会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 5. 发明授权
    • Process for the preparation of 1-acyl-4-arylpiperidines
    • 1-酰基-4-芳基哌啶的制备方法
    • US5789596A
    • 1998-08-04
    • US933527
    • 1997-09-18
    • Walter BriedenDidier LoetscherAndrew Naughton
    • Walter BriedenDidier LoetscherAndrew Naughton
    • C07D211/02B01J27/08B01J31/24C07B61/00C07D211/20C07D211/82
    • C07D211/20
    • 1-Acyl-4-arylpiperidines of the general formula: ##STR1## wherein R.sup.1 is an aryl group optionally substituted by one or more C.sub.1-6 -alkyl groups, C.sub.1-6 -alkoxy groups, benzyloxy groups or C.sub.1-6 -alkylthio groups and/or one or more fluorine atoms, and R.sup.2 is a C.sub.1-6 -alkyl group, a C.sub.1-6 -alkoxy group, an optionally substituted aryl group, alkylaryl group or a benzyloxy group optionally substituted on the phenyl radical. The 1-acyl-4-arylpiperidines of formula I are prepared by reacting an arylmagnesium halide with a 1-acylpyridinium halide, obtainable from pyridine and an acyl halide, in the presence of a copper compound to give the corresponding 1-acyl-4-aryl-1,4-dihydropyridine, and hydrogenating the latter. The 1-acyl-4-arylpiperidines are intermediates in the synthesis of pharmaceutical active ingredients, for example, neurokinin receptor antagonists.
    • 具有以下通式的1-酰基-4-芳基哌啶:其中R 1是任选被一个或多个C 1-6 - 烷基,C 1-6 - 烷氧基,苄氧基或C 1-6 - 烷硫基任选取代的芳基 基团和/或一个或多个氟原子,并且R 2是任选在苯基上被取代的C 1-6 - 烷基,C 1-6 - 烷氧基,任选取代的芳基,烷基芳基或苄氧基。 式I的1-酰基-4-芳基哌啶通过在铜化合物的存在下使卤化芳基镁卤化物与可从吡啶和酰基卤获得的1-酰基吡啶鎓卤化物反应来制备,得到相应的1-酰基-4- 芳基-1,4-二氢吡啶,并将其加氢。 1-酰基-4-芳基哌啶是合成药物活性成分例如神经激肽受体拮抗剂的中间体。
    • 6. 发明授权
    • Process for the preparation of 1-Acyl-4-arylpiperidines
    • 1-酰基-4-芳基哌啶的制备方法
    • US5908935A
    • 1999-06-01
    • US80929
    • 1998-05-19
    • Walter BriedenDidier LoetscherAndrew Naughton
    • Walter BriedenDidier LoetscherAndrew Naughton
    • C07D211/02B01J27/08B01J31/24C07B61/00C07D211/20C07D211/82
    • C07D211/20
    • 1-Acyl-4-arylpiperidines of the general formula: ##STR1## wherein R.sup.1 is an aryl group optionally substituted by one or more C.sub.1-6 -alkyl groups, C.sub.1-6 -alkoxy groups, benzyloxy groups or C.sub.1-6 -alkylthio groups and/or one or more fluorine atoms, and R.sup.2 is a C.sub.1-6 -alkyl group, a C.sub.1-6 -alkoxy group, an optionally substituted aryl group, alkylaryl group or a benzyloxy group optionally substituted on the phenyl radical. The 1-acyl-4-arylpiperidines of formula I are prepared by reacting an arylmagnesium halide with a 1-acylpyridinium halide, obtainable from pyridine and an acyl halide, in the presence of a copper compound to give the corresponding 1-acyl-4-aryl-1,4-dihydropyridine, and hydrogenating the latter. The 1-acyl-4-arylpiperidines are intermediates in the synthesis of pharmaceutical active ingredients, for example, neurokinin receptor antagonists.
    • 具有以下通式的1-酰基-4-芳基哌啶:其中R 1是任选被一个或多个C 1-6 - 烷基,C 1-6 - 烷氧基,苄氧基或C 1-6 - 烷硫基取代的芳基和/或 一个或多个氟原子,R 2是任选在苯基上被取代的C 1-6 - 烷基,C 1-6 - 烷氧基,任选取代的芳基,烷基芳基或苄氧基。 式I的1-酰基-4-芳基哌啶通过在铜化合物的存在下使卤化芳基镁卤化物与可从吡啶和酰基卤获得的1-酰基吡啶鎓卤化物反应来制备,得到相应的1-酰基-4- 芳基-1,4-二氢吡啶,并将其加氢。 1-酰基-4-芳基哌啶是合成药物活性成分例如神经激肽受体拮抗剂的中间体。
    • 7. 发明授权
    • Process for preparing optically active 3,3,3-trifluoromethyl-2-alkylpropionic acid derivatives
    • 光学活性3,3,3-三氟甲基-2-烷基丙酸衍生物的制备方法
    • US06599721B2
    • 2003-07-29
    • US09938333
    • 2001-08-23
    • Andrew NaughtonNicholas Shaw
    • Andrew NaughtonNicholas Shaw
    • C12P1302
    • C07C235/06C07B2200/07
    • The invention relates to a novel method for the preparation of optically active 3,3,3-trifluoromethyl-2-alkyl propionic acid derivatives of the general formulae (I) and (II), in which R is ethyl or methyl and X is OH or NH2, provided that if R is methyl X≠—OH. The method comprises the reaction of a racemic propionic acid amide of the general formula (III) either by means of microorganisms which are able to use the propionic acid amide in the form of the racemate or one of its optically active isomers as the only nitrogen source or by means of a polypeptide with amidohydrolase activity which is able to hydrolyze the propionic acid amide. The invention also relates to new optically active representatives of this category of compounds.
    • 本发明涉及一种制备通式(I)和(II)的光学活性3,3,3-三氟甲基-2-烷基丙酸衍生物的新方法,其中R是乙基或甲基,X是OH 或NH 2,条件是如果R是甲基X≠-OH。 该方法包括通过能够使用外消旋体形式的丙酰胺或其旋光异构体之一的微生物作为唯一的氮源,使通式(III)的外消旋丙酸酰胺反应 或通过能够水解丙酸酰胺的具有酰胺水解酶活性的多肽。 本发明还涉及这类化合物的新的光学活性代表。