CN111094274A - 一种吡咯并氨基哒嗪酮化合物的制备方法及其中间体 - Google Patents

一种吡咯并氨基哒嗪酮化合物的制备方法及其中间体 Download PDF

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Publication number
CN111094274A
CN111094274A CN201980004505.6A CN201980004505A CN111094274A CN 111094274 A CN111094274 A CN 111094274A CN 201980004505 A CN201980004505 A CN 201980004505A CN 111094274 A CN111094274 A CN 111094274A
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formula
compound represented
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compound
alkyl
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祝令建
管忠俊
姜威
黄建
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Jiangsu Hengrui Medicine Co Ltd
Shanghai Shengdi Pharmaceutical Co Ltd
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Jiangsu Hengrui Medicine Co Ltd
Shanghai Shengdi Pharmaceutical Co Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/66—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
    • C07C69/67—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of saturated acids
    • C07C69/716—Esters of keto-carboxylic acids or aldehydo-carboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C15/00—Cyclic hydrocarbons containing only six-membered aromatic rings as cyclic parts
    • C07C15/40—Cyclic hydrocarbons containing only six-membered aromatic rings as cyclic parts substituted by unsaturated carbon radicals
    • C07C15/42—Cyclic hydrocarbons containing only six-membered aromatic rings as cyclic parts substituted by unsaturated carbon radicals monocyclic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C205/00—Compounds containing nitro groups bound to a carbon skeleton
    • C07C205/27—Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by etherified hydroxy groups
    • C07C205/32—Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by etherified hydroxy groups having nitro groups bound to acyclic carbon atoms and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • 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
    • C07C235/70—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/72—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms
    • C07C235/74—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of a saturated carbon skeleton
    • 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
    • C07D207/30—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 two double bonds between ring members or between ring members and non-ring members
    • C07D207/32—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 two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/33—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 two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems

Abstract

本发明涉及一种吡咯并氨基哒嗪酮化合物的制备方法及其中间体。具体涉及制备式(I)所示化合物的方法，通过改变起始原料和中间体制备目标产物，该方法具备起始原料等反应物简单易购买、反应条件简单可控、反应后处理方法简单、产率高、利于工业扩大生产。

Description

PCT国内申请，说明书已公开。

Claims (35)

  1. PCT国内申请，权利要求书已公开。
CN201980004505.6A 2018-04-13 2019-04-12 一种吡咯并氨基哒嗪酮化合物的制备方法及其中间体 Pending CN111094274A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201810328604 2018-04-13
CN2018103286047 2018-04-13
PCT/CN2019/082367 WO2019196915A1 (zh) 2018-04-13 2019-04-12 一种吡咯并氨基哒嗪酮化合物的制备方法及其中间体

Publications (1)

Publication Number Publication Date
CN111094274A true CN111094274A (zh) 2020-05-01

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CN201980004505.6A Pending CN111094274A (zh) 2018-04-13 2019-04-12 一种吡咯并氨基哒嗪酮化合物的制备方法及其中间体

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Country Link
US (1) US20210147428A1 (zh)
JP (1) JP2021521208A (zh)
KR (1) KR20200144546A (zh)
CN (1) CN111094274A (zh)
AU (1) AU2019251278A1 (zh)
BR (1) BR112020020876A2 (zh)
CA (1) CA3096414A1 (zh)
MX (1) MX2020010773A (zh)
TW (1) TW201943711A (zh)
WO (1) WO2019196915A1 (zh)
ZA (1) ZA202006128B (zh)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021057998A1 (zh) * 2019-09-29 2021-04-01 上海森辉医药有限公司 一种吡咯并氨基哒嗪酮化合物的制备方法
CN112745255A (zh) * 2019-10-30 2021-05-04 江苏恒瑞医药股份有限公司 一种btk激酶抑制剂的制备方法
CN114751850B (zh) * 2022-06-06 2023-08-25 上海再启生物技术有限公司 一种btk激酶抑制剂关键中间体的制备方法
CN114989062A (zh) * 2022-07-04 2022-09-02 上海再启生物技术有限公司 一种btk激酶抑制剂中间体的晶型及其制备方法

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070105904A1 (en) * 2005-10-31 2007-05-10 Eisai R&D Management Co., Ltd. Heterocycles substituted pyridine derivatives and antifungal agent containing thereof
CN103848810A (zh) * 2012-11-30 2014-06-11 北京赛林泰医药技术有限公司 鲁顿酪氨酸激酶抑制剂
CN105837576A (zh) * 2015-01-14 2016-08-10 湖北生物医药产业技术研究院有限公司 Btk抑制剂
CN106573001A (zh) * 2014-07-07 2017-04-19 永恒生物科技公司 作为蛋白激酶抑制剂的氨基哒嗪酮化合物
CN106939002A (zh) * 2016-01-05 2017-07-11 江苏恒瑞医药股份有限公司 一种btk激酶抑制剂的结晶形式及其制备方法
WO2017118277A1 (zh) * 2016-01-05 2017-07-13 江苏恒瑞医药股份有限公司 一种btk激酶抑制剂的结晶形式及其制备方法

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070105904A1 (en) * 2005-10-31 2007-05-10 Eisai R&D Management Co., Ltd. Heterocycles substituted pyridine derivatives and antifungal agent containing thereof
CN103848810A (zh) * 2012-11-30 2014-06-11 北京赛林泰医药技术有限公司 鲁顿酪氨酸激酶抑制剂
CN106573001A (zh) * 2014-07-07 2017-04-19 永恒生物科技公司 作为蛋白激酶抑制剂的氨基哒嗪酮化合物
CN105837576A (zh) * 2015-01-14 2016-08-10 湖北生物医药产业技术研究院有限公司 Btk抑制剂
CN106939002A (zh) * 2016-01-05 2017-07-11 江苏恒瑞医药股份有限公司 一种btk激酶抑制剂的结晶形式及其制备方法
WO2017118277A1 (zh) * 2016-01-05 2017-07-13 江苏恒瑞医药股份有限公司 一种btk激酶抑制剂的结晶形式及其制备方法

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ZA202006128B (en) 2022-01-26
TW201943711A (zh) 2019-11-16
WO2019196915A1 (zh) 2019-10-17
JP2021521208A (ja) 2021-08-26
MX2020010773A (es) 2021-03-02
BR112020020876A2 (pt) 2021-01-26
US20210147428A1 (en) 2021-05-20
AU2019251278A1 (en) 2020-10-08
KR20200144546A (ko) 2020-12-29
EP3778591A1 (en) 2021-02-17
CA3096414A1 (en) 2019-10-17

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