CN112839928B - 用于制备3-[5-氨基-4-(3-氰基苯甲酰基)-吡唑化合物的合成方法 - Google Patents

用于制备3-[5-氨基-4-(3-氰基苯甲酰基)-吡唑化合物的合成方法 Download PDF

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Publication number
CN112839928B
CN112839928B CN201980063294.3A CN201980063294A CN112839928B CN 112839928 B CN112839928 B CN 112839928B CN 201980063294 A CN201980063294 A CN 201980063294A CN 112839928 B CN112839928 B CN 112839928B
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compound
reaction mass
reaction
optionally
aprotic solvent
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CN112839928A (zh
Inventor
马克·梅森巴赫
本杰明·马丁
尼克·约翰内斯·朗德
卡门·鲁伊斯
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Mereo Biopharma 1 Ltd
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Mereo Biopharma 1 Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
    • C07D231/38—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C243/00—Compounds containing chains of nitrogen atoms singly-bound to each other, e.g. hydrazines, triazanes
    • C07C243/10—Hydrazines
    • C07C243/22—Hydrazines having nitrogen atoms of hydrazine groups bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/56—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and doubly-bound oxygen atoms bound to the carbon skeleton
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/16—Systems containing only non-condensed rings with a six-membered ring the ring being unsaturated

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (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)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201980063294.3A 2018-09-26 2019-09-26 用于制备3-[5-氨基-4-(3-氰基苯甲酰基)-吡唑化合物的合成方法 Active CN112839928B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB1815695.0A GB201815695D0 (en) 2018-09-26 2018-09-26 Synthetic method
GB1815695.0 2018-09-26
PCT/GB2019/052718 WO2020065323A1 (en) 2018-09-26 2019-09-26 Synthetic method for the preparation of a 3-[5-amino-4-(3-cyanobenzoyl)-pyrazol compound

Publications (2)

Publication Number Publication Date
CN112839928A CN112839928A (zh) 2021-05-25
CN112839928B true CN112839928B (zh) 2024-04-30

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Country Link
US (1) US11649213B2 (enExample)
EP (1) EP3856721B1 (enExample)
JP (1) JP7291782B2 (enExample)
KR (1) KR102711257B1 (enExample)
CN (1) CN112839928B (enExample)
AU (1) AU2019350525B2 (enExample)
CA (1) CA3112993A1 (enExample)
DK (1) DK3856721T3 (enExample)
ES (1) ES2943289T3 (enExample)
GB (1) GB201815695D0 (enExample)
IL (1) IL281636B2 (enExample)
WO (1) WO2020065323A1 (enExample)

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3658838A (en) * 1968-11-16 1972-04-25 Bayer Ag Process for the preparation of 1 5-disubstituted-4-cyano-pyrazoles
US5922741A (en) * 1996-04-24 1999-07-13 Celltech Therapeutics Ltd. 5-aminopyrazoles useful as tyrosine kinase inhibitors
US6103900A (en) * 1992-12-17 2000-08-15 Pfizer Inc Pyrazoles and pyrazolopyrimidines having CRF antagonistic activity
CN1832928A (zh) * 2003-06-26 2006-09-13 诺瓦提斯公司 以5元杂环为基础的p38激酶抑制剂

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4686221A (en) * 1985-10-01 1987-08-11 Kanebo, Ltd. Quinolinecarboxylic acid compounds and antimicrobial agent containing the same
US6005109A (en) * 1997-10-30 1999-12-21 Pflizer Inc. Pyrazoles and pyrazolopyrimidines having CRF antagonistic activity
FR2732967B1 (fr) 1995-04-11 1997-07-04 Sanofi Sa 1-phenylpyrazole-3-carboxamides substitues, actifs sur la neurotensine, leur preparation, les compositions pharmaceutiques en contenant
PL344004A1 (en) * 1998-05-05 2001-09-10 Hoffmann La Roche Pyrazole derivatives as p-38 map kinase inhibitors
WO2005007632A1 (en) 2003-07-18 2005-01-27 Pharmacia Corporation Substituted pyridazinones as inhibitors of p38
US7485657B2 (en) * 2004-05-12 2009-02-03 Boehringer Ingelheim Pharmaceuticals, Inc. Anti-cytokine heterocyclic compounds
WO2007083320A2 (en) 2006-01-19 2007-07-26 Matrix Laboratories Ltd Conversion of aromatic diazonium salt to aryl hydrazine
US20100292290A1 (en) 2007-08-02 2010-11-18 Vinayak Gore Novel process to prepare almotriptan
CN101910139B (zh) 2008-01-10 2012-09-26 北兴化学工业株式会社 苯基三唑啉酮类的制造方法
JP5602387B2 (ja) 2008-05-02 2014-10-08 キヤノン株式会社 インクジェット用インク、インクジェット記録方法、インクカートリッジ、記録ユニット、及びインクジェット記録装置
CN102964270B (zh) 2012-11-21 2015-01-07 合肥星宇化学有限责任公司 一种亚硫酸钠还原重氮盐合成肼的方法
WO2018059533A1 (zh) * 2016-09-29 2018-04-05 南京明德新药研发股份有限公司 p38αMAPK激酶抑制剂及其制备方法和应用

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3658838A (en) * 1968-11-16 1972-04-25 Bayer Ag Process for the preparation of 1 5-disubstituted-4-cyano-pyrazoles
US6103900A (en) * 1992-12-17 2000-08-15 Pfizer Inc Pyrazoles and pyrazolopyrimidines having CRF antagonistic activity
US5922741A (en) * 1996-04-24 1999-07-13 Celltech Therapeutics Ltd. 5-aminopyrazoles useful as tyrosine kinase inhibitors
CN1832928A (zh) * 2003-06-26 2006-09-13 诺瓦提斯公司 以5元杂环为基础的p38激酶抑制剂

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
1-甲基-5-氨基-4-氰基吡唑的合成;陆慧, 洪梅, 陈书明, 肖亚平;江苏化工(第03期);第35-36页 *
Microwave-assisted synthesis of a pyrazolyl ketone library for evaluation as p38 MAPK inhibitors in Werner syndrome cells;Bagley, Mark C et al.;《Future Medicinal Chemistry》;第2卷(第2期);第203-213页 *
Synthesis of 4-cyano- and 5-aminopyrazoles and deamination of 5-aminopyrazoles;Toche, R. B et al.;《Organic Preparations and Procedures International》;第40卷(第6期);第551-556页 *

Also Published As

Publication number Publication date
EP3856721B1 (en) 2023-03-29
US20210395207A1 (en) 2021-12-23
IL281636B1 (en) 2024-04-01
DK3856721T3 (da) 2023-04-24
KR102711257B1 (ko) 2024-09-30
CN112839928A (zh) 2021-05-25
EP3856721A1 (en) 2021-08-04
ES2943289T3 (es) 2023-06-12
CA3112993A1 (en) 2020-04-02
IL281636A (en) 2021-05-31
KR20210069044A (ko) 2021-06-10
AU2019350525A1 (en) 2021-04-15
JP7291782B2 (ja) 2023-06-15
WO2020065323A1 (en) 2020-04-02
JP2022502400A (ja) 2022-01-11
AU2019350525B2 (en) 2024-05-02
GB201815695D0 (en) 2018-11-07
IL281636B2 (en) 2024-08-01
US11649213B2 (en) 2023-05-16

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