CAS: 148849-67-6; (S)-3-(3-(((3,4-Dimethoxybicyclo[4.2.0]Octa-1,3,5-Trien-7-yl)Methyl)(Methyl)Amino)Propyl)-7,8-Dimethoxy-1,3,4,5-Tetrahydro-2H-Benzo[d]Azepin-2-One Hydrochloride

上下游产品

1-[(7S)-3,4-dimethoxybicyclo[4.2.0]°Cta-1,3,5-trien-7-yl]-N-methylmethanamine hydr°Chloride ivabradine 3,4-dimethoxy-bicyclo[4.2.0]°Cta-1,3,5-triene-7-carbonitrile (R,S)-4,5-dimethoxy-1,2-dihydr°Cyclobutabenzene-1-carboxylic acidivabradine {2-[2-({3-[{[(7S)-3,4-dimethoxybicyclo[4.2.0]°Cta-4,3,5-trien-7-yl]methyl}(methyl)-amino]propyl}amino)ethyl]-4,5-dimethoxyphenyl}acetic acid

4,5-二甲氧基苯并环丁烷-1-甲酸置于palladium 10% On Activated Carbon,N,N-二甲基甲酰胺 盐酸,硼烷四氢呋喃络合物,草酰氯,氢气,Potassium Carbonate,Sodium Iodide体系中,用 四氢呋喃,N-甲基吡咯烷酮,二氯甲烷,水,乙酸乙酯 用作溶剂,60.0 °C,1.0 Mpa 条件下,反应 11.16H,反应生成盐酸伊伐布雷定
参考文献: Industrial Process For The Synthesis Of Ivabradine Salts[fr] Procédé Industriel Pour La Synthèse De Sels D'Ivabradine
标题: Industrial Process For The Synthesis Of Ivabradine Salts[fr] Procédé Industriel Pour La Synthèse De Sels D'Ivabradine
摘要:合成ivabradine盐(化学式为(i))的过程,其化学名称为:3-{3-[((S)-3,4-二甲氧基-双环[4.2.0]辛烷-1,3,5-三烯-7-基甲基)-甲基-氨基]-丙基}-7,8-二甲氧基-1,3,4,5-四氢-2H-3-苯并蒽啉-2-酮盐(hq=hcl,Hbr,Hi,Hno3,Hclo4,(cooh)2),以及其新的中间体.Ivabradine(i)与硝酸(i,Hq=hno3),盐酸(i,Hq=hcl),溴酸(i,Hq=hbr),碘酸(i,Hq=hi),草酸(i,Hq=(cooh)2)和高氯酸(i,Hq=hclo4)的酸加合物的某些晶体形式.

专利信息

专利号:US-9506095-B2
优先权日:2012-02-09
标 题:Process for the enzymatic synthesis of (7S)-3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-triene-7-carboxylic acid or esters thereof, and application in the synthesis of ivabradine and salts thereof
发明人：PEDRAGOSA-MOREAU SANDRINE; LEFOULON FRANÇOIS
权利人:SERVIER LAB; LES LABORATORIES SERVIER
摘要:Process for the enzymatic synthesis of the compound of formula (I): n nwherein R 1 represents a hydrogen atom or an alkyl group.n n Application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid.

专利号:US-7928223-B2
优先权日:2008-06-20
标题:Process for the synthesis of 7,8-dimethoxy-1,3-dihydro-2H-3-benzazepin-2-one, and application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid
发明人：LERESTIF JEAN-MICHEL; LECOUVE JEAN-PIERRE; BRIGOT DANIEL
权利人:SERVIER LAB
摘要:Process for the synthesis of the compound of formula (I): n n n n n n n n n n Application in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.

专利号:US-9045788-B2
优先权日:2012-07-17
标题:Process for the enzymatic synthesis of (7S)-1-(3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl) N-methyl methanamine, and application in the synthesis of ivabradine and salts thereof
发明人：PEDRAGOSA-MOREAU SANDRINE; LEFOULON FRANÇOIS; MORIS VARAS FRANCISCO; GONZALEZ SABIN JAVIER
权利人:SERVIER LAB
摘要:Process for the enzymatic synthesis of the compound of formula (I), (7S)-1-(3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl)N-methyl methanamine: n nand application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid.

专利号:US-8927708-B2
优先权日:2013-03-26
标 题 :Process for the synthesis of 7,8-dimethoxy-1,3-dihydro-2H-3-benzazepin-2-one compounds, and application in the synthesis of ivabradine
发明人：LE FLOHIC ALEXANDRE
权利人:SERVIER LAB
摘要:Process for the synthesis of the compound of formula (I): n nwherein R represents a para-methoxybenzyl (PMB) group or the following group:n n nApplication in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid.

专利号:US-9476071-B2
优先权日:2013-02-28
标 题 :Process for the enzymatic synthesis of (7S)-3,4-dimethoxybicyclo[4.2.0]OCTA-1,3,5-triene-7-carboxylic acid and application in the synthesis of ivabradine and salts thereof
发明人：PEDRAGOSA-MOREAU SANDRINE; LEFOULON FRANÇOIS
权利人:SERVIER LAB
摘要:Process for the enzymatic synthesis of the compound of formula (I): n ncomprising enantioselective enzymatic hydrolysis of the nitrile of formula (IV):n n nusing the nitrilase of Rhodococcus rhodochrous of EMBL accession number EF467367.1, and the application of such a process in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid.

专利号:WO-2019202611-A1
优先权日:2018-04-21
标题:An improved process for the synthesis of ivabradine and its pharmaceutically acceptable salts
发明人：NANDEPU Venkateswara Rao; BOPPANA DURGA PRASAD
权利人:METROCHEM API PVT
摘要:: Disclosed herein is an improved process for the preparation of Ivabradine and pharmaceutically acceptable salts thereof. The invention more particularly disclosesthe synthesis of key intermediates viz.,(S)-N-[(4,5-dimethoxybenzocydobut-l-yl)-methyl]-N- (methyl)amine hydrochloride of Formula-II and 3-(3-Iodopropyl)-7,8-dimethoxy-1,3-dihydro-2H-3-benzapin-2-one of Formula-III, and its use in industrial synthesis of Ivabradine and pharmaceutically acceptable salts thereof.