AR092960A1 - Procedimiento para preparar compuestos tienopirimidina - Google Patents

Procedimiento para preparar compuestos tienopirimidina

Info

Publication number
AR092960A1
AR092960A1 ARP130103666A ARP130103666A AR092960A1 AR 092960 A1 AR092960 A1 AR 092960A1 AR P130103666 A ARP130103666 A AR P130103666A AR P130103666 A ARP130103666 A AR P130103666A AR 092960 A1 AR092960 A1 AR 092960A1
Authority
AR
Argentina
Prior art keywords
formula
methyl
morpholinothiene
piperazin
pyrimidin
Prior art date
Application number
ARP130103666A
Other languages
English (en)
Original Assignee
Hoffmann La Roche
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR092960A1 publication Critical patent/AR092960A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • 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
    • C07D295/16—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 acylated on ring nitrogen atoms
    • C07D295/18—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 acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings

Abstract

Reivindicación 1: Procedimiento para la preparación de (S)-1-(4-((2-(2-aminopirimidin-5-il)-7-metil-4-morfolinotieno[3,2-d]pirimidin-6-il)metil)piperazín-1-il)-2-hidroxipropán-1-ona, que presenta la estructura de fórmula (1), y estereoisómeros, isómeros geométricos, tautómeros y sales farmacéuticamente aceptables de los mismos, que comprende: (a) hacer reaccionar una sal de (S)-2-hidroxi-1-(piperazín-1-il)propán-1-ona de fórmula (5) y 2-cloro-7-metil-4-morfolinotieno[3,2-d]pirimidin-6-carbaldehido de fórmula (4) con un agente reductor, proporcionando (S)-1-(4-((2-cloro-7-metil-4-morfolinotieno[3,2-d]pirimidin-6-il)metil)piperazín-1-il)-2-hidroxipropán-1-ona de fórmula (2); y (b) hacer reaccionar el compuesto de fórmula (2), un catalizador de paladio, y ácido 2-aminopirimidín-5-ilborónico que presenta la estructura de fórmula (3) proporcionando el compuesto de fórmula (1).
ARP130103666A 2012-10-10 2013-10-09 Procedimiento para preparar compuestos tienopirimidina AR092960A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201261711900P 2012-10-10 2012-10-10

Publications (1)

Publication Number Publication Date
AR092960A1 true AR092960A1 (es) 2015-05-06

Family

ID=49322377

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP130103666A AR092960A1 (es) 2012-10-10 2013-10-09 Procedimiento para preparar compuestos tienopirimidina

Country Status (13)

Country Link
US (1) US8895729B2 (es)
EP (1) EP2906566B1 (es)
JP (1) JP6123097B2 (es)
KR (1) KR101698283B1 (es)
CN (2) CN104718212B (es)
AR (1) AR092960A1 (es)
BR (1) BR112015007970A8 (es)
CA (1) CA2883513A1 (es)
ES (1) ES2594078T3 (es)
HK (2) HK1244272A1 (es)
MX (1) MX349551B (es)
RU (1) RU2637309C2 (es)
WO (1) WO2014056955A1 (es)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2594078T3 (es) * 2012-10-10 2016-12-15 F. Hoffmann-La Roche Ag Proceso para preparar compuestos de tienopirimidina
CN105189519B (zh) 2013-05-06 2018-01-30 豪夫迈·罗氏有限公司 用于制备硼酸中间体的方法
IL286427B1 (en) 2014-01-28 2024-04-01 Mayo Found Medical Education & Res BCL-2 ANTI-APOPTOTIC PROTEIN FAMILY MEMBERS inhibitors for the treatment of a non-cancerous disease or a disease of the eye
US20170216286A1 (en) 2014-01-28 2017-08-03 Mayo Foundation For Medical Education And Research Killing senescent cells and treating senescence-associated conditions using a src inhibitor and a flavonoid
TW201825465A (zh) 2016-09-23 2018-07-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201815787A (zh) 2016-09-23 2018-05-01 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201813963A (zh) 2016-09-23 2018-04-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
CA3040727A1 (en) * 2016-11-02 2018-05-11 Curis, Inc. Combination therapy with a phosphoinositide 3-kinase inhibitor with a zinc binding moiety
WO2019180141A1 (en) 2018-03-23 2019-09-26 Bayer Aktiengesellschaft Combinations of rogaratinib
CN113717049A (zh) * 2021-08-05 2021-11-30 江西兄弟医药有限公司 一种制备（s）-乙酰氧基丙酰氯的半连续方法

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GB9208135D0 (en) 1992-04-13 1992-05-27 Ludwig Inst Cancer Res Polypeptides having kinase activity,their preparation and use
US6274327B1 (en) 1992-04-13 2001-08-14 Ludwig Institute For Cancer Research Polypeptides having kinase activity, their preparation and use
US5846824A (en) 1994-02-07 1998-12-08 Ludwig Institute For Cancer Research Polypeptides having kinase activity, their preparation and use
US6307087B1 (en) 1998-07-10 2001-10-23 Massachusetts Institute Of Technology Ligands for metals and improved metal-catalyzed processes based thereon
US6395916B1 (en) 1998-07-10 2002-05-28 Massachusetts Institute Of Technology Ligands for metals and improved metal-catalyzed processes based thereon
US7223879B2 (en) 1998-07-10 2007-05-29 Massachusetts Institute Of Technology Ligands for metals and improved metal-catalyzed processes based thereon
CN100528329C (zh) 2001-07-12 2009-08-19 里艾克沙有限公司 微囊包封的催化剂,它们的制备方法和使用方法
GB0423653D0 (en) 2004-10-25 2004-11-24 Piramed Ltd Pharmaceutical compounds
GB0608264D0 (en) * 2006-04-26 2006-06-07 Piramed Ltd Pharmaceutical compounds
WO2007127175A2 (en) 2006-04-26 2007-11-08 F. Hoffmann-La Roche Ag Pharmaceutical compounds
ZA200904531B (en) 2006-12-07 2010-09-29 Hoffmann La Roche Phosphoinositide 3-kinase inhibitor compounds and methods of use
ES2544082T3 (es) 2006-12-07 2015-08-27 F. Hoffmann-La Roche Ag Compuestos inhibidores de fosfoinosítido 3-quinasa y métodos de uso
ZA200904534B (en) * 2006-12-07 2010-09-29 Hoffmann La Roche Phosphoinositide 3-kinase inhibitor compounds and methods of use
CL2008002687A1 (es) 2007-09-12 2009-01-16 Genentech Inc Uso de una combinacion farmaceutica de un compuesto derivado de tieno[3,2-d]pirimidina con un agente quimioterapeutico en el tratamiento de un trastorno hiperproliferativo; kit farmaceutico.
WO2009055730A1 (en) 2007-10-25 2009-04-30 Genentech, Inc. Process for making thienopyrimidine compounds
WO2009076622A2 (en) 2007-12-12 2009-06-18 Massachusetts Institute Of Technology Ligands for transition-metal-catalyzed cross-couplings, and methods of use thereof
JP5709766B2 (ja) 2009-03-12 2015-04-30 ジェネンテック， インコーポレイテッド 造血器腫瘍の治療のためのホスホイノシチド３キナーゼ阻害剤化合物と化学療法剤の併用
AR086647A1 (es) 2011-06-03 2014-01-15 Hoffmann La Roche Metodos para tratar el mesotelioma con un compuesto inhibidor de la pi3k
CN102399235A (zh) * 2011-10-25 2012-04-04 江苏弘和药物研发有限公司 一种2-氨基-5-嘧啶硼酸频哪醇酯的合成方法
CN102367260A (zh) * 2011-12-12 2012-03-07 南京药石药物研发有限公司 2-氨基嘧啶-5-硼酸的合成方法
CN102675323B (zh) * 2012-06-01 2014-04-09 南京药石药物研发有限公司 吡咯并[2,1-f][1,2,4]三嗪衍生物及其抗肿瘤用途
ES2594078T3 (es) * 2012-10-10 2016-12-15 F. Hoffmann-La Roche Ag Proceso para preparar compuestos de tienopirimidina
CN102993163A (zh) * 2012-12-07 2013-03-27 青岛前线生物工程有限公司 3-甲基噻吩-2-甲醛的合成方法

Also Published As

Publication number Publication date
US20140100366A1 (en) 2014-04-10
US8895729B2 (en) 2014-11-25
JP2015534572A (ja) 2015-12-03
CN107188898A (zh) 2017-09-22
KR101698283B1 (ko) 2017-01-19
EP2906566A1 (en) 2015-08-19
MX2015004467A (es) 2015-07-14
CN104718212B (zh) 2017-06-16
HK1211026A1 (en) 2016-05-13
RU2015113747A (ru) 2016-12-10
KR20150054945A (ko) 2015-05-20
CA2883513A1 (en) 2014-04-17
EP2906566B1 (en) 2016-08-24
RU2637309C2 (ru) 2017-12-04
CN107188898B (zh) 2019-12-03
BR112015007970A8 (pt) 2019-08-27
HK1244272A1 (zh) 2018-08-03
WO2014056955A1 (en) 2014-04-17
JP6123097B2 (ja) 2017-05-10
ES2594078T3 (es) 2016-12-15
MX349551B (es) 2017-08-02
BR112015007970A2 (pt) 2017-07-04
CN104718212A (zh) 2015-06-17

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