CAS: 138402-05-8; 2-Butyl-1,3-Diazaspiro[4.4]Non-2-En-4-One

相似化合物

151257-01-1 1003959-62-3 1713163-91-7

上下游产品

CAS号1664-35-3 1-氨基环戊烷-1-羧酸乙酯 | CAS号999-09-7 ethyl pentanimidate | CAS号253269-07-7 (N-valeryl)-1-a... | CAS号17193-28-1 顺式-2-氨基-1-环戊甲酰胺 | CAS号638-29-9 正戊酰氯 | CAS号138402-11-6 厄贝沙坦 | CAS号138401-24-8 2-丁基-3-[[2'-氰基-...

1-氨基-1-环戊烷羧酰胺置于三乙胺,Potassium Hydroxide体系中,用 甲醇,二氯甲烷 用作溶剂,化学反应 3.0H,反应生成2-丁基-1,3-二氮杂螺环-[4,4]壬-1-烯-4酮
参考文献:设计,合成和评估新型有效的血管紧张素ii受体1拮抗剂.
标题:设计,合成和评估新型有效的血管紧张素ii受体1拮抗剂.
摘要:设计,合成和评估了一系列新的血管紧张素ii(ang Ii)受体1拮抗剂.所有化合物在放射性配体结合试验中均显示出与1型血管紧张素ii受体的纳摩尔亲和力,并且可以显着降低自发性高血压大鼠(shrs)的血压.由此可见,化合物2B在放射性配体结合测定中显示出与血管紧张素ii 1型受体更高的亲和力结合,与厄贝沙坦的数量级相同,Ic50值为1.26 +/-0.08 Nm.2B显示出有效且持久的降血压效果,在shr中,最大降低反应为15 Mg / Kg时mbp为40.62 +/-4.08 Mmhg,10 Mg / Kg时为10 Mg / Kg 28.39 +/-2.09 Mmhg,39.56 + /-Rhr中15 Mg / Kg时为4.83 Mmhg,10 Mg / Kg时为29.05 +/-2.20 Mmhg,在shr和rhr中,显着的降压作用持续超过12小时.在单剂量药代动力学实验中,口
Doi:10.1016/j.Ejmech.2016.07.023

专利信息

专利号:US-6271375-B1
优先权日:1997-06-30
标 题 :Ortho-metalation process for the synthesis of 2-substituted-1-(tetrazol-5-yl)benzenes
发明人：VILLA MARCO; ALLEGRINI PIETRO; ARRIGHI KATIUSCIA; PAIOCCHI MAURIZIO
权利人:ZAMBON SPA
摘要:A process of direct metalation of phenyltetrazoles useful for preparing compounds of formula (II) intermediates for the synthesis of angiotensin II antagonists is described.

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-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:US-10300471-B2
优先权日:2013-10-08
标题 :Ruthenium-catalyzed synthesis of biaryl compounds in water
发明人：KOOHANG ALI AIDEN; MEHTA ANITA
权利人:CHICAGO DISCOVERY SOLUTIONS LLC
摘要:Using a [RuCl 2 (arene)] 2 complex and a formate source, a directed ortho C—H insertion and aryl-aryl coupling sequence in water provides biaryl compounds useful in the preparation of biologically active molecules and intermediates. Reactions may be conducted in the ambient atmosphere. Ruthenium catalysts prepared from [RuCl 2 (arene)] 2 and a formate source may be prepared in situ or isolated for later use.