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    Synthesis of n-5-methyltetrahydrohomofolic acid and related reduced derivatives of homofolic acid
    3.
    发明授权
    Synthesis of n-5-methyltetrahydrohomofolic acid and related reduced derivatives of homofolic acid 失效
    合成N-5-甲基异烟酸和相关的还原型异烟酸衍生物

    公开(公告)号：US3870719A

    公开(公告)日：1975-03-11

    申请号：US26355972

    申请日：1972-06-16

    申请人： US HEALTH

    发明人： KNOTT ROGER L ,  TAUNTON-RIGBY ALISON

    IPC分类号： A61K31/505 ,  A61K31/519 ,  A61P35/02 ,  C07D475/04 ,  C07D487/14 ,  C07D51/48

    CPC分类号： C07D487/14 ,  C07D475/04 ,  Y10S514/908

    摘要： The preparation of N5-methyltetrahydrohomofolic acid and alkali metal salts thereof is from homofolic acid starting material (HFA) by catalytic reduction with platinum oxide in the dark under hydrogen at a slight overpressure to produce tetrahydrohomofolate (THHF), then immediately reacting this product with formaldehyde to produce 5,11methylenetetrahydrohomofolate and reducing this methylene intermediate without isolation with sodium borohydride to give the desired 5-methyltetrahydrohomofolate in the disodium salt form. The 5-methyl product is recovered by precipitating side products at a pH of about 3.8 with acetic acid and refrigerating the product filtrate overnight at about 3*-10*C. The filtrate containing the product 5-methyltetrahydrohomofolate (5-MeTHHF) is treated with charcoal, concentrated to an oil and the 5-methyl product is precipitated with absolute ethanol. The 5,11methylenetetrahydrofolate may be separately recovered and in a second reaction an additional product known as the 5,11-methenyl is formed by reaction with formic acid. These products show increased stability over folate analogues and show biological promise in the treatment of cancer and leukemia as antifolates and specifically against L1210-FR8 tumor in mice.

    摘要翻译： N5-甲基四氢异佛尔酮酸及其碱金属盐的制备通过在黑暗中在氧气中在氧气中在稍微超压下通过催化还原与氢氧化铝反应生成四氢异佛酸酯（THHF），然后立即使该产物与甲醛反应，由均聚酸原料（HFA） 生成5,11-亚甲基四氢异佛酸酯并且用硼氢化钠分离而还原该亚甲基中间体，得到所需的二钠盐形式的5-甲基四氢异佛酸酯。 通过用乙酸在约3.8的pH下沉淀副产物回收5-甲基产物，并将产物滤液在约3℃-10℃下冷冻过夜。将含有5-甲基四氢异佛酸酯（5-MeTHHF）的产物的滤液处理 用木炭，浓缩成油，用无水乙醇沉淀出5-甲基产物。 可以单独回收5,11-亚甲基四氢叶酸，在第二反应中，通过与甲酸反应形成称为5,11-亚甲基的另外的产物。 这些产品显示出比叶酸类似物更高的稳定性，并且在治疗作为抗叶酸剂的癌症和白血病以及特异性地针对小鼠中的L1210-FR8肿瘤方面表现出生物学上的前景。

    Bronchodilator 5,6-dihydro-tetrazolo(1,5-c) quinazolines
    6.
    发明授权
    Bronchodilator 5,6-dihydro-tetrazolo(1,5-c) quinazolines 失效
    二茂铁（5,6-DIHYDRO-TETRAZOLO）（1,5-C）喹唑啉

    公开(公告)号：US3835138A

    公开(公告)日：1974-09-10

    申请号：US29746772

    申请日：1972-10-13

    申请人： DOW CHEMICAL CO

    发明人： WAGNER E

    IPC分类号： C07D487/04 ,  C07D487/10 ,  C07D491/14 ,  C07D51/48

    CPC分类号： C07D487/04 ,  C07D487/10 ,  C07D491/14 ,  Y10S514/826

    摘要： Tetrazoloquinazoline compounds such as 5,6-dihydro-5-ethyl-8,9dimethoxy-5-methyl-tetrazolo(1,5-c)-quinazoline are prepared by the reaction of a 5-(2-aminophenyl)tetrazole with a ketone or aldehyde. The compounds are useful as bronchodilator agents.

    摘要翻译： 四氢喹唑啉化合物如5,6-二氢-5-乙基-8,9-二甲氧基-5-甲基 - 四唑（1,5-c） - 喹唑啉通过5-（2-氨基苯基）四唑与 酮或醛。 该化合物可用作支气管扩张剂。

    4-substituted-amino-quinazolines and nitrates thereof
    7.
    发明授权
    4-substituted-amino-quinazolines and nitrates thereof 失效
    4-取代的氨基喹啉及其硝酸酯

    公开(公告)号：US3833584A

    公开(公告)日：1974-09-03

    申请号：US16844671

    申请日：1971-08-02

    申请人： SANDOZ AG

    发明人： GABEL L ,  SIMPSON W

    IPC分类号： C07D491/04 ,  C07D51/48

    CPC分类号： C07D491/04 ,  Y10S514/929

    摘要： THE INVENTION DISCLOSED COMPOUNDS OF THE CLASS WHICH ARE NITRATES OF 4-SUBSTITUTED-AMINO-QUINAZOLINES, E.G., 4-(2HYDROXYETHYL)AMINO-6,7 - DIMETHOXYQUINAZOLINE NITRATE, HAVING PHARMACOLOGICAL ACTIVITY IN ANIMALS AND USEFUL, FOR EXAMPLE, AS HYPOTENSIVE AND ANTI-ANGINAL AGENTS. ALSO DISCLOSED, ARE THE HYDROXY INTERMEDIATES USEFUL IN PREPARATION OF SAID NITRATES.

    Certain 3 - (beta-carbethoxyethyl)- and 3 - (beta-carboxyethyl) - 4 -phenyl-3,4-dihydro-and 1,2,3,4-tetrahydro-quinazolines
    9.
    发明授权
    Certain 3 - (beta-carbethoxyethyl)- and 3 - (beta-carboxyethyl) - 4 -phenyl-3,4-dihydro-and 1,2,3,4-tetrahydro-quinazolines 失效
    某些3-（β-甲氧基乙基） - 和3-（β-羧基乙基）-4-苯基-3,4-二氢 - 和1,2,3,4-四氢喹啉酮

    公开(公告)号：US3741969A

    公开(公告)日：1973-06-26

    申请号：US3741969D

    申请日：1971-01-18

    申请人： SANDOZ AG

    发明人： OTT H

    IPC分类号： C07D239/74 ,  C07D245/06 ,  C07D51/48

    CPC分类号： C07D239/74 ,  C07D245/06

    摘要： THE INVENTION DISCLOSES COMPOUNDS OF THE CLASS OF 6PHENYL-3,4-DIHYDRO(1,5)BENZODIAZOCIN-2-(IH)-ONES USEFUL AS TRANQUILIZERS. ALSO DISCLOSED IS PREPARATION OF SAID COMPOUNDS FEATURING INTERMEDIATES WHICH ARE 1,5-METHANO-1, 5-BENZODIAZOCIN-2-ONES WHICH ARE CONVERTED BY ACID TREATMENT TO THE CORRESPONDING 6-PHENYL-3,4,5,6-TETRAHYDRO(1, 5)BENZODIAZOCIN-2-(1H)-ONES WHICH IN TURN MAY BE OXIDIZED TO OBTAIN THE FIRST-MENTIONED CLASS OF COMPOUNDS. THE BRIDGE INTERMEDIATES ARE PREPARED BY DEHYDRATION OF A 3-(B-CARBOXYETHYL)-4-PHENYL-1,2,3,4-TETRAHYDROQUINAZOLINE WHICH IS PREPARED BY REDUCTION OF A 3-(B-CARBOXYETHYL)-4-PHENYL-3,4-DIHYDROQUINAZOLINE WHICH IS PREPARED BY HYDROLYSIS OF A CORRESPONDING ESTER.

    Certain 3-(3-amino-2-benzoyloxypropyl)-4(3h)-quinazolinones
    10.
    发明授权
    Certain 3-(3-amino-2-benzoyloxypropyl)-4(3h)-quinazolinones 失效
    某些3-（3-氨基-2-苯甲酰基丙基）-4（3H） - 喹唑啉酮

    公开(公告)号：US3738985A

    公开(公告)日：1973-06-12

    申请号：US3738985D

    申请日：1971-04-22

    申请人： BEYERLE R ,  STACHEL A ,  STACHEL I ,  NITZ R ,  SCHOLTHOLT J

    发明人： BEYERLE R ,  STACHEL A ,  SCHOLTHOLT J ,  STACHEL I ,  NITZ R

    IPC分类号： C07D239/91 ,  C07D239/88 ,  C07D239/95 ,  C07D51/48

    CPC分类号： C07D239/88

    摘要： THE PRESENT INVENTION RELATES TO PHARMACEUTICALLY ACTIVE BASICALLY SUBSTITUTED 4(3H)-QUINAZOLINONE DERIVATIVES POSSESSING EXCELLENT CORONARY DILATOR PROPERTIES AND HAVING THE STRUCTURAL FORMULA

    4-(O=),3-((R3)M-C6H4-COO-CH(-CH2-R'')-CH2-),2-R1,(R2)N-

    3,4-DIHYDROQUINAZOLINE

    WHEREIN THE VARIOUS RADICALS HAVE THE ABOVE-GIVEN MEANINGS.

    OOC-C6H4-(R3)M

    R1-CO-NH-((R2)N-1,2-PHENYLENE)-CO-NH-CH2-CH(-CH2-R'')-

    OR A FUNCTIONAL DERIVATIVE THEREOF: OR, THE SAID DERIVATIVES MAY BE PRODUCED BY CYCLIZING, IN THE PRESENCE OF DEHYDRATING AGENTS, 2-ACYLAMINOBENZAMIDES HAVING THE STRUCTURAL FORMULA

    (R2)M-C6H4-COOH

    WHEREIN R2 AND M HAVE THE ABOVE-GIVEN MEANINGS, SAID R MAY ALSO REPRESENT THE RADICAL OF THE UNDERLYING HYDROXY COMPOUND, WITH AN ALKOXY BENZOIC ACID OF THE FORMULA

    (R2)M-C6H4-COO-

    WHEREIN R1, R2 AND N HAVE THE ABOVE-GIVEN MEANINGS, R IS IDENTICAL WITH R'', OR, IN CASE R'' CONTAINS AN ACYLOXY RADICAL OF THE STRUCTURAL FORMULA

    QUINAZOLINE

    4-(O=),3-(R-CH2-CH(-OH)-CH2-),2-R1,(R2)N-3,4-DIHYDRO-

    WHEREIN R'' STANDS FOR A RADICAL SELECTED FROM THE GROUP CONSISTING OF SECONDARY ALIPHATIC, CYCLOALIPHATIC OR ARALIPHATIC AMINES HAVING 2-10 CARBON ATOMS AND 5-, 6- OR 7MEMBERED HETEROCYCLIC NITROGEN BASES WHICH CONTAIN IN ADDITION TO THE NITROGEN ATOM A CORRESPONDING NUMBER OF METHYLENE GROUPS, AS WELL AS OPTIONALLY AN ADDITIONAL NITROGEN ATOM, AN O OR AN S ATOM, SAID RADICAL BEING BOUND, VIA A NITROGEN ATOM, R1 STANDS FOR HYDROGEN, AN ALKYL RADICAL HAVING FROM 1 TO 4 CARBON ATOMS, A PYRIDYL RADICAL, A BENZYL OR PHENYL RADICAL, THE TWO LATTER BEING OPTIONALLY SUBSTITUTED BY LOWER ALKYL, LOWER ALKOXY GROUPS OR HALOGEN, R2 REPRESENTS HYDROGEN, NITRO, AMINO, TRIFLUOROMETHYL OR LOWER ALKOXY GROUPS HAVING FROM 1 TO 4 CARBON ATOMS, R3 STANDS FOR ALKOXY HAVING FROM 1 TO 4 CARBON ATOMS, M MEANS ONE OF THE INTEGERS 1, 2 OR 3 AND N MEANS AN INTEGER FROM 1 TO 4, AND TO THE PRODUCTION OF SUCH DERIVATIVES BY ACYLATING, OPTIONALLY IN THE PRESENCE OF AN ACID-BINDING AGENT, 4(3H)-QUINAZOLINONES HAVING THE STRUCTURAL FORMULA