CAS: 81403-68-1; N-(3-((4-Amino-6,7-Dimethoxyquinazolin-2-yl)(Methyl)Amino)Propyl)Tetrahydrofuran-2-Carboxamide Hydrochloride

上下游产品

tetrahydrofuran-2-carboxamideN-3-(methylamino)propyltetrahydrofuran-2-carboxamide 2-chloro-6,7-dimethoxyquinazolin-4-amine tetrahydro-2-furancarboxylic acid tetrahydro-N-(3-cyanopropyl)-N-methylfurancarboxamide alfuzosin

(乙基碳酸)四氢呋喃-2-羧酸酐置于rh On Carbon 氨,氢气体系中,用 四氢呋喃,异戊醇 作为反应溶剂,25.0~80.0 °C,5.79 Mpa 条件下,反应 12.0H,反应生成 盐酸阿夫唑嗪
参考文献:一系列4-氨基-6,7-二甲氧基喹唑啉衍生物的合成及其降压活性.
标题:一系列4-氨基-6,7-二甲氧基喹唑啉衍生物的合成及其降压活性.
摘要:合成了一系列的n2-[(酰基氨基)烷基]-6,7-二甲氧基-2,4-喹唑啉二胺作为潜在的α1-肾上腺素受体拮抗剂.当以10 Mg / Kg Po自发性高血压大鼠给药时,许多丙烷二胺衍生物显示出非常好的降压活性,而乙二胺衍生物尽管在结构上与哌唑嗪密切相关,却缺乏该特性.活性最高的衍生物n-[3-[(4-氨基-6,7-二甲氧基-2-喹唑啉基)甲基氨基]丙基]四氢-2-呋喃甲酰胺x盐酸盐阿夫唑嗪(12)对外围α1具有很高的选择性.-结后肾上腺素受体.在等剂量的降压剂量下,其对清醒犬体位变化的升压反应的作用不如哌唑嗪所显示.根据这些结果,
DOI:10.1021/jm00151A003

专利信息

专利号:WO-2009001369-A1
优先权日:2007-06-22
标 题 :An improved process for the preparation of alfuzosin hydrochloride
发明人：DEO KESHAV; DESAI SANJAY; RATHOD DHIRAJ MOHANSINH; PARIKH CHIRAG CHANDRAKANT; PATEL RIPALKUMAR KANTIBHAI
权利人:ALEMBIC LTD; DEO KESHAV; DESAI SANJAY; RATHOD DHIRAJ MOHANSINH; PARIKH CHIRAG CHANDRAKANT; PATEL RIPALKUMAR KANTIBHAI
摘要:The present invention relates to an improved process for the preparation of Alfuzosin hydrochloride of formula (I) comprising a step of reacting compound of formula (IV) with compound of formula (V) in presence of aprotic solvent to obtain compound of formula (III) which is a useful intermediate for synthesis of Alfuzosin hydrochloride of formula (I).

专利号:WO-2008084493-A3
优先权日:2007-01-09
标 题 :A novel process for the preparation of 2-halo-4-aminoquinazolines
发明人：BHOBE AJIT MADHUKAR; DAMLE SUBHASH VISHWANATH; ADHVARYU RUSHI DRUPADBHAI
权利人:UNICHEM LAB LTD; BHOBE AJIT MADHUKAR; DAMLE SUBHASH VISHWANATH; ADHVARYU RUSHI DRUPADBHAI
摘要:2-Halo-4-aminoquinazolines are produced by a one-step process involving intramolecular cyclization of appropriately substituted formamide derivatives in the presence of phosphorous oxyhalides. Exemplary of the process is the intramolecular cyclization of 3,4-dimethoxy-6-cyanoaniline-1-yl formamide in the presence of phosphorous oxychloride to 2-chloro-4-amino-6,7-dimethoxyquinazoline. These chemical compounds are utilized as intermediates in the preparation of some of the important antihypertensive agents e.g. 2-chloro-4-amino-6,7-dimethoxyquinazolines is used for the synthesis of alfuzosin hydrochloride.

专利号:US-2006062846-A1
优先权日:2004-09-17
标题 :Alfuzosin tablets and synthesis
发明人：SCHEER MATHIAS; REY HELENE; FISCHER MARC; KRAMER DIRK
权利人:CIMEX PHARMA AG
摘要:A monolithic composition includes alfuzosin in a polymeric matrix adapted to release 13-33% of the alfuzosin within 2 hours, 40-60% of the alfuzosin within 7 hours, and greater than 80% of the alfuzosin within 20 hours of administration. A unit dosage form includes: a heterogeneous mixture of alfuzosin hydrochloride anhydrate, lactose monohydrate, hydroxypropylmethylcellulose, polyvinylpyrrolidone and magnesium stearate, wherein the heterogeneous mixture is heterogeneously distributed throughout the unit dosage form. A manufacturing process includes: mixing a hydrophilic polymer and alfuzosin to provide a blend; granulating the blend to provide granules; drying the granules on a dryer to provide dried granules; sizing the dried granules to provide sized granules; mixing the sized granules with a lubricant to obtain a mixture; and compressing the mixture to obtain a tablet. A method of treating benign prostatic hyperplasia, includes administering to a patient the composition or unit dosage form once a day.

专利号:US-2011201633-A1
优先权日:2004-09-17
标题 :Alfuzosin tablets and synthesis
发明人：SCHEER MATHIAS; KELBERT MICHEL
权利人:ACINO PHARMA AG
摘要:A monolithic composition includes alfuzosin in a polymeric matrix adapted to release 13-33% of the alfuzosin within 2 hours, 40-60% of the alfuzosin within 7 hours, and greater than 80% of the alfuzosin within 20 hours of administration. A unit dosage form includes: a heterogeneous mixture of alfuzosin hydrochloride, lactose monohydrate, hydroxypropylmethylcellulose, polyvinylpyrrolidone and magnesium stearate, wherein the heterogeneous mixture is heterogeneously distributed throughout the unit dosage form. A manufacturing process includes: mixing a hydrophilic polymer and alfuzosin to provide a blend; granulating the blend to provide granules; drying the granules on a dryer to provide dried granules; sizing the dried granules to provide sized granules; mixing the sized granules with a lubricant to obtain a mixture; and compressing the mixture to obtain a tablet. A method of treating benign prostatic hyperplasia, includes administering to a patient the composition or unit dosage form once a day.