N,N-二甲氨基氯丙烷盐酸盐置于potassium Hydroxide体系中,用 四氢呋喃,水 用作溶剂,化学反应 4.75H,反应生成4-(4-二甲胺基-1-对氟苯基-1-羟基丁基)-3-(羟甲基)苯腈 参考文献:Preparation Of Escitalopram,Its Salts And Intermediates 标题:Preparation Of Escitalopram,Its Salts And Intermediates 摘要:本专利申请涉及一种改进的埃司他洛普兰,其盐和中间体的制备方法.它还涉及到西酞普兰二醇中间体的一种新的结晶形式s,以及用于制备西酞普兰,埃司他洛普兰及其盐的方法.
专利号:US-2008119662-A1 优先权日:2004-02-16 标 题:One Spot Synthesis of Citalopram from 5-Cyanophthalide 发明人:NARAHARI BABU AMBATI; SRINIVAS GOUD VUDDAMARI; GAONKAR SANTOSH LAXMAN; MANJUNATHA SULUR G; KULKARNI ASHOK KRISHNA; KULKARNI MADHARI A 权利人:JUBILANT ORGANOSYS LIMTED 摘要:A process for one pot synthesis of citalopram is disclosed. The process comprises subjecting 5-cyano phthalide to Grignard reduction followed cyclization and followed by C-alkylation reaction to obtain citalopram without isolation and purification of any intermediates. In another embodiment, 5-cyano phthalide is subjected to sequential Grignard reactions followed by cyclization to obtain citalopram without isolation and purification of any intermediate stages.
专利号:US-2008199922-A1 优先权日:2005-06-22 标题 :Chemoenzymatic Process for the Synthesis of Escitalopram 发明人:COTTICELLI GIOVANNI; SALVETTI RAUL; BERTONI CHIARA 权利人:ADORKEM TECHNOLOGY SPA 摘要:A process is described for the preparation of escitalopram and the pharmaceutically acceptable salts thereof starting from 5-cyanophthalide by a process which provides an enantioselective enzymatic deacylation reaction of a complex of the formula (IV) where R represents a C 1 -C 4 alkyl residue or an aryl residue under the action of an esterase from Aspergillus niger.
专利号:US-7166729-B2 优先权日:2001-08-02 标 题:Process for the preparation of 5-substituted isobenzofurans 发明人:DALL ASTA LEONE; COTTICELLI GIOVANNI 权利人:INFOSINT SA 摘要:There is described a process for the preparation of citalopram and of its pharmaceutically acceptable salts, which comprises treating a 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5 isobenzofurancarbaldoxime, O-substituted preferably with a diphenylmethyl or triphenylmethyl group, with formic-acetic anhydride. Furthermore, the total synthesis of citalopram, as free base or in form of its pharmaceutically acceptable salt, starting from 5-formylphthalide is described.
专利号:CN-106892837-A 优先权日:2017-03-23 标题 :Synthesis of 4-[4-(dimethylamino)-1-(4-fluorophenyl)-1-hydroxybutyl]-3-hydroxymethylbenzonitrile
专利号:CH-692298-A5 优先权日:1999-10-25 标 题 :Process for the preparation of intermediates for citalopram synthesis and for the production of escitalopram.