• 专利附录
  • 专利说明
  • 权利要求
  • 类似技术
  • 同族专利
  • 引用文献
  • 法律状态
  • 优先权
    • 专利摘要:
    An improved method is disclosed for producing antihypertensively active 6,7-dimethoxy-4-amino-2-[4-(2-furoyl)-1-piperazinyl] quinazoline hydrochloride, viz prazosine hydrochloride, by reacting methyl-N-(3,4-dimethoxy-6-cyano-phenyl)-[4-(2-furoyl)-1-piperazinyl]th ioformamidate with a large excess of ammonium chloride.
    公开号:SU900812A3
    申请号:SU802874898
    申请日:1980-01-30
    公开日:1982-01-23
    发明作者:Юхани Хонканен Эркки；Кюлликки Пиппури Айно；Юхани Каирисало Пекка；Талер Хейнрик；Катрина Коивисто Майя；Аннели Туоми Сирпа
    申请人:Орион-Ихтюмя Ой (Фирма)；
    IPC主号:
    专利说明:

    (54) METHOD FOR OBTAINING HYDROCHLORIDE 6,7-D№1ETOXI-4-AMINO-2-G4- (2-FUROSH1) -1-SHSHERASINIL-CHINOLASOLNA
    one
    This invention relates to a new process for the preparation of 6,7-dimethoxy-4-amino-2-C4- (2-furoyl) -1-pinperazine-quinosoline hydrochloride
     Vr - -lLlit)

    which has antihypertensive CIM action, and can be used in medicine.
    A known method for the preparation of 6,7-dimethoxy-4-amino-2-14- (2-furoyl) -1-piperazinyl-quinazoline hydrochloride, of the formula I, comprising the compound of the formula
    SISO
    (1a)

    where Q is a cyanogroup or a -C (-NH) -NH4 group or its salt, is subjected to
    interaction with piperazine formula
    , 0
    /
    A-S V1-W-J I5)
    where AC (NH) -0-CjHj-group,
    at 50-180 s, in the presence of the main catalyst Ul
    ten
     The disadvantage of this method is the complexity of the process technology, as well as the complexity of cleaning 15 of the target product.
    The purpose of the invention is to simplify the process.
    The goal is achieved
    20 of the proposed method for the preparation of a compound of formula I, namely, that intramolecular shorting of methyl-N- (3,4-dimethoxy-6
    权利要求:
    Claims (2)
    [1]
    SUMMARY OF THE INVENTION I. Method for the preparation of 6,7-dimethoxy-4-amino 2-G4- (2-furoyl) -1-piperazinyl] -quinazoline hydrochloride of the formula I of the formula in that in order to simplify the process, an intramolecular circuit of methyl N- (3,4-dimethoxy-6-cyanophenl) - [4- (2-furonl) -1-piperaznyl] thioformamcdate of the formula It is carried out
    M with 30-40 mol of ammonium chloride in formamide at 100-140 e C.
    [2]
    ‘2. The method according to η.I, with the fact that the process is carried out at 120 ° C for 15-20 hours
    类似技术:
    公开号 | 公开日 | 专利标题
    TR200003632T2|2001-04-20|Benzothioepine-1,1-dioxide derivatives, method of production, drugs containing them.
    SU900812A3|1982-01-23|Process for producing 6,7-dimethoxy-4-amino-2-/4-|-1-piperazinyl/ quinazoline hydrochloride
    EA200401533A1|2005-06-30|METHOD OF OBTAINING ROSUVASTATIN
    TR200103352T2|2005-03-21|Kinase pyrolotriazine inhibitors
    TR200101160T2|2002-01-21|New esters derived from substituted phenylcyclohexyl compounds.
    JPH04261170A|1992-09-17|Quinazoline derivative and production thereof
    RU96118435A|1999-02-20|CHLORPYRIMIDINE INTERMEDIATE COMPOUNDS
    TR199800608A2|1998-10-21|Propanolamine derivatives, their method of production.
    JPH04243878A|1992-08-31|1-|-1h-indol-5-yl substituted carbamate
    RU93046065A|1996-02-27|METHOD OF OBTAINING DERIVATIVES OF PHYSOSTYGMINCARBAMATE
    US4522943A|1985-06-11|Chemical compounds
    JPS6019789A|1985-01-31|Imidazo|pyrimidine derivative
    US4526973A|1985-07-02|Chemical compounds
    CA2211646A1|1996-08-01|Substituted phenyl compounds as endothelin antagonists
    SE7413856L|1975-05-12|
    EP0146642A1|1985-07-03|Process for the preparation of 4-amino-6,7-dimethoxy-2-|-piperazin-1-yl)-quinazoline and its physiologically acceptable salt
    JPS5793977A|1982-06-11|Acylaminoquinazoline derivative and its preparation
    RU2678969C1|2019-02-05|Antiarrhythmic drug based on hybrid molecules of amlodipine with |acetic acid
    HU180041B|1983-01-28|Process for producing 2-bracket-4-furoyl-piperazinyl-bracket closed-4-amino-6,7-dimethoxy-quinasoline derivatives of blood pressure reducing activity
    Kitagawa et al.1974|Equilibrium Studies of 5-Substituted 4-Hydroxy-2-methylpyrimidines. I. The Ionization Constants in Aqueous Solution
    ES8604488A1|1986-02-01|Aralykyl | aralkyl amines for use as vasodilators and antihypertensives.
    EA200200733A1|2002-12-26|NEW HETEROARRYLIC DERIVATIVES, THEIR RECEIVING AND APPLICATION
    EP0399953A3|1992-01-08|Piperidine-triazine compounds for use as stabilizers for organic materials
    EP0172509A3|1988-01-07|Process for the preparation of optically active, substituted 1,4-dihydropyridines and their use as medicaments
    US4546188A|1985-10-08|Substituted 1,2-diaminocyclobutene-3,4-diones
    同族专利:
    公开号 | 公开日
    SE8000777L|1980-08-01|
    DE3002553A1|1980-08-07|
    YU5880A|1983-02-28|
    PL221684A1|1980-10-20|
    ATA19580A|1983-09-15|
    NO152298B|1985-05-28|
    US4271300A|1981-06-02|
    GB2041932A|1980-09-17|
    FI790320A|1980-08-01|
    CS214692B2|1982-05-28|
    SE430692B|1983-12-05|
    BE881297A|1980-05-16|
    FR2447920B1|1982-12-03|
    DK158352C|1990-10-08|
    NL8000289A|1980-08-04|
    YU41498B|1987-08-31|
    NO794279L|1980-08-01|
    DK158352B|1990-05-07|
    NL190701C|1994-07-01|
    HU181016B|1983-05-30|
    DE3002553C2|1988-10-27|
    NO152298C|1985-09-04|
    NL190701B|1994-02-01|
    PL126994B1|1983-09-30|
    JPS6310955B2|1988-03-10|
    DD148952A1|1981-06-17|
    GB2041932B|1982-10-27|
    DK42680A|1980-08-01|
    ZA80501B|1981-02-25|
    JPS55104280A|1980-08-09|
    AT374475B|1984-04-25|
    FI67699B|1985-01-31|
    FR2447920A1|1980-08-29|
    CA1128945A|1982-08-03|
    CH644605A5|1984-08-15|
    FI67699C|1985-05-10|
    引用文献:
    公开号 | 申请日 | 公开日 | 申请人 | 专利标题
    US3511836A|1967-12-13|1970-05-12|Pfizer & Co C|2,4,6,7-tetra substituted quinazolines|
    GB1390014A|1971-05-07|1975-04-09|Koninklijke Pharma Fab Nv|Process for the preparation of carbocyclic fused pyrimidinederivatives|
    US3935213A|1973-12-05|1976-01-27|Pfizer Inc.|Process for hypotensive 4-amino-2- quinazoline derivatives|
    US4092315A|1976-03-01|1978-05-30|Pfizer Inc.|Novel crystalline forms of prazosin hydrochloride|
    FI58124C|1976-12-15|1980-12-10|Orion Yhtymae Oy|NY MELLANPROTUKT 3,4-DIMETOXY-6- -1-PIPERAZINYLTHOUREA) -BENONITRIL FOR FRAMSTAELLNING AV 6,7-DIMETOXY-4-AMINO-2- -1 -PIPERAZINYL) QUINAZOLINE WITH BLODTRYCKSSAENKANDE VERKAN|
    FI58125C|1976-12-15|1985-01-02|Orion Yhtymae Oy|PROCEDURE FOR FRAMSTATING AV 6,7-DIMETOXY-4-AMINO-2- -1-PIPERAZINYL) QUINAZOLINE WITH BLODTRYCKSSAENKANDE VEKAN|FI70411C|1980-12-29|1986-09-19|Pfizer|FORM OF ANTHYPERTENSIVE 4-AMINO-6,7-DIMETOXY-2-PIPERAZINOQUINAZOLE DERIVATIVES|
    FI79107C|1984-06-25|1989-11-10|Orion Yhtymae Oy|Process for the preparation of stable form of prazosin hydrochloride.|
    US4601897A|1985-11-06|1986-07-22|Pfizer Inc.|Prazosin-pirbuterol combination for bronchodilation|
    AT384218B|1985-12-04|1987-10-12|Gerot Pharmazeutika|METHOD FOR PRODUCING NEW CHINAZOLINE DERIVATIVES|
    YU70890A|1989-04-21|1992-05-28|Egyt Gyogyszervegyeszeti Gyar|Process for obtaining quinazoline derivatives|
    CA2077252C|1992-08-31|2001-04-10|Khashayar Karimian|Methods of making ureas and guanidines, and intermediates therefor|
    法律状态:
    优先权:
    申请号 | 申请日 | 专利标题
    FI790320A|FI67699C|1979-01-31|1979-01-31|PROCEDURE FOR THE FRAMSTATION OF AV 6,7-DIMETOXY-4-AMINO-2--1-PIPERAZINYL) QUINAZOLINE HYDROCHLORIDE WITH BLODTRYCKSSAENKANDE VERKAN|
    [返回顶部]