CN109206361A - 用于托法替尼制备的有用中间体手性3-氨基哌啶的改进制备方法 - Google Patents

用于托法替尼制备的有用中间体手性3-氨基哌啶的改进制备方法 Download PDF

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Publication number
CN109206361A
CN109206361A CN201810568925.4A CN201810568925A CN109206361A CN 109206361 A CN109206361 A CN 109206361A CN 201810568925 A CN201810568925 A CN 201810568925A CN 109206361 A CN109206361 A CN 109206361A
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formula
compound
salt
enantiomeric excess
optical configuration
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Chinese (zh)
Inventor
米瑞娅·帕斯托阿吉拉尔
萨拉·普雷西亚多加莱戈
埃马努埃莱·米泽拉齐
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Fabbrica Italiana Sintetici SpA (FIS)
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Fabbrica Italiana Sintetici SpA (FIS)
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 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
    • C07D211/56—Nitrogen atoms
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J31/00—Catalysts comprising hydrides, coordination complexes or organic compounds
    • B01J31/16—Catalysts comprising hydrides, coordination complexes or organic compounds containing coordination complexes
    • B01J31/22—Organic complexes
    • B01J31/2282—Unsaturated compounds used as ligands
    • B01J31/2291—Olefins
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J31/00—Catalysts comprising hydrides, coordination complexes or organic compounds
    • B01J31/16—Catalysts comprising hydrides, coordination complexes or organic compounds containing coordination complexes
    • B01J31/22—Organic complexes
    • B01J31/2282—Unsaturated compounds used as ligands
    • B01J31/2295—Cyclic compounds, e.g. cyclopentadienyls
    • 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
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J2231/00—Catalytic reactions performed with catalysts classified in B01J31/00
    • B01J2231/60—Reduction reactions, e.g. hydrogenation
    • B01J2231/64—Reductions in general of organic substrates, e.g. hydride reductions or hydrogenations
    • B01J2231/641—Hydrogenation of organic substrates, i.e. H2 or H-transfer hydrogenations, e.g. Fischer-Tropsch processes
    • B01J2231/645—Hydrogenation of organic substrates, i.e. H2 or H-transfer hydrogenations, e.g. Fischer-Tropsch processes of C=C or C-C triple bonds
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J2531/00—Additional information regarding catalytic systems classified in B01J31/00
    • B01J2531/80—Complexes comprising metals of Group VIII as the central metal
    • B01J2531/82—Metals of the platinum group
    • B01J2531/822—Rhodium
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J2531/00—Additional information regarding catalytic systems classified in B01J31/00
    • B01J2531/80—Complexes comprising metals of Group VIII as the central metal
    • B01J2531/84—Metals of the iron group
    • B01J2531/842—Iron
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Inorganic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Materials Engineering (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hydrogenated Pyridines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
CN201810568925.4A 2017-06-29 2018-06-05 用于托法替尼制备的有用中间体手性3-氨基哌啶的改进制备方法 Pending CN109206361A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP17178755.9A EP3421455B1 (en) 2017-06-29 2017-06-29 Improved process for the preparation of chiral 3-amino-piperidins, useful intermediates for the preparation of tofacitinib
EP17178755.9 2017-06-29

Publications (1)

Publication Number Publication Date
CN109206361A true CN109206361A (zh) 2019-01-15

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Family Applications (1)

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CN201810568925.4A Pending CN109206361A (zh) 2017-06-29 2018-06-05 用于托法替尼制备的有用中间体手性3-氨基哌啶的改进制备方法

Country Status (4)

Country Link
US (1) US20190002407A1 (https=)
EP (1) EP3421455B1 (https=)
JP (1) JP6917949B2 (https=)
CN (1) CN109206361A (https=)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109761884A (zh) * 2019-01-30 2019-05-17 湖北扬信医药科技有限公司 一种手性胺b的制备方法及其应用
CN113125587A (zh) * 2019-12-30 2021-07-16 成都百裕制药股份有限公司 一种托法替尼中间体及其对映异构体的检测方法
CN113614069A (zh) * 2019-04-05 2021-11-05 柳韩洋行 用于制备(3r,4r)-1-苄基-n,4-二甲基哌啶-3-胺或其盐的方法以及使用其制备托法替尼的方法
CN113899831A (zh) * 2021-10-11 2022-01-07 湖北科益药业股份有限公司 一种枸橼酸托法替布起始物料的液相色谱检测方法

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CN1984877A (zh) * 2004-07-08 2007-06-20 默克公司 四取代的烯酰胺的形成及其立体选择性还原
CN101233138A (zh) * 2005-07-29 2008-07-30 辉瑞产品公司 吡咯并[2，3-d]嘧啶衍生物、其中间体和合成方法
JP2015507023A (ja) * 2012-02-21 2015-03-05 セルジーン コーポレイション アミノスルホン化合物の調製のための不斉合成方法
CN105189521A (zh) * 2013-02-12 2015-12-23 拜耳医药股份公司 结合至血小板特异性糖蛋白IIb/IIIa的金属螯合化合物
CN105431414A (zh) * 2013-07-08 2016-03-23 先正达参股股份有限公司 用作杀线虫剂的4元环甲酰胺

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PE20081849A1 (es) * 2007-01-04 2009-01-26 Prosidion Ltd Derivados de piperidin-4-il-propoxi-benzamida como agonistas de gpcr
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CN101233138A (zh) * 2005-07-29 2008-07-30 辉瑞产品公司 吡咯并[2，3-d]嘧啶衍生物、其中间体和合成方法
JP2015507023A (ja) * 2012-02-21 2015-03-05 セルジーン コーポレイション アミノスルホン化合物の調製のための不斉合成方法
CN105189521A (zh) * 2013-02-12 2015-12-23 拜耳医药股份公司 结合至血小板特异性糖蛋白IIb/IIIa的金属螯合化合物
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WEILING CAI ET AL.: "Investigation of Practical Routes for the Kilogram-Scale Production of cis-3-Methylamino-4-methylpiperidines", 《ORGANIC PROCESS RESEARCH & DEVELOPMENT》 *
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YOGESH S. PATIL ET AL.: "An Improved and Efficient Process for the Preparation of Tofacitinib Citrate", 《ORGANIC PROCESS RESEARCH & DEVELOPMENT》 *

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109761884A (zh) * 2019-01-30 2019-05-17 湖北扬信医药科技有限公司 一种手性胺b的制备方法及其应用
CN113614069A (zh) * 2019-04-05 2021-11-05 柳韩洋行 用于制备(3r,4r)-1-苄基-n,4-二甲基哌啶-3-胺或其盐的方法以及使用其制备托法替尼的方法
CN113614069B (zh) * 2019-04-05 2024-05-28 柳韩洋行 用于制备(3r,4r)-1-苄基-n,4-二甲基哌啶-3-胺或其盐的方法以及使用其制备托法替尼的方法
CN113125587A (zh) * 2019-12-30 2021-07-16 成都百裕制药股份有限公司 一种托法替尼中间体及其对映异构体的检测方法
CN113899831A (zh) * 2021-10-11 2022-01-07 湖北科益药业股份有限公司 一种枸橼酸托法替布起始物料的液相色谱检测方法
CN113899831B (zh) * 2021-10-11 2023-08-15 湖北科益药业股份有限公司 一种枸橼酸托法替布起始物料的液相色谱检测方法

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Publication number Publication date
JP6917949B2 (ja) 2021-08-11
EP3421455A1 (en) 2019-01-02
US20190002407A1 (en) 2019-01-03
JP2019023181A (ja) 2019-02-14
EP3421455B1 (en) 2019-03-27

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