 (2013-12-31), pages 5448 - 5451, XP055615949, ISSN: 1523-7052 * |
PLATTNER, J.J. ET AL.: "Aminomethyl)aryl]oxy]acetic acid esters. A New Class of High- Ceiling Diuretics. 2. Modifications of the Oxyacetic Side Chain", JOURNAL OF MEDICINAL CHEMISTRY, vol. 27, no. 12, 31 December 1984 (1984-12-31), pages 1587 - 1596, XP002357524, ISSN: 0022-2623, doi:10.1021/jm00378a011 * |
See also references of EP3719002A4 * |
Also Published As
Publication number | Publication date |
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CA3083618A1 (en) | 2019-06-06 |
BR112020010618B1 (pt) | 2023-12-26 |
EP3719002B1 (en) | 2023-01-04 |
EP3719002A1 (en) | 2020-10-07 |
MX2020005544A (es) | 2022-11-28 |
EP3719002A4 (en) | 2021-09-29 |
BR112020010618A2 (pt) | 2020-11-10 |
AU2018377588A1 (en) | 2020-07-16 |
US11512044B2 (en) | 2022-11-29 |
EP3719002A9 (en) | 2021-11-10 |
CN109836341B (zh) | 2021-08-27 |
CN109836341A (zh) | 2019-06-04 |
JP7454498B2 (ja) | 2024-03-22 |
US20210053907A1 (en) | 2021-02-25 |
KR20200103693A (ko) | 2020-09-02 |
JP2021504458A (ja) | 2021-02-15 |
EP3719002B8 (en) | 2023-04-05 |
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