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专利名称：METHOD FOR THE PREPARATION OF
CITALOPRAM
发明人：PETERSEN, Hans,AHMADIAN, Haleh申请号：EP01957785.7申请日：20010814公开号：EP1309581A1公开日：20030514
摘要：Preparation of citalopram (I) involves conversion of a 5-halogenated compound(II) to a 5-carboxylic acid intermediate (III) followed by conversion of (III) to (I). -Preparation of citalopram (1-(3-(dimethylamino)propyl)-1-(4-fluorophenyl)-1,3-dihydro-5-isobenz ofurancarbonitrile) (I) involves conversion of 5-halogenated compound offormula (II) to a 5-carboxylic acid intermediate of formula (III) followed by conversion of(III) to (I). - Z = halo. - An INDEPENDENT CLAIM is included for the preparation ofcompounds of formula (III) and (V). - X = halo, CN, OR5, SR6 or NR7R8; - R5, R6 = 1-6Calkyl, (hetero)aryl or benzyl (all optionally substituted with T); - T = halo, 1-4C alkyl,cyano, -OH, 1-4C alkoxy, trifluoromethyl, nitro, amino, mono- or di-(1-4C)alkylamino; - Y =O, S or NR9; and - R7-R9 = R5 or H. - ACTIVITY - Antidepressant. - MECHANISM OFACTION - Serotonin (5-hydroxytryptamine; 5-HT) reuptake inhibitor. - No biological datagiven.
申请人：H. LUNDBECK A/S
地址：9, Ottiliavej 2500 Copenhagen DK
国籍：DK
代理机构：Nielsen, Leila
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