PE20110417A1 - Proceso para la preparacion de derivados de l-alanina protegidos - Google Patents

Proceso para la preparacion de derivados de l-alanina protegidos

Info

Publication number
PE20110417A1
PE20110417A1 PE2011000939A PE2011000939A PE20110417A1 PE 20110417 A1 PE20110417 A1 PE 20110417A1 PE 2011000939 A PE2011000939 A PE 2011000939A PE 2011000939 A PE2011000939 A PE 2011000939A PE 20110417 A1 PE20110417 A1 PE 20110417A1
Authority
PE
Peru
Prior art keywords
formula
compound
organic solvent
alkyl
mixture
Prior art date
Application number
PE2011000939A
Other languages
English (en)
Inventor
Luigi Anzalone
Penina Feibush
Frank J Villani
Original Assignee
Janssen Pharmaceutica Nv
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41796530&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20110417(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of PE20110417A1 publication Critical patent/PE20110417A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C227/00—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C227/14—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof
    • C07C227/16—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof by reactions not involving the amino or carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00—Preparation of carboxylic acid amides
    • C07C231/06—Preparation of carboxylic acid amides from nitriles by transformation of cyano groups into carboxamide groups
    • 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
    • C07C269/06—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 by reactions not involving the formation of carbamate groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/04—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C229/06—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton
    • C07C229/10—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
    • C07C229/12—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings to carbon atoms of acyclic carbon skeletons
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00—Preparation of carboxylic acid amides
    • C07C231/14—Preparation of carboxylic acid amides by formation of carboxamide groups together with reactions not involving the carboxamide groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/64—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/65—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/28—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton
    • C07C237/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C253/00—Preparation of carboxylic acid nitriles
    • C07C253/16—Preparation of carboxylic acid nitriles by reaction of cyanides with lactones or compounds containing hydroxy groups or etherified or esterified hydroxy groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/22—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C303/00—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
    • C07C303/26—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of esters of sulfonic acids
    • C07C303/28—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of esters of sulfonic acids by reaction of hydroxy compounds with sulfonic acids or derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F3/00—Compounds containing elements of Groups 2 or 12 of the Periodic Table
    • C07F3/06—Zinc compounds

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Health & Medical Sciences (AREA)
  • Toxicology (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Catalysts (AREA)

Abstract

REFERIDA A UN PROCESO DE PREPARACION DE UN COMPUESTO DE FORMULA (I), DONDE PG1 ES UN GRUPO PROTECTOR DE NITROGENO TAL COMO TERT-BUTOXICARBONILO (Boc); R0 ES H, ALQUILO C1-C4 Y BENCILO; R6 ES H O ALQUILO C1-C6; R4 ES ARILO O HETEROARILO. DICHO PROCESO CONSISTE EN HACER REACCIONAR UN COMPUESTO DE FORMULA (X), EN PRESENCIA DE UNA FUENTE DE YODO, EN UN PRIMER SOLVENTE ORGANICO O UNA MEZCLA DE SOLVENTES ORGANICOS, PARA OBTENER UN COMPUESTO DE FORMULA (XI) QUE SE HACE REACCIONAR CON UN COMPUESTO DE FORMULA R4-LG1, EN PRESENCIA DE UN CATALIZADOR DE PALADIO Y UN SISTEMA DE LIGANDOS DE FOSFINA QUE ES UNA COMBINACION DE Pd2(dba)3 Y P(o-tol)3, EN UN SEGUNDO DISOLVENTE ORGANICO O UNA MEZCLA DE DISOLVENTES ORGANICOS, PARA OBTENER EL COMPUESTO DE FORMULA (I); DONDE PG1 ES UN GRUPO DE PROTECCION DE NITROGENO CON ZINC, EL PRIMER SOLVENTE ORGANICO NO ES REACTIVO A LA FUENTE DE YODO Y ES DIMETILACETAMIDA, LG1 ES UN GRUPO SALIENTE TAL COMO BROMO. LOS COMPUESTOS DERIVADOS DE L-ALANINA OBTENIDOS MEDIANTE ESTE PROCEDIMIENTO SON UTILES COMO INTERNEDIARIOS DE LA SINTESIS DE COMPUESTOS MODULADORES OPIOIDES MU/DELTA
PE2011000939A 2008-10-27 2009-10-27 Proceso para la preparacion de derivados de l-alanina protegidos PE20110417A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US10864908P 2008-10-27 2008-10-27

Publications (1)

Publication Number Publication Date
PE20110417A1 true PE20110417A1 (es) 2011-06-22

Family

ID=41796530

Family Applications (2)

Application Number Title Priority Date Filing Date
PE2014000876A PE20141698A1 (es) 2008-10-27 2009-10-27 Proceso para la preparacion de derivados de l-alanina protegidos
PE2011000939A PE20110417A1 (es) 2008-10-27 2009-10-27 Proceso para la preparacion de derivados de l-alanina protegidos

Family Applications Before (1)

Application Number Title Priority Date Filing Date
PE2014000876A PE20141698A1 (es) 2008-10-27 2009-10-27 Proceso para la preparacion de derivados de l-alanina protegidos

Country Status (25)

Country Link
US (3) US8710256B2 (es)
EP (1) EP2362868B1 (es)
JP (2) JP5592893B2 (es)
KR (1) KR101690195B1 (es)
CN (2) CN102264691B (es)
AR (1) AR075291A1 (es)
AU (1) AU2009320156B2 (es)
BR (1) BRPI0920834B1 (es)
CA (1) CA2741790C (es)
CL (1) CL2011000936A1 (es)
CO (1) CO6361989A2 (es)
CR (1) CR20110286A (es)
EA (1) EA018913B1 (es)
EC (1) ECSP11011008A (es)
ES (1) ES2657676T3 (es)
HN (1) HN2011001186A (es)
HU (1) HUE038302T2 (es)
IL (1) IL212464A (es)
MX (1) MX2011004393A (es)
NI (1) NI201100078A (es)
NZ (1) NZ592415A (es)
PE (2) PE20141698A1 (es)
TW (1) TWI468375B (es)
UA (1) UA110600C2 (es)
WO (1) WO2010062590A2 (es)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI468375B (zh) * 2008-10-27 2015-01-11 Janssen Pharmaceutica Nv 製備經保護之ｌ－丙胺酸衍生物之方法
TWI640541B (zh) 2011-12-28 2018-11-11 中外製藥股份有限公司 Peptide compound having an annular portion and pharmaceutical composition thereof
WO2015117147A1 (en) 2014-02-03 2015-08-06 Quadriga Biosciences, Inc. Beta-substituted beta-amino acids and analogs as chemotherapeutic agents
WO2015117146A1 (en) 2014-02-03 2015-08-06 Quadriga Biosciences, Inc. Beta-substituted gamma-amino acids and analogs as chemotherapeutic agents
KR20180035894A (ko) 2015-08-03 2018-04-06 콰드리가 바이오사이언시스 인코포레이티드 화학치료제로서의 베타-치환된 베타-아미노산 및 유사체 및 이들의 용도
WO2017043626A1 (ja) * 2015-09-11 2017-03-16 株式会社カネカ 光学活性４－カルバモイル－２，６－ジメチルフェニルアラニン誘導体の製造法
CN107129444B (zh) * 2016-02-29 2018-08-31 尚科生物医药（上海）有限公司 (s)-2-叔丁氧羰基氨基-3-(4-氨甲酰基-2,6-二甲基苯基)丙酸制备方法
CN105777584B (zh) * 2016-03-28 2018-01-02 成都伊诺达博医药科技有限公司 丙氨酸衍生物的制备方法
CN105693554B (zh) * 2016-04-06 2017-08-08 成都伊诺达博医药科技有限公司 丙氨酸衍生物的制备方法
WO2018055528A2 (en) * 2016-09-20 2018-03-29 Sun Pharmaceutical Industries Limited Processes for the preparation of eluxadoline
CN106636246B (zh) * 2016-12-28 2020-03-24 尚科生物医药（上海）有限公司 生物法制备(s)-1-(5-苯基-1h-咪唑-2-基)乙胺
CN106636241B (zh) * 2016-12-28 2020-04-03 尚科生物医药（上海）有限公司 一种酶法制备艾沙度林中间体的方法
CN106866463B (zh) * 2017-01-24 2018-08-28 富乐马鸿凯（大连）医药有限公司 艾沙度林中间体的制备方法
EP3636656A4 (en) 2017-06-09 2021-04-14 Chugai Seiyaku Kabushiki Kaisha PROCESS FOR SYNTHESIS OF A PEPTIDE CONTAINING AN N-SUBSTITUTED AMINO ACID
JP7411414B2 (ja) 2017-12-15 2024-01-11 中外製薬株式会社 ペプチドの製造方法、及び塩基の処理方法
CN110092735B (zh) * 2018-01-31 2021-05-11 尚科生物医药（上海）有限公司 一种l-丙氨酸衍生物的制备方法
WO2019197274A1 (en) 2018-04-09 2019-10-17 Quimica Sintetica, S. A. Process for the preparation of opioid modulators
WO2020111238A1 (ja) 2018-11-30 2020-06-04 中外製薬株式会社 ペプチド化合物、またはアミド化合物の脱保護法および固相反応における脱樹脂方法、並びにペプチド化合物の製造方法
JP7472101B2 (ja) 2019-03-15 2024-04-22 中外製薬株式会社 芳香族アミノ酸誘導体の製造方法
CN111620876B (zh) * 2020-05-07 2021-09-28 普济生物科技（台州）有限公司 瑞德西韦关键中间体的合成方法

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JP2780372B2 (ja) 1989-08-29 1998-07-30 株式会社日立製作所 デイスク制御装置のキヤツシユ組込制御方法
JP2881473B2 (ja) * 1990-03-30 1999-04-12 日産化学工業株式会社 α―置換シクロペンテノン誘導体及びその製造法並びに該誘導体を得るための有機亜鉛試剤
US5554753A (en) 1993-08-25 1996-09-10 Indiana University Foundation Catalytic enantioselective synthesis of α-amino acid derivatives by phase-transfer catalysis
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CA2601674A1 (en) * 2005-03-14 2006-09-21 Janssen Pharmaceutica N.V. Process for the preparation of opioid modulators
TWI468375B (zh) * 2008-10-27 2015-01-11 Janssen Pharmaceutica Nv 製備經保護之ｌ－丙胺酸衍生物之方法

Also Published As

Publication number Publication date
JP5592893B2 (ja) 2014-09-17
AU2009320156A1 (en) 2010-06-03
WO2010062590A2 (en) 2010-06-03
EP2362868B1 (en) 2017-12-20
WO2010062590A3 (en) 2010-07-08
BRPI0920834A2 (pt) 2019-04-09
AU2009320156B2 (en) 2014-02-13
ES2657676T3 (es) 2018-03-06
CR20110286A (es) 2012-01-06
KR101690195B1 (ko) 2016-12-27
CA2741790C (en) 2017-09-05
HN2011001186A (es) 2014-06-09
US8710256B2 (en) 2014-04-29
MX2011004393A (es) 2011-05-25
CN102264691A (zh) 2011-11-30
NI201100078A (es) 2011-10-21
EA201170618A1 (ru) 2011-12-30
JP2012506909A (ja) 2012-03-22
AR075291A1 (es) 2011-03-23
US8853445B2 (en) 2014-10-07
CN102264691B (zh) 2017-05-03
EP2362868A2 (en) 2011-09-07
CN107382781A (zh) 2017-11-24
UA110600C2 (uk) 2016-01-25
EA018913B1 (ru) 2013-11-29
CA2741790A1 (en) 2010-06-03
TWI468375B (zh) 2015-01-11
ECSP11011008A (es) 2011-05-31
CO6361989A2 (es) 2012-01-20
PE20141698A1 (es) 2014-11-19
IL212464A0 (en) 2011-06-30
IL212464A (en) 2014-11-30
US20140135525A1 (en) 2014-05-15
US20100145090A1 (en) 2010-06-10
US20140378701A1 (en) 2014-12-25
JP2015013862A (ja) 2015-01-22
BRPI0920834B1 (pt) 2020-11-24
CL2011000936A1 (es) 2012-04-09
TW201035020A (en) 2010-10-01
US9187408B2 (en) 2015-11-17
HUE038302T2 (hu) 2018-10-29
NZ592415A (en) 2013-01-25
KR20110077005A (ko) 2011-07-06

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