SG11201407043PA - Method for the preparation of triazole compounds - Google Patents

Method for the preparation of triazole compounds

Info

Publication number
SG11201407043PA
SG11201407043PA SG11201407043PA SG11201407043PA SG11201407043PA SG 11201407043P A SG11201407043P A SG 11201407043PA SG 11201407043P A SG11201407043P A SG 11201407043PA SG 11201407043P A SG11201407043P A SG 11201407043PA SG 11201407043P A SG11201407043P A SG 11201407043PA
Authority
SG
Singapore
Prior art keywords
triazol
morpholin
keto
enol
internationales
Prior art date
Application number
SG11201407043PA
Inventor
Hans-Christian Militzer
Johannes Eggert
Original Assignee
Bayer Pharma AG
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=48325714&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=SG11201407043P(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Bayer Pharma AG filed Critical Bayer Pharma AG
Publication of SG11201407043PA publication Critical patent/SG11201407043PA/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three 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, directly attached to ring carbon atoms
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/42One nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/041,2,3-Triazoles; Hydrogenated 1,2,3-triazoles

Abstract

(12) NACH DEM VERTRAG UBER DIE INTERNATIONALE ZUSAMMENARBEIT AUF DEM GEBIET DES PATENTWESENS (PCT) VEROFFENTLICHTE INTERNATIONALE ANMELDUNG (19) Weltorganisation fiir geistiges Eigentum Internationales Biiro _ (10) Internationale Veroffentlichungsnummer (43) Internationales Veroffentlichungsdatum 14. November 2013 (14.11.2013) WIPOIPCT WO 2013/167552 A1 (51) Internationale Patentklassifikation: C07D 403/14 (2006.01) C07D 249/04 (2006.01) (21) Internationales Aktenzeichen: (22) Internationales Anmeldedatum: (25) Einreichungssprache: (26) Veroffentlichungssprache: PCT/EP2013/059418 6. Mai 2013 (06.05.2013) Deutsch Deutsch (30) Angaben zur Prioritat: 12167152.3 8. Mai 2012 (08.05.2012) EP (71) Anmelder: BAYER PHARMA AKTIENGESELLSCHAFT [DE/DE]; Mullerstr. 178, 13353 Berlin (DE). (72) Erflnder: MILITZER, Hans-Christian; Waldweg 2, 51519 Odenthal (DE). EGGERT, Johannes; Johann- Sebastian-Bach-Str. 64, 61250 Usingen (DE). (74) Anwalt: BIP PATENTS; c/o Bayer Intellectual Property — GmbH, Creative Campus Monheim, Alfred-Nobel-Str. 10, 40789 Monheim (DE). (81) Bestimmungsstaaten (soweit nicht anders angegeben, fiir jede verfiigbare nationale Schutzrechtsart): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (84) Bestimmungsstaaten (soweit nicht anders angegeben, fiir jede verfiigbare regionale Schutzrechtsart)'. ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW), eurasisches (AM, AZ, BY, KG, KZ, RU, TJ, TM), europaisches (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG). Erklarungen gemaB Regel 4.17 : hinsichtlich der Berechtigung des Anmelders, ein Patent zu beantragen und zu erhalten (Regel 4.17 Ziffer ii) Veroffentlicht: — mit internationalem Recherchenbericht (Artikel 21 Absatz V (54) Title: METHOD FOR THE PREPARATION OF TRIAZOLE COMPOUNDS (54) Bezeichnung : VERFAHREN ZUR HERSTELLUNG VON TRIAZOL-VERBINDUNGEN (') AA Keto-Form BB Enol-Form CJ i> i-H cn i-H o CJ o & AA Keto form BB Enol form (57) Abstract: The present invention relates to a method for the preparation of l-[ 6-(morpholino-4-yl)-pyrimidino-4-yl]-4-(lH- l,2,3-triazolo-l-yl)-lH-pyrazolo-5-ol (I - enol form) or 2-[6-(morpholino-4-yl)-pyrimidino-4-yl]-4-(lH-l,2,3-triazolo-l-yl)-l,2- dihydro-3H-pyrazolo-3-one (I - keto form) and sodium-l-[6-(morpholino-4-yl)-pyrimidino-4-yl]-4-(lH-l,2,3-triazolo-l-yl)-lH- pyrazolo-5-olate (II) starting from 1, 2,3-triazole (HI), methylbromoacetate (IV-Me-Br) or ethylbromoacetate (IV-Et-Br), 4,6- dichloropyrimidine (VIII), morpholine (IX) and hydrazine (XII). (57) Zusammenfassung: Die vorliegende Erfmdung betrifft ein Verfahren zur Herstellung von l-[6-(Morpholin-4-yl)pyrimidin-4- yl]-4-(lH-l,2,3-triazol-l-yl)-lH-pyrazol-5-ol (I - Enol-Form) bzw. 2-[6-(Morpholin-4-yl)pyrimidin-4-yl]-4-(lH-l,2,3-triazol-l-yl)- l,2-dihydro-3H-pyrazol-3-on (I - Keto-Form) und Natrium-l-[6-(morpholin-4-yl)pyrimidin-4-yl]-4-(lH-l,2,3-triazol-l-yl)-lH- pyrazol-5-olat (II) ausgehend vonl,2,3-Triazol (HI), Bromessigsauremethylester (IV-Me-Br) oder Bromessigsaureethylester (IV-Et- Br), 4,6-Dichlorpyrimidin (VIII), Morpholin (IX) und Hydrazin (XII).
SG11201407043PA 2012-05-08 2013-05-06 Method for the preparation of triazole compounds SG11201407043PA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP12167152 2012-05-08
PCT/EP2013/059418 WO2013167552A1 (en) 2012-05-08 2013-05-06 Method for the preparation of triazole compounds

Publications (1)

Publication Number Publication Date
SG11201407043PA true SG11201407043PA (en) 2014-12-30

Family

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SG10201609319YA SG10201609319YA (en) 2012-05-08 2013-05-06 Method for the preparation of triazole compounds

Family Applications After (1)

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Country Status (36)

Country Link
US (1) US10301289B2 (en)
EP (1) EP2847183B1 (en)
JP (1) JP6149104B2 (en)
KR (1) KR102086389B1 (en)
CN (1) CN104411704B (en)
AP (1) AP2014008089A0 (en)
AU (1) AU2013258107B2 (en)
BR (1) BR112014027564B1 (en)
CA (1) CA2872726C (en)
CL (2) CL2014003003A1 (en)
CO (1) CO7121324A2 (en)
CR (1) CR20140514A (en)
CU (1) CU20140128A7 (en)
DK (1) DK2847183T3 (en)
DO (1) DOP2014000254A (en)
EA (1) EA027804B1 (en)
ES (1) ES2641205T3 (en)
HK (1) HK1208027A1 (en)
HR (1) HRP20171321T1 (en)
HU (1) HUE034430T2 (en)
IL (1) IL235441A (en)
LT (1) LT2847183T (en)
MX (1) MX350519B (en)
MY (1) MY184577A (en)
NZ (1) NZ701661A (en)
PE (1) PE20142453A1 (en)
PH (1) PH12014502482A1 (en)
PL (1) PL2847183T3 (en)
PT (1) PT2847183T (en)
RS (1) RS56255B1 (en)
SG (2) SG11201407043PA (en)
SI (1) SI2847183T1 (en)
TN (1) TN2014000469A1 (en)
UA (1) UA116349C2 (en)
WO (1) WO2013167552A1 (en)
ZA (1) ZA201408571B (en)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2017259872B2 (en) * 2016-05-03 2021-06-24 Bayer Pharma Aktiengesellschaft Method for producing 5-hydroxyalkyl-substituted 1-phenyl-1,2,4- triazole derivatives
CN108084099B (en) * 2017-12-20 2019-01-29 天驰药业有限公司 A kind of synthetic method of 1,2,3- 3-triazole compounds
US10702525B1 (en) 2019-09-04 2020-07-07 United Arab Emirates University Pyrimidine derivatives as anti-diabetic agents
EP3888684A1 (en) 2020-03-31 2021-10-06 Bayer Animal Health GmbH Composition having improved voluntary acceptance
CN114264752B (en) * 2021-12-29 2023-08-15 北京金城泰尔制药有限公司 Detection method of methyl bromoacetate

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DK135184A (en) 1983-03-03 1984-10-10 Riker Laboratories Inc TRIAZOL (4.3-C) - AND TRIAZOL (1.5-C) PYRIMIDINES
US4572910A (en) * 1983-03-03 1986-02-25 Riker Laboratories, Inc. Triazolo[1,5-c]pyrimidines substituted by nitrogen-containing heterocyclic rings
US4752910A (en) 1984-10-30 1988-06-21 Prime Computer, Inc. Method and apparatus for continuous after-imaging
UY27813A1 (en) * 2002-05-31 2003-12-31 Smithkline Beecham Corp PEPTIDE-DISFORMILASE INHIBITORS
AR042052A1 (en) 2002-11-15 2005-06-08 Vertex Pharma USEFUL DIAMINOTRIAZOLS AS INHIBITORS OF PROTEINQUINASES
WO2005044785A1 (en) * 2003-10-30 2005-05-19 Merck & Co., Inc. Aralkyl amines as cannabinoid receptor modulators
US7745630B2 (en) 2003-12-22 2010-06-29 Justin Stephen Bryans Triazolyl piperidine arginine vasopressin receptor modulators
DE102008020113A1 (en) * 2008-04-23 2009-10-29 Bayer Schering Pharma Aktiengesellschaft Substituted dihydropyrazolones and their use
CA2605899C (en) 2005-04-26 2011-02-08 Pfizer Limited Triazole derivatives as vasopressin antagonists
EP1885713A1 (en) 2005-05-18 2008-02-13 Pfizer Limited 1, 2, 4 -triazole derivatives as vasopressin antagonists
DE102006050516A1 (en) * 2006-10-26 2008-04-30 Bayer Healthcare Ag New pyrazol-3-one compounds are hypoxia-inducible transcription factor-prolyl-4-hydroxylase inhibitors useful e.g. to treat and/or prophylaxis heart-circulation diseases, heart failure, anemia, chronic kidney diseases and renal failure
DE102010041236A1 (en) * 2010-09-23 2012-03-29 Osram Ag Optoelectronic semiconductor component
DE102010044131A1 (en) * 2010-11-18 2012-05-24 Bayer Schering Pharma Aktiengesellschaft Substituted sodium 1H-pyrazole-5-olate

Also Published As

Publication number Publication date
AU2013258107B2 (en) 2017-06-22
PE20142453A1 (en) 2015-01-17
ES2641205T3 (en) 2017-11-08
CU20140128A7 (en) 2015-03-30
CN104411704A (en) 2015-03-11
MX350519B (en) 2017-09-08
US20150087827A1 (en) 2015-03-26
CO7121324A2 (en) 2014-11-20
HUE034430T2 (en) 2018-02-28
DOP2014000254A (en) 2016-01-31
CR20140514A (en) 2014-12-02
CN104411704B (en) 2017-12-22
UA116349C2 (en) 2018-03-12
SI2847183T1 (en) 2017-10-30
HK1208027A1 (en) 2016-02-19
PL2847183T3 (en) 2017-11-30
US10301289B2 (en) 2019-05-28
CA2872726A1 (en) 2013-11-14
KR102086389B1 (en) 2020-03-09
KR20150018534A (en) 2015-02-23
SG10201609319YA (en) 2016-12-29
EP2847183B1 (en) 2017-06-21
AP2014008089A0 (en) 2014-11-30
HRP20171321T1 (en) 2017-10-20
AU2013258107A1 (en) 2014-11-27
PT2847183T (en) 2017-10-02
RS56255B1 (en) 2017-11-30
DK2847183T3 (en) 2017-10-02
BR112014027564A2 (en) 2017-08-22
TN2014000469A1 (en) 2016-03-30
PH12014502482A1 (en) 2015-01-12
CA2872726C (en) 2020-07-07
EP2847183A1 (en) 2015-03-18
CL2014003003A1 (en) 2015-02-13
WO2013167552A1 (en) 2013-11-14
LT2847183T (en) 2017-09-25
JP2015516403A (en) 2015-06-11
JP6149104B2 (en) 2017-06-14
IL235441A (en) 2017-09-28
EA027804B1 (en) 2017-09-29
BR112014027564B1 (en) 2022-05-03
CL2016001165A1 (en) 2016-12-02
EA201492032A1 (en) 2015-04-30
NZ701661A (en) 2016-08-26
MX2014013448A (en) 2014-12-08
MY184577A (en) 2021-04-06
ZA201408571B (en) 2016-03-30

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