HK1108893A1 - Exo- and diastereo- selective syntheses of himbacine analogs himbacine - Google Patents

Exo- and diastereo- selective syntheses of himbacine analogs himbacine

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Publication number
HK1108893A1
HK1108893A1 HK08102973.9A HK08102973A HK1108893A1 HK 1108893 A1 HK1108893 A1 HK 1108893A1 HK 08102973 A HK08102973 A HK 08102973A HK 1108893 A1 HK1108893 A1 HK 1108893A1
Authority
HK
Hong Kong
Prior art keywords
himbacine
diastereo
exo
analogs
selective syntheses
Prior art date
Application number
HK08102973.9A
Other languages
English (en)
Inventor
George G Wu
Anantha Sudhakar
Tao Wang
Ji Xie
Frank Xing Chen
Marc Poirier
Mingsheng Huang
Vijay Sabesan
Daw-Long Kwok
Jian Cui
Xiaojing Yang
Tiruvettipuram K Thiruvengadam
Jing Liao
Ilia Zavialov
Hoa N Nguyen
Ngiap Kie Lim
Original Assignee
Schering Corp
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
Application filed by Schering Corp filed Critical Schering Corp
Publication of HK1108893A1 publication Critical patent/HK1108893A1/xx

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    • C07ORGANIC CHEMISTRY
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    • 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
    • C07D263/54Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/56Benzoxazoles; Hydrogenated benzoxazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C201/00Preparation of esters of nitric or nitrous acid or of compounds containing nitro or nitroso groups bound to a carbon skeleton
    • C07C201/06Preparation of nitro compounds
    • C07C201/10Preparation of nitro compounds by substitution of functional groups by nitro groups
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C201/00Preparation of esters of nitric or nitrous acid or of compounds containing nitro or nitroso groups bound to a carbon skeleton
    • C07C201/06Preparation of nitro compounds
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C205/00Compounds containing nitro groups bound to a carbon skeleton
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    • C07C205/55Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by carboxyl groups having nitro groups or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the carbon skeleton
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00Preparation of carboxylic acid amides
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00Preparation of carboxylic acid amides
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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/02Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/28Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and unsaturated
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    • 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
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    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/02Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/07Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing oxygen atoms bound to the carbon skeleton
    • C07C309/08Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing oxygen atoms bound to the carbon skeleton containing hydroxy groups bound to the carbon skeleton
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    • C07C69/00Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/52Esters of acyclic unsaturated carboxylic acids having the esterified carboxyl group bound to an acyclic carbon atom
    • C07C69/606Esters of acyclic unsaturated carboxylic acids having the esterified carboxyl group bound to an acyclic carbon atom having only or additionally carbon-to-carbon triple bonds as unsaturation in the carboxylic acid moiety
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    • C07C69/00Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/66Esters 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
    • C07C69/73Esters 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
    • C07C69/732Esters 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
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62Benzothiazoles
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    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/92Naphthofurans; Hydrogenated naphthofurans
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/54Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D333/56Radicals substituted by oxygen atoms
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    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
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    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic System
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/18Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804Compounds having Si-O-C linkages
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    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576Six-membered rings
    • C07F9/58Pyridine rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/12Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/16Systems containing only non-condensed rings with a six-membered ring the ring being unsaturated
    • 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
HK08102973.9A 2005-01-14 2008-03-13 Exo- and diastereo- selective syntheses of himbacine analogs himbacine HK1108893A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US64446405P 2005-01-14 2005-01-14
PCT/US2006/000954 WO2006076415A2 (en) 2005-01-14 2006-01-12 Exo- and diastereo- selective syntheses of himbacine analogs

Publications (1)

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HK1108893A1 true HK1108893A1 (en) 2008-05-23

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US (4) US7605275B2 (sl)
EP (4) EP2196454B1 (sl)
JP (3) JP4681616B2 (sl)
CN (2) CN102757423B (sl)
AR (1) AR056919A1 (sl)
AT (2) ATE458726T1 (sl)
CA (2) CA2594871C (sl)
CY (2) CY1109896T1 (sl)
DE (1) DE602006012450D1 (sl)
DK (2) DK2206697T3 (sl)
ES (3) ES2412981T3 (sl)
HK (1) HK1108893A1 (sl)
HR (2) HRP20100218T1 (sl)
ME (1) ME01967B (sl)
MX (1) MX2007008665A (sl)
PL (2) PL2206697T3 (sl)
PT (2) PT1848705E (sl)
RS (2) RS52117B (sl)
SG (2) SG192505A1 (sl)
SI (2) SI2206697T1 (sl)
WO (1) WO2006076415A2 (sl)
ZA (1) ZA200706711B (sl)

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MX2007008622A (es) * 2005-01-14 2007-09-11 Schering Corp Una sintesis exo-selectiva de analogos de himbacina.
DK2206697T3 (da) 2005-01-14 2012-02-13 Schering Corp Exo- og diastereo-selektive synteser af himbacinanaloger
PT1853592E (pt) * 2005-01-14 2011-05-10 Schering Corp S?ntese de an?logos da himbacina
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AR061727A1 (es) 2006-06-30 2008-09-17 Schering Corp Sintesis de dietil [[ 5- ( 3-fluorofenil) -piridin -2il] metil] fosfonato
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CA2701482C (en) 2007-10-08 2018-10-23 Lux Biosciences, Inc. Ophthalmic compositions comprising calcineurin inhibitors or mtor inhibitors
MX2010004453A (es) * 2007-10-24 2010-07-28 Schering Corp Procedimiento sintetico de alta pureza para la preparacion de intermediarios de ester de acido dodecahidro-nafto-furanil-carbami co.
US9120935B2 (en) * 2011-06-21 2015-09-01 Bluestar Silicones France Sas Hydrosilylation reaction inhibitors, and use thereof for preparing stable curable silicone compositions
CN105330689B (zh) * 2014-08-08 2018-08-17 博瑞生物医药(苏州)股份有限公司 制备Himbacine类似物中间体的制备方法
CN105985303B (zh) * 2015-02-13 2020-08-14 上海彩迩文生化科技有限公司 抗凝血剂的制备方法、中间体及其制备方法
CN105348241B (zh) * 2015-12-11 2017-09-05 南京华威医药科技开发有限公司 一种硫酸沃拉帕沙中间体的合成方法
US11247940B2 (en) 2016-10-26 2022-02-15 The Regents Of The University Of California Efficient integration of manufacturing of upcycled concrete product into power plants
CN106749138B (zh) * 2016-12-07 2019-08-16 扬子江药业集团四川海蓉药业有限公司 一种硫酸沃拉帕沙中间体醛的制备方法
CN106866450B (zh) * 2017-01-13 2019-01-11 阜阳欣奕华材料科技有限公司 硫酸沃拉帕沙中间体的制备方法
CN108658910B (zh) * 2017-03-29 2020-11-03 北京新领先医药科技发展有限公司 一种沃拉帕沙中间体1-α的制备方法
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US11230473B2 (en) 2017-06-30 2022-01-25 The Regents Of The University Of California CO2 mineralization in produced and industrial effluent water by pH-swing carbonation
BR112020003106A2 (pt) 2017-08-14 2020-09-01 The Regents Of The University Of California métodos de fabricação e produtos de concreto
WO2019057946A1 (en) 2017-09-25 2019-03-28 F. Hoffmann-La Roche Ag MULTI-CYCLIC AROMATIC COMPOUNDS AS D-FACTOR INHIBITORS
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KR101026929B1 (ko) * 2002-04-16 2011-04-04 쉐링 코포레이션 트리사이클릭 트롬빈 수용체 길항제
ATE406366T1 (de) * 2004-05-28 2008-09-15 Schering Corp Gehinderte himbacinanaloga als thrombinrezeptorantagonisten
DK2206697T3 (da) 2005-01-14 2012-02-13 Schering Corp Exo- og diastereo-selektive synteser af himbacinanaloger
MX2007008622A (es) * 2005-01-14 2007-09-11 Schering Corp Una sintesis exo-selectiva de analogos de himbacina.
PT1853592E (pt) * 2005-01-14 2011-05-10 Schering Corp S?ntese de an?logos da himbacina
US7541471B2 (en) * 2005-01-14 2009-06-02 Schering Corporation Synthesis of himbacine analogs

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CA2875768A1 (en) 2006-07-20
ATE458726T1 (de) 2010-03-15
CY1112371T1 (el) 2015-12-09
US20060247450A1 (en) 2006-11-02
CA2875768C (en) 2018-03-06
PT2206697E (pt) 2012-01-10
JP5911447B2 (ja) 2016-04-27
US20090281321A1 (en) 2009-11-12
EP2196454B1 (en) 2014-08-27
CN102757423B (zh) 2016-04-20
CY1109896T1 (el) 2014-09-10
US20120296093A1 (en) 2012-11-22
RS52117B (en) 2012-08-31
EP2206697B1 (en) 2011-10-26
CN102757423A (zh) 2012-10-31
CA2594871C (en) 2015-04-07
CN101193880B (zh) 2012-08-22
DE602006012450D1 (de) 2010-04-08
CA2594871A1 (en) 2006-07-20
EP1848705B1 (en) 2010-02-24
WO2006076415A3 (en) 2006-11-16
MX2007008665A (es) 2008-03-04
US7989653B2 (en) 2011-08-02
SI1848705T1 (sl) 2010-06-30
EP1848705A2 (en) 2007-10-31
ES2374379T3 (es) 2012-02-16
JP5388231B2 (ja) 2014-01-15
AR056919A1 (es) 2007-11-07
PT1848705E (pt) 2010-05-10
JP2008526972A (ja) 2008-07-24
DK2206697T3 (da) 2012-02-13
HRP20100218T1 (hr) 2010-05-31
HRP20110963T1 (hr) 2012-01-31
ATE530516T1 (de) 2011-11-15
EP2206697A1 (en) 2010-07-14
US7605275B2 (en) 2009-10-20
EP2196468B1 (en) 2013-04-10
EP2196454A2 (en) 2010-06-16
EP2196468A1 (en) 2010-06-16
SI2206697T1 (sl) 2012-02-29
US8258319B2 (en) 2012-09-04
JP2011098967A (ja) 2011-05-19
RS51315B (sr) 2010-12-31
JP4681616B2 (ja) 2011-05-11
CN101193880A (zh) 2008-06-04
JP2013177407A (ja) 2013-09-09
US20110251392A1 (en) 2011-10-13
ES2339696T3 (es) 2010-05-24
ME01967B (me) 2012-08-31
DK1848705T3 (da) 2010-06-14
SG158888A1 (en) 2010-02-26
PL2206697T3 (pl) 2012-03-30
SG192505A1 (en) 2013-08-30
ZA200706711B (en) 2014-01-29
ES2412981T3 (es) 2013-07-15
PL1848705T3 (pl) 2010-07-30
WO2006076415A2 (en) 2006-07-20
US8618314B2 (en) 2013-12-31
EP2196454A3 (en) 2010-09-22

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