CN102639492A - β-氨基-α-羟基酰胺的对映-和立体-有择合成 - Google Patents

β-氨基-α-羟基酰胺的对映-和立体-有择合成 Download PDF

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Publication number
CN102639492A
CN102639492A CN2010800438143A CN201080043814A CN102639492A CN 102639492 A CN102639492 A CN 102639492A CN 2010800438143 A CN2010800438143 A CN 2010800438143A CN 201080043814 A CN201080043814 A CN 201080043814A CN 102639492 A CN102639492 A CN 102639492A
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CN
China
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formula
alkyl
aryl
benzyl
alkynyl
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Pending
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CN2010800438143A
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English (en)
Chinese (zh)
Inventor
J·特拉弗斯
W·W·梁
S·P·米勒
J·阿尔巴内斯-沃克
T·J·亨特
L·王
H·廖
A·阿拉萨潘
S·T·特尔扎斯卡
R·M·史密斯
A·勒克哈尔
S·L·博根
J·孔
F·贝内特
F·G·约罗格
M·波瓦里耶
S-C·扩
Y·陈
K·S·马修斯
P·德蒙肖瓦
A·费雷拉
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Merck Sharp and Dohme LLC
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Schering Corp
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Publication of CN102639492A publication Critical patent/CN102639492A/zh
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/52—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C315/00—Preparation of sulfones; Preparation of sulfoxides
    • C07C315/02—Preparation of sulfones; Preparation of sulfoxides by formation of sulfone or sulfoxide groups by oxidation of sulfides, or by formation of sulfone groups by oxidation of sulfoxides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C315/00—Preparation of sulfones; Preparation of sulfoxides
    • C07C315/04—Preparation of sulfones; Preparation of sulfoxides by reactions not involving the formation of sulfone or sulfoxide groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/26—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C317/28—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C319/00—Preparation of thiols, sulfides, hydropolysulfides or polysulfides
    • C07C319/14—Preparation of thiols, sulfides, hydropolysulfides or polysulfides of sulfides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C319/00—Preparation of thiols, sulfides, hydropolysulfides or polysulfides
    • C07C319/14—Preparation of thiols, sulfides, hydropolysulfides or polysulfides of sulfides
    • C07C319/20—Preparation of thiols, sulfides, hydropolysulfides or polysulfides of sulfides by reactions not involving the formation of sulfide groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/347—Preparation of carboxylic acids or their salts, halides or anhydrides by reactions not involving formation of carboxyl groups
    • C07C51/353—Preparation of carboxylic acids or their salts, halides or anhydrides by reactions not involving formation of carboxyl groups by isomerisation; by change of size of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C67/00—Preparation of carboxylic acid esters
    • C07C67/04—Preparation of carboxylic acid esters by reacting carboxylic acids or symmetrical anhydrides onto unsaturated carbon-to-carbon bonds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Engineering & Computer Science (AREA)
  • Virology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pulmonology (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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN2010800438143A 2009-07-29 2010-07-27 β-氨基-α-羟基酰胺的对映-和立体-有择合成 Pending CN102639492A (zh)

Applications Claiming Priority (11)

Application Number Priority Date Filing Date Title
US22963609P 2009-07-29 2009-07-29
US22961309P 2009-07-29 2009-07-29
US22961809P 2009-07-29 2009-07-29
US22965209P 2009-07-29 2009-07-29
US22964809P 2009-07-29 2009-07-29
US61/229,648 2009-07-29
US61/229,652 2009-07-29
US61/229,636 2009-07-29
US61/229,613 2009-07-29
US61/229,618 2009-07-29
PCT/US2010/043356 WO2011014494A1 (en) 2009-07-29 2010-07-27 ENANTIO- AND STEREO-SPECIFIC SYNTHESES OF β-AMINO-α- HYDROXY AMIDES

Publications (1)

Publication Number Publication Date
CN102639492A true CN102639492A (zh) 2012-08-15

Family

ID=42753493

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2010800438143A Pending CN102639492A (zh) 2009-07-29 2010-07-27 β-氨基-α-羟基酰胺的对映-和立体-有择合成

Country Status (12)

Country Link
US (1) US8680294B2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
EP (1) EP2459525B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
JP (1) JP2013500971A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CN (1) CN102639492A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
AR (1) AR077506A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
AU (1) AU2010276490B2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CA (1) CA2768838A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
EA (1) EA022038B1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
GE (1) GEP20207101B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
IN (1) IN2012DN00346A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
SG (1) SG178115A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
WO (1) WO2011014494A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115160205A (zh) * 2022-07-08 2022-10-11 上海皓鸿生物医药科技有限公司 一种制备(s)-1-(叔丁氧羰基)-2,5-二氢-1h-吡咯-2-羧酸及盐的方法

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JOP20180009A1 (ar) 2017-02-06 2019-01-30 Gilead Sciences Inc مركبات مثبط فيروس hiv

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101076516A (zh) * 2004-02-27 2007-11-21 先灵公司 作为丙型肝炎病毒ns3丝氨酸蛋白酶抑制剂的硫化合物

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4825129B2 (ja) 2003-06-17 2011-11-30 シェーリング コーポレイション （１ｒ，２ｓ，５ｓ）−６，６−ジメチル−３−アザビシクロ［３，１，０］ヘキサン−２−カルボキシレートまたはその塩の調製のためのプロセスおよび中間体
CN100450585C (zh) * 2004-04-07 2009-01-14 K·I化成株式会社 包括硫化氢和硫醇等硫化物的除去方法
US7834190B2 (en) * 2006-05-26 2010-11-16 Kaneka Corporation Process for production of optically active-3-amino-2-hydroxypropionic cyclopropylamide derivatives and salts thereof
DE102006059317A1 (de) * 2006-07-04 2008-01-10 Evonik Degussa Gmbh Verfahren zur Herstellung von β-Amino-α-hydroxy-carbonsäureamiden

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101076516A (zh) * 2004-02-27 2007-11-21 先灵公司 作为丙型肝炎病毒ns3丝氨酸蛋白酶抑制剂的硫化合物

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
ASHOK ARASAPPAN,ET AL.: "Discovery of Narlaprevir (SCH 900518): A Potent, Second Generation HCV NS3 Serine Protease Inhibitor", 《ACS MEDICINAL CHEMISTRY LETTERS》 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115160205A (zh) * 2022-07-08 2022-10-11 上海皓鸿生物医药科技有限公司 一种制备(s)-1-(叔丁氧羰基)-2,5-二氢-1h-吡咯-2-羧酸及盐的方法
CN115160205B (zh) * 2022-07-08 2024-06-07 上海皓鸿生物医药科技有限公司 一种制备(s)-1-(叔丁氧羰基)-2,5-二氢-1h-吡咯-2-羧酸及盐的方法

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Publication number Publication date
EP2459525B1 (en) 2017-03-01
AU2010276490B2 (en) 2013-11-14
US8680294B2 (en) 2014-03-25
US20120178942A1 (en) 2012-07-12
IN2012DN00346A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) 2015-05-08
EP2459525A1 (en) 2012-06-06
AU2010276490A1 (en) 2012-03-08
CA2768838A1 (en) 2011-02-03
EA201270223A1 (ru) 2012-07-30
AR077506A1 (es) 2011-08-31
WO2011014494A1 (en) 2011-02-03
JP2013500971A (ja) 2013-01-10
GEP20207101B (en) 2020-05-11
SG178115A1 (en) 2012-03-29
GEAP202012594A (en) 2020-01-27
EA022038B1 (ru) 2015-10-30

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Applicant before: SCHERING CORP (US)

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Application publication date: 20120815