CAS: 151257-01-1; 2-Butyl-1,3-Diazaspiro[4.4]Non-1-En-4-One Hydrochloride

相似化合物

151257-01-1 759442-73-4 3012580-81-0

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CAS号194984-24-2 N- (1- cyano cy...

1-Cyano-1-N-Pentanoylaminocyclopentane置于盐酸体系中,用 丙醇 用作溶剂,化学反应生成2-丁基-1,3-二氮杂螺环[4,4]壬-1-烯-4-酮盐酸盐
参考文献:Process For The Preparation Of 4-Oxoimidazolinium Salts
标题:Process For The Preparation Of 4-Oxoimidazolinium Salts
摘要:通用公式为:##str1##其中r.Sup.1和r.Sup.2分别独立为c.Sub.1-10-烷基,C.Sub.2-10-烯基,C.Sub.3-7-环烷基或可选择取代的芳基,芳基烷基,杂环芳基或杂环芳基烷基,或者r.Sup.1和r.Sup.2与它们结合的碳原子一起形成一个三元至七元的饱和或不饱和碳环或杂环,R.Sup.3是c.Sub.1-10-烷基,C.Sub.1-10-烯基,C.Sub.3-7-环烷基,芳基,芳基烷基或杂环芳基,而a.Sup.--是强酸的阴离子,通过在非水溶剂中,在较低醇和强酸的存在下,环化α-酰胺基腈制备.这些化合物是制药活性物质的中间体,例如血管紧张素ii拮抗剂.

专利信息

专利号:US-6211382-B1
优先权日:1997-07-25
标题 :Process for the preparation of 1,3-diaza-spiro (4.4) non-1-en-4-one derivatives and 1-cyano-1-acylaminocyclopentane intermediates
发明人：HUSZAR CSABA; KIS-TAMAS ATTILA; NEMETH ATTILA; NAD ZSUZSANNA; MAKOVI ZOLTAN; GAJARY ANTAL; KOLLAR ENDRE; ARANYOSI PETER; GYUERE KAROLY; MESZAROS ISTVAN; HARI ZSUZSANNA CSETRIN; SUPIC ATTILA; ZRINYI ILONA DERVALICSNE; DUBOVSZKI KATALIN; PALIN LAJOSNE; KARASH AGNES; BOGNAR ERZSEBET
权利人:SANOFI SYNTHELABO
摘要:Process for the preparation of compounds of formula (I) wherein R means hydrogen atom, or C1-6 alkyl group, or C7-12 aralkyl group or phenyl group, characterised in that a) the compound of formula (III) is reacted with a compound of formula (IV) wherein X means halogen atom or C1-5 alkoxy group or hydroxyl group, and the resulting compound of formula (II) is transformed, in a reaction medium with pH above 7, into the compound of formula (I) or b) the compound of formula (III) is reacted with an anhydride of general formula (V) and the resulting compound of formula (II) transformed, in a reaction medium with pH above 7, into the compound of formula (I), or c) a compound of formula (II) is transformed, in a reaction medium with pH above 7, into the compound of formula (I), and if desired, the resulting compounds of formula (I), before or after isolation, are transformed into acid addition salts, or the compounds of formula (I) are liberated from their acid addition salts. Thus a process for the preparation of intermediates useful in synthesis of angiotensin II antagonists is disclosed.

专利号:US-6239286-B1
优先权日:1997-07-25
标 题:Process for the preparation of 1,3-diaza-spiro (4.4) non-1-en-4-one derivatives and 1-cyano-1-acylamino-cyclopentane intermediates
发明人：KIS-TAMAS ATTILA; HUSZAR CSABA; CASTRO BERTRAND; NEMETH ATTILA; ARANYOSI PETER; GYUERE KAROLY; MESZAROS ISTVAN; ZRINYI ILONA DERVALICSN; DUBOVSZKI KATALIN; PALI LAJOSNE; GAJARY ANTAL; SUPIC ATTILA; NAD ZSUZSANNA; MAKOVI ZOLTAN; KOLLAR ENDRE; HARI ZSUZSANNA CSETRIN; KARASZA GN; BOGNAR ERZSEBET
权利人:SANOFI SYNTHELABO
摘要:Process for the preparation of compounds of formula (I) wherein R means hydrogen atom, or C1-6 alkyl group, or C7-12 aralkyl group or phenyl group, characterised in that: a) the compound of formula (III) is reacted with a compound of formula (IV) wherein X means halogen atom or C1-5 alkoxy group or hydroxyl group and the resulting compound of formula (II) is transformed in the presence of an oxidising agent in a reaction medium with pH above 7, into the compound of formula (I), or b) the compound of formula (III) is reacted with an anhydride of general formula (V) and the resulting compound of formula (II) transformed in the presence of an oxidising agent, in a reaction medium with pH above 7, into the compound of formula (I), or c) a compound of formula (II) is transformed in the presence of an oxidising agent, in a reaction medium with pH above 7, into the compound of formula (I), and if desired, the resulting compounds of formula (I), before or after isolation, are transformed into acid addition salts, or the compounds of formula (I) are liberated from their acid addition salts. Thus a process for the preparation of intermediates useful in synthesis of angiotensin II antagonists is disclosed.

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.