CAS: 114772-54-2; 4'-(Bromomethyl)-[1,1'-Biphenyl]-2-Carbonitrile

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CAS号114772-53-1 2-氰基-4'-甲基联苯 | CAS号4419-11-8 偶氮二异庚腈 | CAS号34241-39-9 2-(2-cyanopropa... | CAS号94-36-0 过氧化苯甲酰 | CAS号108-90-7 氯苯 | CAS号3839-22-3 2-氰基苯甲酸 | CAS号131-63-5 ammonium 2-(ami... | CAS号57598-33-1 2-(2-甲氧基苯基)-4,4... | CAS号74201-13-1 N-(2-羟基-1,1-二甲基... | CAS号84392-32-5 4,4-二甲基-2-(4'-甲... | CAS号141745-71-3 N-[(2'-Cyano[1,... | CAS号482577-59-3 N-[(2'-氰基联苯-4-基... | CAS号133690-92-3 4'-氨甲基-2-氰基联苯 | CAS号139481-38-2 methyl 2-[[4-(2... | CAS号154709-19-0 4-(2-氰基苯基)苄醇 | CAS号138402-11-6 厄贝沙坦 | CAS号124750-99-8 氯沙坦钾 | CAS号139481-28-0 甲酯C4 | CAS号138401-24-8 2-丁基-3-[[2'-氰基-... | CAS号137863-89-9 缬沙坦烃化物

邻甲氧基苯甲酸置于吡啶,N-溴代丁二酰亚胺(Nbs),氯化亚砜,三氯氧磷,过氧化苯甲酰体系中,用 四氢呋喃,四氯化碳,二氯甲烷 用作溶剂,化学反应 29.0H,反应生成2-氰基-4'-溴甲基联苯
参考文献:非肽血管紧张素ii受体拮抗剂:发现了一系列n-(联苯基甲基)咪唑类有效的口服活性降压药.
标题:非肽血管紧张素ii受体拮抗剂:发现了一系列n-(联苯基甲基)咪唑类有效的口服活性降压药.
摘要:制备了一系列新的非肽血管紧张素ii(aii)受体拮抗剂.这些n-(联苯基-甲基)咪唑,例如2-丁基-1-[[(2'-羧基联苯-4-基)甲基]-4-氯-5-(羟甲基)咪唑,不同于先前报道的n-(苯甲酰氨基苄基)咪唑和相关化合物,因为它们在口服时产生有效的降压作用;较早的系列通常仅在静脉内给药时才有效.已经发现联苯的2'-位的酸性基团是必不可少的.仅邻位取代的酸具有对aii受体的高亲和力和非常好的口服降压效能.羧酸基团已被各种酸性等排体取代,并且发现四唑环是最有效的.四唑衍生物dup 753
Doi:10.1021/jm00112A031

专利信息

专利号:WO-2005049586-A1
优先权日:2003-11-24
标 题:Process for production of (s) -n-pentanoyl-n-[[2’-(1h-tetrazole-5yl) [1,1’-biphenyl]-4-yl]methyl]-l-valine
发明人：CEPANEC IVICA; LITVIC MLADEN; KORETIC STEFANIJA; BARTOLINCIC ANAMARIJA; DRUSKOVIC VINKA; SPOREC ANITA
权利人:BELUPO LIJEKOVI KOZMETIKA D D; CEPANEC IVICA; LITVIC MLADEN; KORETIC STEFANIJA; BARTOLINCIC ANAMARIJA; DRUSKOVIC VINKA; SPOREC ANITA
摘要:The patent relates to a new process of synthesis of an antihypertensive agent, N-pentanoyl-N-[[2'-(1H-tetrazole-5-yl)[1,1'-biphenyl]-4-yl]methyl]-L-valine (1), also known under the generic name of valsartan, by selective reaction of N-pentanoyl-N-[[2'-(1H-tetrazole-5-yl) [1,1'-biphenyl]-4-yl]methyl]-L-valine methyl-ester (14) with metallic or quaternary ammonium trialkylsilanolates by SN2 reaction. The compound 14 was produced in four reaction steps starting from 2N-trityl-5-(4'-methylbiphenyl-2-yl)tetrazole (17) and L-valine methyl-ester (11). Free-radical bromination of the compound 17 with N-bromosuccinimide produced 2N-trityl-5-(4'-bromomethylbiphenyl-2-yl)tetrazole (7), which in the reaction with L-valine methyl-ester (11) results in N-[[2'-(2N-trityl-tetrazole-5-yl)[1,1'-biphenyl]-4­yl]methyl]-L-valine methyl-ester hydrobromide (15). Acylation of the compound 15 with pentanoyl chloride in the presence of trialkylamine bases results in N-pentanoyl-N-[[2'-(2N­trityl-tetrazole-5-yl)[1,1'-biphenyl] -4-yl]methyl]-L-valine methyl-ester (16). Removal of trityl protecting group by strong acids produces the key intermediary, compound 14.

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.

专利号:EP-1831186-B1
优先权日:2004-11-30
标题:A process for the synthesis of valsartan
发明人：ZUPANCIC SILVO; PECAVAR ANICA; ZUPET ROK
权利人:KRKA D D NOVO MESTO
摘要:This invention relates to an improved process for preparing a valsartan, or a pharmaceutically acceptable salt thereof, or pharmaceutical preparation containing either entity wherein a compound of formula (II) nor a salt thereof, is reacted with valine or an ester or a salt thereof in a solvent selected from the group consisting of methylene chloride, chloroform, butyl chloride, isopropyl acetate and tert -butyl methyl ether to form a compound of formula (IV) nwhich is then acylated to form a compound of formula (VI) nwherein R is hydrogen, alkyl, alkenyl or benzyl; which is then deprotected to give valsartan, and may be converted to a pharmaceutically acceptable salt and/or a pharmaceutical formulation. The invention also covers intermediates of formula (IV) and (VI) wherein R=H.

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:EP-2149566-A1
优先权日:2008-07-15
标 题 :A process for the preparation of telmisartan
发明人：ROSSI RENZO; BELLINA FABIO; CAUTERUCCIO SILVIA; CASTALDI GRAZIANO
权利人:CHEMO IBERICA SA
摘要:The present invention relates to a process for the preparation of Telmisartan by hydroxycarbonylation of compound of formula (V),n nwherein X is a substituent which can be transformed into a carboxy group by hydroxycarbonylation. The invention also relates to intermediates for the synthesis of Telmisartan.

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.