HRP20120605T1 - Postupci sinteze 9-supstituiranog minociklina - Google Patents

Postupci sinteze 9-supstituiranog minociklina Download PDF

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Publication number
HRP20120605T1
HRP20120605T1 HRP20120605AT HRP20120605T HRP20120605T1 HR P20120605 T1 HRP20120605 T1 HR P20120605T1 HR P20120605A T HRP20120605A T HR P20120605AT HR P20120605 T HRP20120605 T HR P20120605T HR P20120605 T1 HRP20120605 T1 HR P20120605T1
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Croatia
Prior art keywords
minocycline
conditions
substituted
substituted minocycline
compound
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HRP20120605AT
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English (en)
Inventor
Seyedi Farzaneh
Warchol Tadeusz
Grier Mark
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Paratek Pharmaceuticals
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Publication date
Application filed by Paratek Pharmaceuticals filed Critical Paratek Pharmaceuticals
Publication of HRP20120605T1 publication Critical patent/HRP20120605T1/hr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00Preparation of carboxylic acid amides
    • C07C231/12Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00Systems containing at least three condensed rings
    • C07C2603/02Ortho- or ortho- and peri-condensed systems
    • C07C2603/40Ortho- or ortho- and peri-condensed systems containing four condensed rings
    • C07C2603/42Ortho- or ortho- and peri-condensed systems containing four condensed rings containing only six-membered rings
    • C07C2603/44Naphthacenes; Hydrogenated naphthacenes

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (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)

Abstract

Postupak sinteze 9-supstituiranog minociklinskog spoja formule: ,naznačen time ®to se sastoji u: a) reakciji reaktivnog minociklinskog međuprodukta u odgovarajućim uvjetima s ugljičnim monoksidom, uz paladijski katalizator, silan i bazu, kako bi se dobilo 9-karbaldehidno supstituirani minociklinski spoj; ib) reakciji navedenog 9-karbaldehidno supstituiranog minociklinskog spoja iz koraka a), u uvjetima paladijem katalizirane kondenzacije, uvjetima hidrogenolize ili uvjetima reduktivne aminacije, kako bi se dobilo navedeni 9-supstituirani minociklinski spoj navedene formule. Patent sadr·i jo® 4 patentna zahtjeva.

Claims (5)

1. Postupak sinteze 9-supstituiranog minociklinskog spoja formule: [image] , naznačen time što se sastoji u: a) reakciji reaktivnog minociklinskog međuprodukta u odgovarajućim uvjetima s ugljičnim monoksidom, uz paladijski katalizator, silan i bazu, kako bi se dobilo 9-karbaldehidno supstituirani minociklinski spoj; i b) reakciji navedenog 9-karbaldehidno supstituiranog minociklinskog spoja iz koraka a), u uvjetima paladijem katalizirane kondenzacije, uvjetima hidrogenolize ili uvjetima reduktivne aminacije, kako bi se dobilo navedeni 9-supstituirani minociklinski spoj navedene formule.
2. Postupak u skladu s patentnim zahtjevom 1, naznačen time što je navedeni reaktivni minociklinski međuprodukt 9-halogenirani minociklinski međuprodukt.
3. Postupak u skladu s patentnim zahtjevom 2, naznačen time što je navedeni 9-halogenirani minociklinski međuprodukt 9-jod-supstituirani minociklinski međuprodukt, 9-klor-supstituirani minociklinski međuprodukt ili 9-brom-supstituirani minociklinski međuprodukt.
4. Postupak u skladu s patentnim zahtjevom 1, naznačen time što navedeni paladijski katalizator je PdCl2(tBu2PhP)2 [diklorobis(di-tert-butilfenilfosfin)paladij(II)] ili PdCl2(DPEPhos) [bis(difenilfosfinofenil)eterpaladijev(II) klorid].
5. Postupak u skladu s patentnim zahtjevom 1, naznačen time što se sastoji u reakciji navedenog 9-karbaldehidno supstituiranog minociklinskog spoja iz koraka a) u uvjetima reduktivne aminacije.
HRP20120605AT 2007-07-06 2012-07-23 Postupci sinteze 9-supstituiranog minociklina HRP20120605T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US94838507P 2007-07-06 2007-07-06
US6035108P 2008-06-10 2008-06-10
PCT/US2008/008355 WO2009009042A1 (en) 2007-07-06 2008-07-07 Methods for synthesizing substituted tetracycline compounds

Publications (1)

Publication Number Publication Date
HRP20120605T1 true HRP20120605T1 (hr) 2012-09-30

Family

ID=39926392

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20120605AT HRP20120605T1 (hr) 2007-07-06 2012-07-23 Postupci sinteze 9-supstituiranog minociklina

Country Status (18)

Country Link
US (2) US9522872B2 (hr)
EP (2) EP2176216B1 (hr)
JP (2) JP2010532759A (hr)
KR (1) KR20100042276A (hr)
CN (2) CN101811980A (hr)
AT (1) ATE555079T1 (hr)
AU (2) AU2008275701B2 (hr)
BR (2) BRPI0823405A2 (hr)
CA (1) CA2693376A1 (hr)
DK (1) DK2176216T3 (hr)
EA (2) EA201070233A1 (hr)
ES (1) ES2386926T3 (hr)
HK (1) HK1139386A1 (hr)
HR (1) HRP20120605T1 (hr)
IL (1) IL204133A0 (hr)
PT (1) PT2176216E (hr)
WO (1) WO2009009042A1 (hr)
ZA (2) ZA201000034B (hr)

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KR20100042276A (ko) 2010-04-23
ZA201000034B (en) 2011-10-26
HK1139386A1 (en) 2010-09-17
JP2011020996A (ja) 2011-02-03
CN101811980A (zh) 2010-08-25
JP2010532759A (ja) 2010-10-14
EP2176216B1 (en) 2012-04-25
ES2386926T3 (es) 2012-09-06
BRPI0823405A2 (pt) 2012-12-25
AU2008275701A1 (en) 2009-01-15
WO2009009042A1 (en) 2009-01-15
CA2693376A1 (en) 2009-01-15
EA201070048A1 (ru) 2010-10-29
BRPI0813990A2 (pt) 2011-09-13
EP2192111A3 (en) 2010-10-06
EP2176216A1 (en) 2010-04-21
ZA201008646B (en) 2012-02-29
US20090156842A1 (en) 2009-06-18
ATE555079T1 (de) 2012-05-15
DK2176216T3 (da) 2012-07-30
PT2176216E (pt) 2012-07-27
US20170283368A1 (en) 2017-10-05
AU2010200845A1 (en) 2010-04-01
US9522872B2 (en) 2016-12-20
CN101784517A (zh) 2010-07-21
EP2192111A2 (en) 2010-06-02
AU2008275701B2 (en) 2013-04-04
IL204133A0 (en) 2011-07-31
AU2010200845B2 (en) 2013-01-17
EA201070233A1 (ru) 2010-08-30

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