公开(公告)号：US4376771A

公开(公告)日：1983-03-15

申请号：US224939

申请日：1981-01-14

申请人： Rolf Lebkuecher ,  Marco Thyes ,  Horst Koenig ,  Hans D. Lehmann ,  Josef Gries ,  Dieter Lenke ,  Johannes Kunze

发明人： Rolf Lebkuecher ,  Marco Thyes ,  Horst Koenig ,  Hans D. Lehmann ,  Josef Gries ,  Dieter Lenke ,  Johannes Kunze

IPC分类号： C07D237/00 ,  A61K31/50 ,  A61P7/02 ,  A61P9/12 ,  C07D237/04

CPC分类号： C07D237/04

摘要： 6-(p-Acylaminophenyl)-4,5-dihydropyridaz-3-ones of the formula I ##STR1## where R.sup.1 is hydrogen or alkyl of 1 to 3 carbon atoms and R.sup.2, if R.sup.1 is hydrogen, is halogen-substituted alkyl of 3 to 6 carbon atoms or .beta.-haloethyl or, if R.sup.1 is alkyl of 1 to 3 carbon atoms, is halogen-substituted alkyl of 1 to 6 carbon atoms, their manufacture, and therapeutic agents which contain, as the active ingredient, a compound of the formula I, where R.sup.2 may also be halomethyl or .alpha.-haloethyl if R.sup.1 is hydrogen. These compounds may be used as anti-hypertensive agents and for the prophylaxis and therapy of thromboembolic disorders.

摘要翻译： 其中R 1是氢或1至3个碳原子的烷基，R 2，如果R 1是氢，则是式I的6-（对酰氨基苯基）-4,5-二氢哒嗪-3-酮是卤素取代的烷基 3〜6个碳原子或β-卤代乙基，或者如果R1是1〜3个碳原子的烷基，则为1〜6个碳原子的卤素取代烷基，其制造方法和含有作为活性成分的 式I化合物，其中如果R 1是氢，R 2也可以是卤代甲基或α-卤代乙基。 这些化合物可以用作抗高血压药和预防和治疗血栓栓塞性疾病。

公开(公告)号：US4290960A

公开(公告)日：1981-09-22

申请号：US127467

申请日：1980-03-05

申请人： Karl-Heinz Ross ,  Christian Dudeck ,  Walter Himmele ,  Rolf Lebkuecher ,  Wolfgang Sauer

发明人： Karl-Heinz Ross ,  Christian Dudeck ,  Walter Himmele ,  Rolf Lebkuecher ,  Wolfgang Sauer

IPC分类号： C07D303/14 ,  C07D307/20 ,  C07D307/32 ,  C07D307/60

CPC分类号： C07D307/32 ,  C07D303/14 ,  C07D307/20 ,  C07D307/60

摘要： A process for the preparation of the sought-after scent 2,5-dimethyl-4-hydroxy-2,3-dihydrofuran-3-one, and novel intermediates for the preparation of this compound.2,5-Dimethyl-4-hydroxy-2,3-dihydrofuran-3-one is prepared by first epoxidizing hex-3-ene-2,5-diol in the liquid phase with hydrogen peroxide to give the novel compound 3,4-epoxy-hexane-2,5-diol, which at 40.degree.-280.degree. C. is converted, by means of a catalytic amount of an acid, to the novel compound 2,5-dimethyl-3,4-dihydroxy-tetrahydro-furan. The latter is dehydrogenated by means of oxygen over a silver catalyst or copper catalyst to give the nove compound 2,5-dimethyl-4-hydroxy-tetrahydrofuran-3-one, which is oxidized by means of bismuth oxide, in concentrated acetic acid solution, to give the desired compound 2,5-dimethyl-4-hydroxy-2,3-dihydrofuran-3-one.

摘要翻译： 制备所需香味2,5-二甲基-4-羟基-2,3-二氢呋喃-3-酮的方法，以及制备该化合物的新型中间体。 通过用过氧化氢在液相中首先环己化己-3-烯-2,5-二醇制备2,5-二甲基-4-羟基-2,3-二氢呋喃-3-酮，得到新化合物3,4 - 环氧己烷-2,5-二醇，其在40℃-280℃下通过催化量的酸转化为新化合物2,5-二甲基-3,4-二羟基 - 四氢 呋喃 后者通过氧气在银催化剂或铜催化剂上脱氢，得到通过氧化铋在浓缩乙酸溶液中氧化的化合物2,5-二甲基-4-羟基 - 四氢呋喃-3-酮 ，得到所需化合物2,5-二甲基-4-羟基-2,3-二氢呋喃-3-酮。