EA002056B1 - Получение промежуточных соединений эндотелина реакцией ассиметрического сопряженного присоединения с использованием хиральной добавки - Google Patents

Получение промежуточных соединений эндотелина реакцией ассиметрического сопряженного присоединения с использованием хиральной добавки Download PDF

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Publication number
EA002056B1
EA002056B1 EA199900661A EA199900661A EA002056B1 EA 002056 B1 EA002056 B1 EA 002056B1 EA 199900661 A EA199900661 A EA 199900661A EA 199900661 A EA199900661 A EA 199900661A EA 002056 B1 EA002056 B1 EA 002056B1
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EA
Eurasian Patent Office
Prior art keywords
alkyl
cycloalkyl
aryl
group
alkenyl
Prior art date
Application number
EA199900661A
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English (en)
Russian (ru)
Other versions
EA199900661A1 (ru
Inventor
Ричард Д. Тилльер
Фенг Ксу
Дэвид М. Щаен
Original Assignee
Мерк Энд Ко., Инк.
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
Priority claimed from GBGB9705858.0A external-priority patent/GB9705858D0/en
Application filed by Мерк Энд Ко., Инк. filed Critical Мерк Энд Ко., Инк.
Publication of EA199900661A1 publication Critical patent/EA199900661A1/ru
Publication of EA002056B1 publication Critical patent/EA002056B1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/28Radicals substituted by singly-bound oxygen or sulphur atoms
    • C07D213/30Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B53/00Asymmetric syntheses
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/44Radicals substituted by doubly-bound oxygen, sulfur, or nitrogen atoms, or by two such atoms singly-bound to the same carbon atom
    • C07D213/46Oxygen atoms
    • C07D213/48Aldehydo radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/54Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/55Acids; Esters
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/84Nitriles
    • C07D213/85Nitriles in position 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Length Measuring Devices By Optical Means (AREA)
  • Steroid Compounds (AREA)
EA199900661A 1997-01-14 1998-01-09 Получение промежуточных соединений эндотелина реакцией ассиметрического сопряженного присоединения с использованием хиральной добавки EA002056B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US3546297P 1997-01-14 1997-01-14
GBGB9705858.0A GB9705858D0 (en) 1997-03-21 1997-03-21 Asymmetric conjugate addition reaction using a chiral additive
PCT/US1998/000263 WO1998030543A1 (en) 1997-01-14 1998-01-09 Endothelin intermediates by asymmetric conjugate addition reaction using a chiral additive

Publications (2)

Publication Number Publication Date
EA199900661A1 EA199900661A1 (ru) 2000-02-28
EA002056B1 true EA002056B1 (ru) 2001-12-24

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
EA199900661A EA002056B1 (ru) 1997-01-14 1998-01-09 Получение промежуточных соединений эндотелина реакцией ассиметрического сопряженного присоединения с использованием хиральной добавки

Country Status (15)

Country Link
EP (1) EP0973742A1 (pt)
JP (1) JP2000507969A (pt)
KR (1) KR20000070085A (pt)
CN (1) CN1243509A (pt)
AU (1) AU728441B2 (pt)
BR (1) BR9806875A (pt)
CA (1) CA2277161A1 (pt)
EA (1) EA002056B1 (pt)
HR (1) HRP980001A2 (pt)
NZ (1) NZ336220A (pt)
PL (1) PL334318A1 (pt)
SK (1) SK93499A3 (pt)
TW (1) TW432028B (pt)
WO (1) WO1998030543A1 (pt)
YU (1) YU30499A (pt)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20010014352A1 (en) 1998-05-27 2001-08-16 Udit Batra Compressed tablet formulation
WO2001019761A2 (en) 1999-09-15 2001-03-22 Massachusetts Institute Of Technology Asymmetric 1,4-reductions of and 1,4-additions to enoates and related systems
GB2355988A (en) 1999-10-28 2001-05-09 Merck & Co Inc Synthesis of cyclopropylacetylene in a one-pot process using a diazo-keto-phos phonate
GB2355724A (en) 1999-10-28 2001-05-02 Merck & Co Inc Synthesis of cyclopropylacetylene from propiolic acid (2-propynoic acid)
WO2010115639A1 (en) 2009-04-09 2010-10-14 Lonza Ltd Process for the synthesis of a propargylic alcohol
WO2010115638A2 (en) 2009-04-09 2010-10-14 Lonza Ltd. Autocatalytic process for the synthesis of chiral propargylic alcohols
EP2447255A1 (en) 2010-10-14 2012-05-02 Lonza Ltd. Process for the synthesis of cyclic carbamates
EP2447247A1 (en) 2010-10-14 2012-05-02 Lonza Ltd. Process for the synthesis of chiral propargylic alcohols

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2086544C1 (ru) * 1991-06-13 1997-08-10 Хоффманн-Ля Рош АГ Бензолсульфонамидные производные пиримидина или их соли, фармацевтическая композиция для лечения заболеваний, связанных с активностью эндотелина
RU2125980C1 (ru) * 1991-11-05 1999-02-10 Смитклайн Бичам Корпорейшн Антагонисты эндотелиновых рецепторов, фармкомпозиция, способ их получения, способ подавления эндотелиновых рецепторов

Also Published As

Publication number Publication date
CA2277161A1 (en) 1998-07-16
TW432028B (en) 2001-05-01
EA199900661A1 (ru) 2000-02-28
KR20000070085A (ko) 2000-11-25
HRP980001A2 (en) 1998-10-31
NZ336220A (en) 2000-12-22
YU30499A (sh) 2002-06-19
AU5908998A (en) 1998-08-03
CN1243509A (zh) 2000-02-02
EP0973742A1 (en) 2000-01-26
BR9806875A (pt) 2000-04-18
JP2000507969A (ja) 2000-06-27
AU728441B2 (en) 2001-01-11
SK93499A3 (en) 2000-05-16
PL334318A1 (en) 2000-02-14
WO1998030543A1 (en) 1998-07-16

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM RU