JP2003507453A - ライノウイルスプロテアーゼ・インヒビター及び鍵中間体の調製の為の合成経路 - Google Patents

ライノウイルスプロテアーゼ・インヒビター及び鍵中間体の調製の為の合成経路

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Publication number
JP2003507453A
JP2003507453A JP2001518419A JP2001518419A JP2003507453A JP 2003507453 A JP2003507453 A JP 2003507453A JP 2001518419 A JP2001518419 A JP 2001518419A JP 2001518419 A JP2001518419 A JP 2001518419A JP 2003507453 A JP2003507453 A JP 2003507453A
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JP
Japan
Prior art keywords
group
formula
compound
chemical
cycloalkyl
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
JP2001518419A
Other languages
English (en)
Japanese (ja)
Inventor
キンピン・ティアン
ナレシュ・ケー・ナヤール
スリニバサン・バブ
ジュンファ・タオ
テレンス・ジャロルド・モラン
レイモンド・ジュニア・ダグニノ
レナート・ジェイ・ミッチェル
タラヴィス・ポール・レマーチュク
マイケル・ジョセフ・メルニック
スティーブン・リー・ベンダー
Original Assignee
アゴウロン・ファーマスーティカルス・インコーポレーテッド
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.)
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Publication date
Application filed by アゴウロン・ファーマスーティカルス・インコーポレーテッド filed Critical アゴウロン・ファーマスーティカルス・インコーポレーテッド
Publication of JP2003507453A publication Critical patent/JP2003507453A/ja
Pending legal-status Critical Current

Links

Classifications

    • 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
    • B01J19/00—Chemical, physical or physico-chemical processes in general; Their relevant apparatus
    • B01J19/24—Stationary reactors without moving elements inside
    • B01J19/2415—Tubular reactors
    • B01J19/2435—Loop-type reactors
    • 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
    • C07D207/18—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 one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—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 one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • 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
    • B01J19/00—Chemical, physical or physico-chemical processes in general; Their relevant apparatus
    • B01J19/24—Stationary reactors without moving elements inside
    • B01J19/2475—Membrane reactors
    • 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
    • C07C229/34—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 containing six-membered aromatic rings
    • 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
    • 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
    • C07C69/73—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 unsaturated acids
    • C07C69/732—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 unsaturated acids of unsaturated hydroxy carboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more 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
    • C07D261/18—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • B01J2219/00—Chemical, physical or physico-chemical processes in general; Their relevant apparatus
    • B01J2219/00049—Controlling or regulating processes
    • B01J2219/00051—Controlling the temperature
    • B01J2219/00074—Controlling the temperature by indirect heating or cooling employing heat exchange fluids
    • B01J2219/00087—Controlling the temperature by indirect heating or cooling employing heat exchange fluids with heat exchange elements outside the reactor
    • B01J2219/00099—Controlling the temperature by indirect heating or cooling employing heat exchange fluids with heat exchange elements outside the reactor the reactor being immersed in the heat exchange medium
    • 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
    • B01J2219/00—Chemical, physical or physico-chemical processes in general; Their relevant apparatus
    • B01J2219/00049—Controlling or regulating processes
    • B01J2219/00051—Controlling the temperature
    • B01J2219/00159—Controlling the temperature controlling multiple zones along the direction of flow, e.g. pre-heating and after-cooling

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Pyrrole Compounds (AREA)
  • Peptides Or Proteins (AREA)
JP2001518419A 1999-08-24 2000-08-23 ライノウイルスプロテアーゼ・インヒビター及び鍵中間体の調製の為の合成経路 Pending JP2003507453A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US15035899P 1999-08-24 1999-08-24
US60/150,358 1999-08-24
PCT/US2000/023033 WO2001014329A1 (en) 1999-08-24 2000-08-23 Synthetic routes for the preparation of rhinovirus protease inhibitors and key intermediates

Publications (1)

Publication Number Publication Date
JP2003507453A true JP2003507453A (ja) 2003-02-25

Family

ID=22534156

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2001518419A Pending JP2003507453A (ja) 1999-08-24 2000-08-23 ライノウイルスプロテアーゼ・インヒビター及び鍵中間体の調製の為の合成経路

Country Status (20)

Country Link
EP (1) EP1206450A1 (xx)
JP (1) JP2003507453A (xx)
KR (1) KR20020046283A (xx)
CN (1) CN1168713C (xx)
AR (1) AR025380A1 (xx)
AU (1) AU770221B2 (xx)
BR (1) BR0013306A (xx)
CA (1) CA2376452A1 (xx)
CO (1) CO5200782A1 (xx)
CZ (1) CZ2002632A3 (xx)
HK (1) HK1049336B (xx)
HU (1) HUP0203365A3 (xx)
IL (1) IL147674A0 (xx)
MX (1) MXPA02001944A (xx)
PE (1) PE20010517A1 (xx)
PL (1) PL353997A1 (xx)
TW (1) TWI245040B (xx)
UY (1) UY26307A1 (xx)
WO (1) WO2001014329A1 (xx)
ZA (1) ZA200200504B (xx)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL351250A1 (en) 1998-04-30 2003-04-07 Agouron Pharma Antipicornaviral compounds, their preparation and use
JP2003506457A (ja) 1999-08-04 2003-02-18 アグロン・ファーマシュウティカルズ・インコーポレーテッド 抗ピコルナウィルス化合物及び組成物、その医薬的使用、並びにその合成のための物質
PA8507801A1 (es) 1999-12-03 2002-08-26 Agouron Pharma Compuestos y composiciones antipicornavirales, sus usos farmaceuticos y los materiales para su sintesis
PE20011277A1 (es) 2000-04-14 2002-01-07 Agouron Pharma Compuestos y composiciones antipicornavirales, sus usos farmaceuticos y los materiales para su sintesis
MXPA02012456A (es) 2000-06-14 2004-01-26 Agouron Pharma Compuestos y composiciones antipicornavirales, sus usos farmaceuticos y materiales para su sintesis.
CN1309712C (zh) * 2004-04-02 2007-04-11 中国科学院上海有机化学研究所 Ag7088类化合物的关键中间体的前体及其合成方法
CA3174069A1 (en) 2020-03-06 2021-09-10 Pfizer Inc. Methods of inhibiting sars-cov-2 replication and treating coronavirus disease 2019
CN115260074A (zh) * 2022-08-02 2022-11-01 爱斯特（成都）生物制药股份有限公司 一种口服抗病毒药物Paxlovid中间体的制备方法
CN115322130B (zh) * 2022-08-02 2024-05-14 南京正济医药研究有限公司 制备(s)-2-(boc-氨基)-3-[(s)-2-氧代-3-吡咯烷基]丙酸甲酯

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2254343A1 (en) * 1996-05-14 1997-11-20 Agouron Pharmaceuticals, Inc. Inhibitors of picornavirus 3c proteases and methods for their use and preparation
WO1998043950A1 (en) * 1997-03-28 1998-10-08 Agouron Pharmaceuticals, Inc. Antipicornaviral compouds, compositions containing them, and methods for their use
US5962487A (en) * 1997-12-16 1999-10-05 Agouron Pharmaceuticals, Inc. Antipicornaviral compounds and methods for their use and preparation
PL351250A1 (en) * 1998-04-30 2003-04-07 Agouron Pharma Antipicornaviral compounds, their preparation and use

Also Published As

Publication number Publication date
CN1168713C (zh) 2004-09-29
UY26307A1 (es) 2001-04-30
IL147674A0 (en) 2002-08-14
KR20020046283A (ko) 2002-06-20
CA2376452A1 (en) 2001-03-01
CO5200782A1 (es) 2002-09-27
WO2001014329A1 (en) 2001-03-01
CZ2002632A3 (cs) 2003-04-16
EP1206450A1 (en) 2002-05-22
HUP0203365A3 (en) 2003-12-29
PL353997A1 (en) 2003-12-15
HUP0203365A2 (hu) 2003-02-28
PE20010517A1 (es) 2001-05-16
TWI245040B (en) 2005-12-11
CN1374947A (zh) 2002-10-16
ZA200200504B (en) 2003-03-26
MXPA02001944A (es) 2002-10-31
HK1049336A1 (en) 2003-05-09
HK1049336B (zh) 2005-05-20
AU6797100A (en) 2001-03-19
AU770221B2 (en) 2004-02-19
BR0013306A (pt) 2002-05-28
AR025380A1 (es) 2002-11-20

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