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    • 25. 发明授权
    • Method for preparing a pharmaceutically active enantiomeric or
enantiomerically enriched sulfoxide compound by enantioselective
bioreduction of a racemate sulfoxide compound
    • 通过外消旋亚砜化合物的对映选择性生物还原来制备药物活性对映体或对映异构体富集的亚砜化合物的方法
    • US5776765A
    • 1998-07-07
    • US569083
    • 1995-12-18
    • Daniel GrahamRobert HoltPer LindbergStephen Taylor
    • Daniel GrahamRobert HoltPer LindbergStephen Taylor
    • C12P41/00A61K31/44A61K31/4427A61P1/04C07D401/12C12P17/18C12R1/19C12R1/37C12P11/00
    • C07D401/12C12P17/182C12P17/185Y10S435/822Y10S435/849Y10S435/873
    • A compound of formula (II), either as a single enantiomer or in an enantiomerically enriched form ##STR1## wherein: ##STR2## and ##STR3## (wherein N in the benzimidazole moiety of Het.sub.2 means that one of the carbon atoms substituted by any one of R.sub.6 to R.sub.9 optionally may be exchanged for an unsubstituted nitrogen atom; R.sub.1, R.sub.2 and R.sub.3 are the same or different and selected from hydrogen, alkyl, alkoxy optionally substituted by fluorine, alkylthio, alkoxyalkoxy, dialkylamino, piperidino, morpholino, halogen, phenylalkyl, phenylakoxy; R.sub.4 and R.sub.4, are the same or different and selected from hydrogen, alkyl, aralkyl; R.sub.5 is hydrogen, halogen, trifluoromethyl, alkyl, alkoxy; R.sub.6 -R.sub.9 are the same or different and selected from hydrogen, alkyl, alkoxy, halogen, haloalkoxy, alkylcarbonyl, alkoxycarbonyl, oxazolyl, trifluoroalkyl or adjacent groups R.sub.6 -R.sub.9 may complete together with the carbon atoms to which they are attached optionally substituted ring structures; R.sub.10 is hydrogen or alkoxycarbonyloxymethyl; R.sub.11 is hydrogen or forms an alkylene chain together with R.sub.3 ; R.sub.12 and R.sub.13 are the same or different and selected from hydrogen, halogen or alkyl) is obtained by stereoselective bioreduction of a compound of formula (II) in racemic form.
    • PCT No.PCT / SE95 / 01416 Sec。 371 1995年12月18日第 102(e)1995年12月18日PCT PCT 1995年11月27日提交的式(II)化合物作为单一对映异构体或以对映异构体富集形式(II),其中:< IMAGE>和< IMAGE& (其中Het2的苯并咪唑部分中的N表示被R6至R9中任一个取代的碳原子之一任选地可以被替换为未取代的氮原子; R 1,R 2和R 3相同或不同,并且选自 氢,烷基,任选被氟取代的烷氧基,烷硫基,烷氧基烷氧基,二烷基氨基,哌啶子基,吗啉代,卤素,苯基烷基,苯基烷氧基; R4和R4相同或不同,选自氢,烷基,芳烷基; R5是氢, 三氟甲基,烷基,烷氧基; R6 -R9相同或不同,选自氢,烷基,烷氧基,卤素,卤代烷氧基,烷基羰基,烷氧基羰基,恶唑基,三氟烷基或相邻基团R6 -R9可以与它们 任选地替换 环形结构; R 10是氢或烷氧基羰氧基甲基; R 11是氢或与R 3一起形成亚烷基链; R 12和R 13相同或不同,选自氢,卤素或烷基)通过外消旋形式的式(II)化合物的立体选择性生物还原获得。