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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

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C227/00Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C227/14Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof
    • C07C227/16Preparation 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00Preparation of carboxylic acid amides
    • C07C231/06Preparation of carboxylic acid amides from nitriles by transformation of cyano groups into carboxamide groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C269/00Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C269/06Preparation 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02Compounds 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
    • C07C229/04Compounds 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
    • C07C229/06Compounds 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
    • C07C229/10Compounds 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
    • C07C229/12Compounds 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00Preparation of carboxylic acid amides
    • C07C231/14Preparation of carboxylic acid amides by formation of carboxamide groups together with reactions not involving the carboxamide groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/64Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/65Carboxylic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/28Carboxylic 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
    • C07C237/42Carboxylic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C253/00Preparation of carboxylic acid nitriles
    • C07C253/16Preparation of carboxylic acid nitriles by reaction of cyanides with lactones or compounds containing hydroxy groups or etherified or esterified hydroxy groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06Esters of carbamic acids
    • C07C271/08Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10Esters 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
    • C07C271/22Esters 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C303/00Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
    • C07C303/26Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of esters of sulfonic acids
    • C07C303/28Preparation 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F3/00Compounds containing elements of Groups 2 or 12 of the Periodic Table
    • C07F3/06Zinc 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
TWI579296B (zh) 2011-12-28 2017-04-21 Chugai Pharmaceutical Co Ltd Cyclization of Peptide Compounds
SG11201606351VA (en) 2014-02-03 2016-09-29 Quadriga Biosciences Inc Beta-substituted beta-amino acids and analogs as chemotherapeutic agents
EP3102194A1 (en) 2014-02-03 2016-12-14 Quadriga Biosciences, Inc. Beta-substituted gamma-amino acids and analogs as chemotherapeutic agents
DK3269809T3 (da) 2015-03-13 2022-09-12 Chugai Pharmaceutical Co Ltd MODIFICERET AMINOACYL-tRNA-SYNTETASE OG ANVENDELSE DERAF
US9783487B2 (en) 2015-08-03 2017-10-10 Quadriga Biosciences, Inc. Beta-substituted beta-amino acids and analogs as chemotherapeutic agents and uses thereof
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
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
US12391971B2 (en) 2017-01-31 2025-08-19 Chugai Seiyaku Kabushiki Kaisha Method for synthesizing peptides in cell-free translation system
US11542299B2 (en) 2017-06-09 2023-01-03 Chugai Seiyaku Kabushiki Kaisha Method for synthesizing peptide containing N-substituted amino acid
US11492369B2 (en) 2017-12-15 2022-11-08 Chugai Seiyaku Kabushiki Kaisha Method for producing peptide, and method for processing bases
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
JP7279073B2 (ja) 2018-11-07 2023-05-22 中外製薬株式会社 O-置換セリン誘導体の製造方法
CN119143631A (zh) 2018-11-30 2024-12-17 中外制药株式会社 用于肽化合物或酰胺化合物的脱保护方法和在固相反应中的树脂脱除方法以及用于生产肽化合物的方法
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
TWI850887B (zh) 2019-11-07 2024-08-01 日商中外製藥股份有限公司 具有Kras抑制作用的環狀胜肽化合物
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
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Also Published As

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

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