CAS: 138401-24-8; 4'-((2-Butyl-4-Oxo-1,3-Diazaspiro[4.4]Non-1-En-3-yl)Methyl)-[1,1'-Biphenyl]-2-Carbonitrile

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CAS号114772-54-2 4'-溴甲基-2-氰基联苯 | CAS号138402-05-8 2-丁基-1,3-二氮杂螺环-... | CAS号15026-80-9 N-戊酰基氨基环戊烷-1-羧酸 | CAS号133690-92-3 4'-氨甲基-2-氰基联苯 | CAS号60421-23-0 环亮氨酸甲酯盐酸盐 | CAS号109-52-4 正戊酸 | CAS号141745-71-3 N-[(2'-Cyano[1,... | CAS号210037-90-4 2-CYANO-4-BROMO... | CAS号138402-11-6 厄贝沙坦 | CAS号138402-10-5 三苯甲基依贝沙坦

环亮氨酸置于sodium Hydroxide,1-羟基苯并三唑,N,N'-二环己基碳二亚胺,三氟乙酸体系中,用 二氯甲烷,水,甲苯 用作溶剂,化学反应 2.0H,反应生成厄贝沙坦烃化物
参考文献:A New Entry To Antihypertensive Active Pharmaceutical Ingredient,Irbesartan And Its Analogues
标题:A New Entry To Antihypertensive Active Pharmaceutical Ingredient,Irbesartan And Its Analogues
摘要:
Doi:10.1515/hc.2006.12.5.323

专利信息

专利号:EP-1546135-B1
优先权日:2002-07-16
标题:Novel synthesis of irbesartan
发明人：NISNEVICH GENNADY; RUKHMAN IGOR; PERTSIKOV BORIS; KAFTANOV JULIA; DOLITZKY BEN-ZION
权利人:TEVA PHARMA
摘要:Provided is a novel synthesis of irbesartan employing a phase transfer catalyst. Also provided is irbesartan having a fine particle size.

专利号:US-7312340-B2
优先权日:2003-02-05
标 题:Synthesis of 2-butyl-3-(1-trityl-1H-tetrazol-5-YL)biphenyl-4-YL)-1,3-diazaspiro[4,4]- non-ene-4-one
发明人：DOLITZKY BEN-ZION; KAFTANOV JULIA; PERTSIKOV BORIS; RUKHMAN IGOR; NISNEVICH GENNADY
权利人:TEVA PHARMA
摘要:Provided is a novel method of making 2-butyl-3-[[2′(1-trityl-1H-tetrazol-5-yl)biphen-4-yl]methyl]-1,3-diazaspiro[4.4]non-1-ene-4-one, which can be converted to irbesartan. Also provided are methods of making irbesartan.

专利号:US-7838683-B2
优先权日:2003-01-16
标题:Synthesis of irbesartan
发明人：NISNEVICH GENNADY; RUKHMAN IGOR; PERTSIKOV BORIS; KAFTANOV JULIA; DOLITZKY BEN-ZION
权利人:TEVA PHARMA
摘要:Provided are a method of making irbesartan via a Suzuki coupling reaction and a novel intermediate, 2-butyl-3-(4′-bromobenzyl)-1,3-diazaspiro[4.4]non-1-ene-4-one, for such process. The novel process includes the step of reacting such intermediate with a protected imidazolephenylboronic acid.

专利号:WO-2005051943-A1
优先权日:2003-11-28
标题:Processes for the preparation of highly pure irbesartan
发明人：KUMAR YATENDRA; PRASAD MOHAN; NATH ASOK; ARORA SURINDER KUMAR
权利人:RANBAXY LAB LTD; KUMAR YATENDRA; PRASAD MOHAN; NATH ASOK; ARORA SURINDER KUMAR
摘要:The present invention relates to processes for synthesis of highly pure irbesartan or pharmaceutically acceptable salts thereof.

专利号:US-7741492-B2
优先权日:2005-02-28
标题:Method for obtaining a pharmaceutically active compound (Irbesartan) and its synthesis intermediate
发明人：HUGUET CLOTET JOAN; DALMASES BARJOAN PERE
权利人:INKE SA
摘要:It is provided a method for obtaining Irbesartan polymorph A, with few synthesis steps, by coupling the intermediate of formula (II) with the compound of formula (III), neutralising one of its alkaline salts in an aqueous medium and recrystallising the crude product obtained. The utilisation of said method obviates protection and deprotection of the tetrazole ring and is therefore of considerable interest for obtaining Irbesartan on a large industrial scale. The invention also refers to the synthesis intermediate of formula (II).

专利号:US-8609859-B2
优先权日:2009-04-08
标题 :One pot process for preparing 2-butyl-3-[[2′-(1H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-1,3-diazaspiro [4, 4] non-1-en-4-one (irbesartan)
发明人：KOLHE PRAKASH YASHWANT; JOSHI RAJESH DILIP; SRIVASTAVA BIMAL KUMAR; PATEL NITIN JERAMBHAI; GAJJAR SANKET SURESHBHAI
权利人:KOLHE PRAKASH YASHWANT; JOSHI RAJESH DILIP; SRIVASTAVA BIMAL KUMAR; PATEL NITIN JERAMBHAI; GAJJAR SANKET SURESHBHAI; CTX LIFE SCIENCES PVT LTD
摘要:A one pot process for the synthesis of Irbesartan comprising reacting 2-n-Butyl-1,3-Diazaspiro[4,4]Non-1-en-4-one (Formula III) and Bromomethyl Cyanobiphenyl (Formula IV) in the presence of base and water with the optional use of PTC to give formula II from which Irbesartan is obtained by reacting with sodium azide and triethylamine hydrochloride in the presence of a non polar solvent.