CN1168713C - 制备鼻病毒蛋白酶抑制剂的合成路线以及关键的中间体 - Google Patents

制备鼻病毒蛋白酶抑制剂的合成路线以及关键的中间体 Download PDF

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Publication number
CN1168713C
CN1168713C CNB008118779A CN00811877A CN1168713C CN 1168713 C CN1168713 C CN 1168713C CN B008118779 A CNB008118779 A CN B008118779A CN 00811877 A CN00811877 A CN 00811877A CN 1168713 C CN1168713 C CN 1168713C
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China
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compound
formula
reaction
group
acid
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Expired - Fee Related
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CNB008118779A
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Chinese (zh)
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CN1374947A (zh
Inventor
ƽ
田清平
N·K·奈亚
S·巴布
��Ī������
陶军华
��˹��ŵ��
T·J·莫兰
С��׳
R·小达尼诺
L·J·小米彻尔
÷
T·P·雷马楚克
M·J·梅尔尼克
S·L·本德
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Agouron Pharmaceuticals LLC
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Agouron Pharmaceuticals LLC
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    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pyrrole Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Peptides Or Proteins (AREA)
CNB008118779A 1999-08-24 2000-08-23 制备鼻病毒蛋白酶抑制剂的合成路线以及关键的中间体 Expired - Fee Related CN1168713C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US15035899P 1999-08-24 1999-08-24
US60/150,358 1999-08-24

Publications (2)

Publication Number Publication Date
CN1374947A CN1374947A (zh) 2002-10-16
CN1168713C true CN1168713C (zh) 2004-09-29

Family

ID=22534156

Family Applications (1)

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CNB008118779A Expired - Fee Related CN1168713C (zh) 1999-08-24 2000-08-23 制备鼻病毒蛋白酶抑制剂的合成路线以及关键的中间体

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
CN1198838C (zh) 1998-04-30 2005-04-27 阿格罗尼制药公司 抗小rna病毒化合物及其制备方法和用途
ES2230135T3 (es) 1999-08-04 2005-05-01 Agouron Pharmaceuticals, Inc. Compuestos y composiciones anti-picornavirales; utilizaciones farmaceuticas y materiales utilizados para su sintesis.
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
PL365470A1 (en) 2000-06-14 2005-01-10 Agouron Pharmaceuticals, Inc. Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis
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
US20230157998A1 (en) 2020-03-06 2023-05-25 Pfizer Inc. Methods of Inhibiting SARS-CoV-2 Replication and Treating Corona Virus Disease 2019
CN115260074B (zh) * 2022-08-02 2024-06-21 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
AU722704B2 (en) * 1996-05-14 2000-08-10 Agouron Pharmaceuticals, Inc. Inhibitors of picornavirus 3c proteases and methods for their use and preparation
CA2289541A1 (en) * 1997-03-28 1998-10-08 Peter S. Dragovich 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
CN1198838C (zh) * 1998-04-30 2005-04-27 阿格罗尼制药公司 抗小rna病毒化合物及其制备方法和用途

Also Published As

Publication number Publication date
CZ2002632A3 (cs) 2003-04-16
HUP0203365A2 (hu) 2003-02-28
BR0013306A (pt) 2002-05-28
UY26307A1 (es) 2001-04-30
HUP0203365A3 (en) 2003-12-29
EP1206450A1 (en) 2002-05-22
JP2003507453A (ja) 2003-02-25
AU770221B2 (en) 2004-02-19
IL147674A0 (en) 2002-08-14
CA2376452A1 (en) 2001-03-01
CN1374947A (zh) 2002-10-16
ZA200200504B (en) 2003-03-26
AU6797100A (en) 2001-03-19
PL353997A1 (en) 2003-12-15
WO2001014329A1 (en) 2001-03-01
AR025380A1 (es) 2002-11-20
HK1049336A1 (en) 2003-05-09
PE20010517A1 (es) 2001-05-16
KR20020046283A (ko) 2002-06-20
HK1049336B (zh) 2005-05-20
TWI245040B (en) 2005-12-11
CO5200782A1 (es) 2002-09-27
MXPA02001944A (es) 2002-10-31

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