首页> 外国专利> NOVEL INTERMEDIATES FOR THE PREPARATION OF ANTIHISTAMINIC 4-DIPHENYLMETHYL/DIPHENYLMETHOXY PIPERIDINE DERIVATIVES

NOVEL INTERMEDIATES FOR THE PREPARATION OF ANTIHISTAMINIC 4-DIPHENYLMETHYL/DIPHENYLMETHOXY PIPERIDINE DERIVATIVES

机译:新型中间体用于制备抗组胺的4-二苯甲基/二苯甲氧基哌啶碱衍生物

摘要

The present invention is relatedto novel intermediates and processeswhich are useful in the preparationof certain antihistaminic piperidinederivatives of formula (I) wherein Wrepresents -C(=O)- or -CH(OH)-; R1represents hydrogen or hydroxy; R2represents hydrogen; R1 and R2 takentogether form a second bond betweenthe carbon atoms bearing R1 and R2;n is an integer of from 1 to 5; m isan integer 0 or 1; R3 is -COOH or-COOalkyl wherein the alkyl moietyhas from 1 to 6 carbon atoms and isstraight or branched; each of A is hydrogen or hydroxy; and pharmaceuticallyacceptable salts and individual optical isomers thereof, withthe proviso that where R1 and R2 are taken together to form a second bondbetween the carbon atoms bearing R1 and R2 or where R1represented hydroxy, m is an integer 0.
机译:本发明涉及新颖的中间体和工艺在准备中很有用某些抗组胺哌啶式(I)的衍生物,其中W代表-C(= O)-或-CH(OH)-; R1代表氢或羟基; R2代表氢; R1和R2已采取一起形成带有R 1和R 2的碳原子;n为1至5的整数; m是整数0或1; R3是-COOH或-COO烷基,其中烷基部分具有1至6个碳原子,并且直或分枝; A各自为氢或羟基;和药学可接受的盐及其单独的光学异构体,条件是R1和R2一起形成第二个键在带有R1和R2的碳原子之间或其中R1代表羟基,m为整数0。

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