专利号:US-6080860-A 优先权日:1992-08-31 标 题:Methods of making ureas and guanidines including, terazosin, prazosin, doxazosin, tiodazosin, trimazosin, quinazosin and bunazosin (exemplary of 2-substituted quinazoline compounds), and meobentine, and bethanidine and intermediates therefor 发明人:KARIMIAN KHASHAYAR; MURTHY KESHAVA; HALL DARREN 权利人:BRANTFORD CHEMICALSS INC 摘要:Novel methods for the synthesis of substituted ureas and guanidines including Terazosin, Prazosin, Doxazosin, Tiodazosin, Trimazosin, Quinasin and Bunazosin (exemplary of 2-amino substituted Quinazolines), Meobentine and Bethanidine and novel intermediates suitable for use in such methods of synthesis are taught.
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-2008039473-A1 优先权日:2006-08-08 标题:Preparation and utility of substituted quinazoline compounds with alpha-adrenergic blocking effects 发明人:GANT THOMAS G; SARSHAR SEPEHR 权利人:AUSPEX PHARMACEUTICALS INC 摘要:The present disclosure is directed to modulators of alpha-adrenergic receptors and pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and the use of such compounds for the treatment and/or management of hypertension, cardiac failure, prostatitis, and benign prostatic hyperplasia, and any other condition in which it is beneficial to modulate an alpha-adrenergic receptor.
专利号:WO-9405628-A1 优先权日:1992-08-31 标 题 :Synthesis of 2-substituted quinazoline compounds (such as terazosin) and meobentine and bethanidine and intermediates therefor
专利号:EP-0656885-A1 优先权日:1992-08-31 标 题 :Synthesis of 2-substituted quinazoline compounds (such as terazosin) and meobentine and bethanidine and intermediates therefor
参考标题:An Expeditious, Practical Large Scale Synthesis Of 4-Amino-2-Chloro-6,7-Dimethoxyquinazolinazoline 作者:G. Kumaraswamy,Nivedita Jena,M. N. V. Sastry,B. Ashok Kumar |发布日期:2004.8 摘要:Converted To 8 By Treatment With Anhydrous Ammonia At Ambient Temperature In Dilute Thf. In Connection With Our Process Development Of (F)-Doxazocin Mesylate," We Had An Opportunity To Evaluate The Synthesis Of 8. Three Major Challenges Were Encountered In Course Of Reproducing The Above Synthetic Route: (I) Oxidation Of Vanillin (1) To Vaniliic Acid (2) Using Traditional Methods Such As Koh Melt5 Or