Preparation of benzosuberonylpiperidine compounds

   
   

Diastereoselective and enantioselective synthetic routes for the preparation of compounds of formula (I): 1 or derivatives thereof, wherein: R is C.sub.1-6alkyl, C.sub.3-7cycloalkyl, C.sub.1-6alkoxy, hydroxy, halo, C.sub.1-6alkenyl, C.sub.1-6alkynyl, amino, C.sub.1-6alkylamino, di(C.sub.1-6alkyl)amino, hydroxyC.sub.1-6alkyl, C.sub.1-6alkoxyC.sub.1-6a- lkyl, arylC.sub.1-6alkoxy, heteroarylC.sub.1-6alkoxy, aminoC.sub.1-6alkyl, (C.sub.1-6alkyl)aminoC.sub.1-6alkyl, di(C.sub.1-6alkyl)aminoC.sub.1-6alky- l, arylC.sub.1-6alkylamino, heteroarylC.sub.1-6alkylamino; R.sup.1 is hydrogen or R; R.sup.2 is hydroxy, C.sub.1-6alkoxy, amino, C.sub.1-6alkylamino, di(C.sub.1-6alkyl)amino; R.sup.3 and R.sup.4 are each independently selected from the list consisting of perhaloC.sub.1-6alkyl, hydrogen, halo, C.sub.1-6alkyl, C.sub.1-6alkoxy, hydroxy, amino, C.sub.1-6alkylamino, di(C.sub.1-6alkyl)amino, hydroxyC.sub.1-6alkyl, C.sub.1-6alkoxyC.sub.1-6a- lkyl, aminoC.sub.1-6alkyl, (C.sub.1-6alkyl)aminoC.sub.1-6alkyl, di(C.sub.1-6alkyl)aminoC.sub.1-6alkyl, aryl, and COX wherein X may be hydroxy, C.sub.1-6alkoxy, C.sub.1-6alkyl, amino, C.sub.1-6alkylamino, or di(C.sub.1-6alkyl)amino; and wherein any alkyl group or the alkyl moiety of any group containing such a moiety may be substituted one or more times by halo.

Diastereoselective и enantioselective трассы синтетики для подготовки смесей формулы (i): 1 или производные thereof, при котором: Р будет C.sub.1-6Јalkyl, C.sub.3-7cycloalkyl, C.sub.1-6Јalkoxy, окси, венчик, C.sub.1-6Јalkenyl, C.sub.1-6Јalkynyl, амино, C.sub.1-6Јalkylamino, di(C.sub.1-6Јalkyl)amino, hydroxyC.sub.1-6Јalkyl, lkyl C.sub.1-6ЈalkoxyC.sub.1-6Јa-, arylC.sub.1-6Јalkoxy, heteroarylC.sub.1-6Јalkoxy, aminoC.sub.1-6Јalkyl, (C.sub.1-6Јalkyl)aminoC.sub.1-6Јalkyl, di(C.sub.1-6Јalkyl)aminoC.sub.1-6Јalky- л, arylC.sub.1-6Јalkylamino, heteroarylC.sub.1-6Јalkylamino; R.sup.1 будет водоподом или р; R.sup.2 окси, C.sub.1-6Јalkoxy, амино, C.sub.1-6Јalkylamino, di(C.sub.1-6Јalkyl)amino; R.sup.3 и R.sup.4 каждое независимо выбранное от списка consist of perhaloC.sub.1-6Јalkyl, водопод, венчик, C.sub.1-6Јalkyl, C.sub.1-6Јalkoxy, окси, амино, C.sub.1-6Јalkylamino, di(C.sub.1-6Јalkyl)amino, hydroxyC.sub.1-6Јalkyl, lkyl C.sub.1-6ЈalkoxyC.sub.1-6Јa-, aminoC.sub.1-6Јalkyl, (C.sub.1-6Јalkyl)aminoC.sub.1-6Јalkyl, di(C.sub.1-6Јalkyl)aminoC.sub.1-6Јalkyl, арил, и COX при котором х может быть окси, C.sub.1-6Јalkoxy, C.sub.1-6Јalkyl, амино, C.sub.1-6Јalkylamino, или di(C.sub.1-6Јalkyl)amino; и при котором любая алкиловая группа или алкиловый moiety любой группы содержа такой moiety могут быть заменены one or more времена венчиком.

 
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