摘要:
A process for preparing a 2-carbamoyloxyalkyl-1,4-dihydropyridine derivative represented by the general formula: which comprises:
(a) reacting a 3-amino-3-carbamoyloxyalkylacrylic acid derivative represented by the general formula: with a benzylidene compound represented by the general formula:
(b) reacting the 3-amino-3-carbamoyloxyalkylacrylic acid derivative of the general formula II with an aldehyde comoound reoresented bv the aeneral formula: and a β-keto-ester compound represented by the general formula:
(c) reacting a 3-carbamoyloxyalkylpropiolic acid derivative represented by the general formula: with the benzylidene compound of the general formula III and ammonia or its salt: or (d) reacting the 3-carbamoyloxyalkylpropiolic acid derivative of the general formula VI with the aldehyde compound of the general formula IV, the β-keto-ester compound of the general formula V and ammonia or its salt, and the intermediates of formula II and VI.
摘要:
Novel 1,4-dihydropyridine derivatives or the pharmacologically acceptable salts thereof represented by the following general formula (I), and process for preparing the same. where R' is dialkoxyalkyl, formyl, formylalkyl, or hydroxyalkyl; R 2 represents alkoxyalkyl, alkenyloxyalkyl, aryloxyalkyl, or aralkyloxyalkyl; R 3 denotes alkyl, haloalkyl, alkoxyalkyl, alkenyloxyalkyl, aryloxyalkyl, aralkyloxyalkyl, or N,N-di-substituted aminoalkyl (the substituents are the same or different alkyl, aralkyl, or aryl); R 4 is alkyl, dialkoxyalkyl, formyl, formylalkyl, or hydroxyalkyl: and R 5 is ortho-, meta-, or paranitro. The compounds of the present invention possess vaso-dilation activities and hypotensive activities, and are expected to be highly useful medicines for the blood circulatory system.
摘要翻译:由以下通式(I)表示的新颖的1,4-二氢吡啶衍生物或其药学上可接受的盐及其制备方法。 其中R 1是二烷氧基烷基,甲酰基,甲酰基烷基或羟烷基; R 2表示烷氧基烷基,烯氧基烷基,芳氧基烷基或芳烷氧基烷基; R 3表示烷基,卤代烷基,烷氧基烷烃,烯氧基烷基,芳氧基烷基,芳烷氧基烷基或N,N-二取代的氨基烷基(取代基是相同或不同的烷基,芳烷基或芳基)。 R 4是烷基,二烷氧基烷基,甲酰基,甲酰基烷基或羟烷基; R 5为邻 - ,间 - 或对硝基苯基。 本发明化合物具有血管扩张活性和降血压作用,预计血液循环系统是非常有用的药物。
摘要:
Novel compounds having vasodilation and hypotensive effects are represented by the formula where R' is halogen, nitro, cyano or lower alkoxy; each of R 2 and R 3 is lower alkyl, lower haloalkyl, lower alkoxyalkyl, aralkyloxyalkyl, aryloxyalkyl, lower alkenoxyalkyl, N,N-di-lower alkylaminoalkyl, N-lower alkyl-N-aralkylaminoalkyl, piperidylalkyl, 4-lower alkyl piperazinylalkyl, norpholinoalkyl or 1-pyrrolidinylalkyl; R' is lower alkyl; A is lower alkylene; and R 5 is hydrogen, lower alkyl, cycloalkyl of 3 to 7 carbon atoms, or aryl unsubstituted or substituted by one or two substituents selected from halogen, nitro, lower alkyl, lower alkoxy, di-lower alkylamino and cyano. Also disclosed are processes for their preparation.