Process for producing scopine esters

专利名称：Process for producing scopine esters发明人：BRANDENBURG, JOERG,PFRENGLE,

WALDEMAR,RALL, WERNER

申请号：EP08159580.3申请日：20021224公开号：EP1972626A2公开日：20080924

摘要：Preparation of quaternized scopine 2,2-di-(hetero)arylalkanoic acid esters (I)involves single-stage reaction of a quaternized scopine compound (II) with a di-(hetero)aryl-alkanoic acid (or activated ester) derivative (III). Preparation of quaternizedscopine esters of formula (I) involves single-stage reaction of a quaternized scopinecompound of formula (II) with a diaryl-alkanoic acid derivative of formula RC(O)C(Ar) 2R1> (III). [Image] X, Y : Cl, Br, I, MeSO 3 or CF 3SO 3; R 1>OH, 1-4C alkyl, 1-4C alkoxy, CF 3or F; Ar : phenyl, naphthyl, thienyl or furyl (all optionally substituted by 1-2 1-4C alkyl, 1-4C alkoxy, OH, F, Cl, Br or CF 3); and R : OH, OMe, OEt, O-N-succinimidyl, O-N-phthalimidyl,nitrophenoxy, fluorophenoxy, pentafluorophenoxy, vinyloxy, 2-allyloxy, SMe, SEt or SPh.An independent claim is also included for the use of (II) as starting materials for theproduction of (I). ACTIVITY : Antiasthmatic; Antiinflammatory. MECHANISM OF ACTION :Anticholinergic.

申请人：BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG

地址：Binger Strasse 173 55216 Ingelheim am Rhein DE

国籍：DE

代理机构：Hammann, Heinz

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