专利摘要:
METHOD OF OBTAINING 6 7-DICHLOR-1, 5-DIHYDROIMIDAZO
公开号:SU1120923A3
申请号:SU792751007
申请日:1979-04-09
公开日:1984-10-23
发明作者:Эндрю Дженкс Томас;Нейл Биверунг Уоррен (Младший);Энтони Партика Ричард
申请人:Бристоль Мейерз Компани (Фирма);
IPC主号:
专利说明:

31
A mixture containing hydrobromic ethid-5,6-dichloro-dihydro-2 (1H) -iminochinazolin-3-acetate 6 g (0.043 mol), absolute ethanol (2.8 ml and triethylamine 0.66 ml (0.004 mol), heated The mixture is cooled and removed by decantation of ethanol as possible. The solid is then suspended in freshly prepared absolute ethanol and, after stirring the mixture for 0.5 h, filtered. The solid is then suspended in a mixture of absolute ethanol ( 3.8 ml) and 95% ethanol (15 ml) and heated under reflux in t chenie 4 hours. The warm mixture was filtered. The solid suschat. under vacuum (0.5-1 mm Hg) over phosphorus pentoxide. A 1.45 g (92%) of product
09234
as a solid ivory.
IR peaks: 1702 (weak), 1638, 1554, 1468 and 1440
5 NMR peaks (TFA): S 7.33 (AB, q, .2H)
4.97 (S, 2H) and 4.59 (S, 2H).
The compounds of formula III have the same structural formula, however, the compound of formula III can exist 10 also in tautomeric form Ilia:
N. ,, NH-HBr
T. about
N II
dHgdodgHs
Moreover, both tautomeric forms, i.e. 20 III and Ilia, when treated with a base, give the required product of formula 1.
权利要求:
Claims (2)
[1]
METHOD FOR PRODUCING 6,7-Dichloro-1,5-dihydroimidazo (2,1-b) quinazoline
[2]
2 (ZN) -0 ON FORMULAS,
Cl comprising the interaction of a compound of the formula with bromine in .kn 2 z o 'CH 2 LNSN 2 С0С g Н5 organic solvent, characterized in that, in order to increase the yield of the target product, toluene and the resulting compound of the formula w NH- are used as an organic solvent HBr
Υ θ
L ΑΛΑ II
Ct γ Sn 2 Cos 2 n 5
Cl is reacted with an equimolar amount of an organic base, for example triethylamine, in ethanol while heating. to the reflux temperature of the solvent.
SU ,,,, 1120923 t 1
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同族专利:
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引用文献:
公开号 | 申请日 | 公开日 | 申请人 | 专利标题

BE794964A|1972-02-04|1973-08-02|Bristol Myers Co|NEW HYPOTENSING AGENTS AND METHOD FOR PREPARING THEM|
US3932407A|1973-11-19|1976-01-13|Bristol-Myers Company|Optionally substituted 1,2,3,5-tetrahydroimidezo-quinazolin-2-ones and 6-1,2,3,4-tetrahydropyimidoquinazolin-2-ones|
US3988340A|1975-01-23|1976-10-26|Bristol-Myers Company|6-Alkoxymethyl-1,2,3,5-tetrahydroimidazo[2,1-b]quinazolin-2-ones and 7-alkoxymethyl-6-[H]-1,2,3,4-tetrahydropyrimido[2,1-b]quinazolin-2-ones|
NL7807507A|1977-07-25|1979-01-29|Hoffmann La Roche|TRICYCLICAL CONNECTIONS.|CA1131631A|1979-06-20|1982-09-14|Madhukar S. Chodnekar|Quinazoline derivatives and pharmaceuticalpreparations|
US4818273A|1983-11-14|1989-04-04|The Dow Chemical Company|Substituted 1,2,4-triazolo[1,5-a]pyrimidine-2-sulfonamides, compositions containing them, and their utility as herbicides|
US4837239A|1985-08-23|1989-06-06|SyntexInc.|Cardiotonic phosphodiesterase inhibitors complexed with water soluble vitamins|
US4761416A|1986-07-25|1988-08-02|SyntexInc.|N-N-disubstituted-ω-[2-amino-3--3, 4-dihydroquinazolinyl]oxyalkylamides and related compounds|
US4739056A|1986-11-26|1988-04-19|SyntexInc.|N-N-disubstituted-omega--3,4-dihydroquinazolinyl)oxy-alkylamides and related compounds|
JPH05271200A|1991-05-22|1993-10-19|Egyt Gyogyszervegyeszeti Gyar|Production of 6,7-dichloro-1,5-dihydro-imidazoquinazolin-2-one|
US5391737A|1991-05-22|1995-02-21|Egis Gyogyszergyar|Process for the preparation of 6,7-dichloro-1,5-dihydroimidazo[2,1-b]quinazolin-2[3H]-one|
US5776962A|1994-08-03|1998-07-07|Cell Pathways, Inc.|Lactone compounds for treating patient with precancerous lesions|
US5696159A|1994-08-03|1997-12-09|Cell Pathways, Inc.|Lactone compounds for treating patients with precancerous lesions|
US6060477A|1995-06-07|2000-05-09|Cell Pathways, Inc.|Method of treating a patient having precancerous lesions with phenyl cycloamino pyrimidinone derivatives|
US6046216A|1995-06-07|2000-04-04|Cell Pathways, Inc.|Method of treating a patient having precancerous lesions with phenyl pyridinone derivatives|
US6232312B1|1995-06-07|2001-05-15|Cell Pathways, Inc.|Method for treating patient having precancerous lesions with a combination of pyrimidopyrimidine derivatives and esters and amides of substituted indenyl acetic acides|
US6200980B1|1995-06-07|2001-03-13|Cell Pathways, Inc.|Method of treating a patient having precancerous lesions with phenyl purinone derivatives|
US5874440A|1995-06-07|1999-02-23|Cell Pathways, Inc.|Method of treating a patient having precancerous lesions with phenyl pyrimidinone derivatives|
US6262059B1|1995-06-07|2001-07-17|Cell Pathways, Inc.|Method of treating a patient having precancerous lesions with quinazoline derivatives|
US6046206A|1995-06-07|2000-04-04|Cell Pathways, Inc.|Method of treating a patient having a precancerous lesions with amide quinazoline derivatives|
CA2171073A1|1995-12-04|1997-06-05|Philip C. Lang|Process for the preparation of ethyl-n- glycine|
CA2238283C|1997-05-30|2002-08-20|Cell Pathways, Inc.|Method for identifying compounds for inhibition of neoplastic lesions, pharmaceutical compositions from such compounds and uses of such compounds and compositions for treating neoplastic lesions|
US5858694A|1997-05-30|1999-01-12|Cell Pathways, Inc.|Method for identifying compounds for inhibition of cancerous lesions|
US5852035A|1997-12-12|1998-12-22|Cell Pathways, Inc.|Method for inhibiting neoplastic cells and related conditions by exposure to substituted N- arylmethyl and heterocyclmethyl-1H-pyrazoloquinolin-4-amines|
US6046199A|1998-01-14|2000-04-04|Cell Pathways, Inc.|Method of inhibiting neoplastic cells with tetracyclic pyrido[3,4-B]indole derivatives|
US6410584B1|1998-01-14|2002-06-25|Cell Pathways, Inc.|Method for inhibiting neoplastic cells with indole derivatives|
US5942520A|1998-01-27|1999-08-24|Cell Pathways, Inc.|Method for inhibiting neoplastic cells by exposure to substituted N-cycloalkylmethyl-1-H-pyrazoloquinolone-4 amines|
US5990117A|1998-04-15|1999-11-23|Cell Pathways, Inc.|Method for inhibiting neoplastic cells and related conditions by exposure to quinazoline derivatives|
US6180629B1|1998-08-14|2001-01-30|Cell Pathways, Inc.|[4,5]-Fused-1,3-disubstituted-1,2-diazine-6-one derivatives with nitrogen containing substitutents in position one for the treatment of neoplasia|
US6268372B1|1998-09-11|2001-07-31|Cell Pathways, Inc.|Method for inhibiting neoplastic cells and related conditions by exposure to 2,9-disubstituted purin-6-ones|
US6124303A|1998-09-11|2000-09-26|Cell Pathways, Inc.|Method for inhibiting neoplastic cells and related conditions by exposure to 9-substituted 2- purin-6-ones|
US6200771B1|1998-10-15|2001-03-13|Cell Pathways, Inc.|Method of using a novel phosphodiesterase in pharmaceutical screeing to identify compounds for treatment of neoplasia|
US6187779B1|1998-11-20|2001-02-13|Cell Pathways, Inc.|Method for inhibiting neoplastic cells and related conditions by exposure to 2,8-disubstituted quinazoline derivatives|
US6369092B1|1998-11-23|2002-04-09|Cell Pathways, Inc.|Method for treating neoplasia by exposure to substituted benzimidazole derivatives|
US6486155B1|1998-11-24|2002-11-26|Cell Pathways Inc|Method of inhibiting neoplastic cells with isoquinoline derivatives|
US6034099A|1998-11-24|2000-03-07|Cell Pathways, Inc.|Method for inhibiting neoplastic lesions by administering 4-- 2, 3- dihydro-pyrazol-3-ones|
US6077842A|1998-11-24|2000-06-20|Cell Pathways, Inc.|Method of inhibiting neoplastic cells with pyrazolopyridylpyridazinone derivatives|
US6025394A|1999-01-29|2000-02-15|Cell Pathways, Inc.|Method for treating patients with acne by administering substituted sulfonyl indenyl acetic acids, amides and alcohols|
US6020379A|1999-02-19|2000-02-01|Cell Pathways, Inc.|Position 7 substituted indenyl-3-acetic acid derivatives and amides thereof for the treatment of neoplasia|
US6130053A|1999-08-03|2000-10-10|Cell Pathways, Inc.|Method for selecting compounds for inhibition of neoplastic lesions|
EP1216037A2|1999-09-21|2002-06-26|Emory University|Methods and compositions for treating platelet-related disorders using mpl pathway inhibitory agents|
US6194420B1|1999-11-30|2001-02-27|Roberts Laboratories Inc.|2-amino-5,6-dichloro-3,4-dihydroquinazoline, its method of making and using and pharmaceutical compositions thereof|
US6555547B1|2000-02-28|2003-04-29|Cell Pathways, Inc.|Method for treating a patient with neoplasia by treatment with a vinca alkaloid derivative|
US6569638B1|2000-03-03|2003-05-27|Cell Pathways, Inc|Method for screening compounds for the treatment of neoplasia|
US6388073B1|2000-07-26|2002-05-14|Shire Us Inc.|Method for the manufacture of anagrelide|
DE10301105B4|2003-01-09|2005-11-24|Chemisch-Pharmazeutisches Labor, Rolf Sachse Gmbh|Use of 2-amino-2H-quinazoline derivatives for the treatment of myeloproliferative disorders, hypertension and bronchodilation|
DE602004026405D1|2003-01-23|2010-05-20|Shire Holdings Ag|FORMULATION AND METHOD FOR THE TREATMENT OF THROMBOCYTHEMIA|
AT412873B|2004-02-20|2005-08-25|Aop Orphan Pharmaceuticals Ag|Preparation of anagrelide hydrochloride, useful for thrombocyte suppression, using 2,3-dichlorobenzaldehyde as starting material, avoids use of toxic reagents|
US20060030574A1|2004-08-04|2006-02-09|Shire Holdings Ag|Quinazoline derivatives useful for the treatment of peripheral arterial disease and as phosphodiesterase inhibitors|
US7700608B2|2004-08-04|2010-04-20|Shire Holdings Ag|Quinazoline derivatives and their use in the treatment of thrombocythemia|
WO2007025177A2|2005-08-26|2007-03-01|Braincells, Inc.|Neurogenesis by muscarinic receptor modulation|
EP2258357A3|2005-08-26|2011-04-06|Braincells, Inc.|Neurogenesis with acetylcholinesterase inhibitor|
WO2007134136A2|2006-05-09|2007-11-22|Braincells, Inc.|Neurogenesis by modulating angiotensin|
CA2625153A1|2005-10-21|2007-04-26|Braincells, Inc.|Modulation of neurogenesis by pde inhibition|
EP1942879A1|2005-10-31|2008-07-16|Braincells, Inc.|Gaba receptor mediated modulation of neurogenesis|
US20100216734A1|2006-03-08|2010-08-26|Braincells, Inc.|Modulation of neurogenesis by nootropic agents|
WO2007104035A1|2006-03-08|2007-09-13|Braincells, Inc.|Modulation of neurogenesis by nootropic agents|
US20100009983A1|2006-05-09|2010-01-14|Braincells, Inc.|5 ht receptor mediated neurogenesis|
EP2026813A2|2006-05-09|2009-02-25|Braincells, Inc.|5 ht receptor mediated neurogenesis|
US7998971B2|2006-09-08|2011-08-16|Braincells Inc.|Combinations containing a 4-acylaminopyridine derivative|
US20100184806A1|2006-09-19|2010-07-22|Braincells, Inc.|Modulation of neurogenesis by ppar agents|
CA2663347A1|2006-09-19|2008-03-27|Braincells, Inc.|Ppar mediated modulation of neurogenesis|
GB0623749D0|2006-11-28|2007-01-10|Shire Llc|Substituted quinazolines|
US7910597B2|2006-11-28|2011-03-22|Shire Llc|Substituted quinazolines|
US8304420B2|2006-11-28|2012-11-06|Shire Llc|Substituted quinazolines for reducing platelet count|
AR064106A1|2006-12-05|2009-03-11|Bayer Schering Pharma Ag|DERIVATIVES OF 2,3-DIHYDROIMIDAZO [1,2-C] SUBSTITUTED QUINAZOLINE USEFUL FOR THE TREATMENT OF HYPER-PROLIFERATIVE DISEASES ASSOCIATED WITH ANGIOGENESIS|
EP2114856A1|2007-02-06|2009-11-11|Cipla Limited|Process for the preparation of ethyl-n- glycine hydrochloride|
CN101463035A|2007-12-19|2009-06-24|华生制药私人有限公司|Improved method for producing anagrelide hydrochloride monohydrate|
GB0808944D0|2008-05-16|2008-06-25|Shire Llc|Substituted quinazolines|
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GB0808951D0|2008-05-16|2008-06-25|Shire Llc|Substituted quinazolines|
GB0808947D0|2008-05-16|2008-06-25|Shire Llc|Substituted quinazolines|
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US20100216805A1|2009-02-25|2010-08-26|Braincells, Inc.|Modulation of neurogenesis using d-cycloserine combinations|
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法律状态:
优先权:
申请号 | 申请日 | 专利标题
US05/894,464|US4146718A|1978-04-10|1978-04-10|Alkyl 5,6-dichloro-3,4-dihydro-2-iminoquinazoline-3-acetate hydrohalides|
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