首页> 外国专利> A PROCESS FOR TH SYNTHESIS OF 1-(4-ARYLPIPERAZIN-1-YL)-ω-(2,5-DIOXOPYRROLIDIN-1-YL)ALKANES AS α1-ADRENORECEPTOR BLOCKERS USEFUL FOR HYPERTENSION AND BENIGN PROSTATIC HYPERPLASIA (BPH)

A PROCESS FOR TH SYNTHESIS OF 1-(4-ARYLPIPERAZIN-1-YL)-ω-(2,5-DIOXOPYRROLIDIN-1-YL)ALKANES AS α1-ADRENORECEPTOR BLOCKERS USEFUL FOR HYPERTENSION AND BENIGN PROSTATIC HYPERPLASIA (BPH)

机译:合成1-(4-芳基哌嗪-1-基)-ω-(2,5-二氧杂吡啶基-1-基)链烷烃作为α1-肾上腺素受体阻滞剂用于高血压和良性前列腺增生症(BPH)的合成方法

摘要

A process for the Preparation of I- (4-ARYLPIPKRAZIN - I - YL) -  - (2, 6-dioxopiperidin-1-yl) alkanes of Formula III, as selected a I - adrenoceptor blockers useful for the treatment of benign prostatic hyperplasia (BPH) and hypertension, as shown in the accompanied drawings, wherein R represents group like chlorophenyl fluorophenyl, methylphenyl, methoxyphenyl, pyridyl, pyrimidyl, di-methylphenyl and trifluoromethylphenyl and n = 2-4, which comprises condensing 2,6-dioxoperidine of formla I With l-(4-arylpiperazin-l-yl) - -chloro-alkanes of the formula II as shown in the accompanied drwings, wherein R and n have the same meanings as defined above, in the presence of a base and a phase transfer catalyst tetrabuyl ammonium bromide and potassium iodide in an organic solvent at a temperature ranging upto I50°C.
机译:制备式III的I-(4-ARYLPIPKRAZIN-I-YL)--(2,6-二氧代哌啶-1-基)烷烃的方法,所述I-肾上腺素受体阻滞剂可用于治疗前列腺如附图所示,其中R代表氯苯基氟苯基,甲基苯基,甲氧基苯基,吡啶基,嘧啶基,二甲基苯基和三氟甲基苯基,并且n = 2-4,其包括缩合的2,6-二氧哌啶式I中式II的1-(4-芳基哌嗪-1-基)-C 1-氯代烷烃的式I的制备,其中R和n在碱存在下与上述定义相同相转移催化剂,在有机溶剂中,在高达50℃的温度下,四丁基溴化铵和碘化钾。

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