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Areno Eindols, preparation method and application as intermediates in the synthesis of products with antitumoral activity

机译:芳烃[E]吲哚,制备方法及在合成抗肿瘤活性产物中的应用

摘要

The areno[e]indols have the formula (I). The methods comprises: (a) reacting (VI) with an aldehyde Ar"--CHO to obtain (VII); (b) oxidizing (VII) to yield the cetone (VIII); (c) reating (VIII) with a strong base and thereafter with an acycle chloride ClCOR, to produce (IX); (d) subjecting to a photochemical cyclization (IX) to produce (I). In said formulas Ar is phenyl or substituted phenyl; Ar' is radical (i) or (ii); R is an acyle group, Ar" is a phenyl, pyrolyl, furanyl or thiophenyl group substituted up to three times by any of the radials R, R. sup.1, R. sup.2, or R.sup.3. The compounds (I) are useful as intermediates in the synthesis of hexahydroareno(e)cyclopropa(c)indol-4- ones with antitumoral activity.
机译:芳族吲哚具有式(I)。所述方法包括:(a)使(VI)与醛Ar” -CHO反应以获得(VII);(b)氧化(VII)以产生丙酮(VIII);(c)以强力反应(VIII)。碱,然后用无环氯化物ClCOR制备(IX);(d)经过光化学环化(IX)制备(I)。在上述式中,Ar是苯基或取代的苯基; Ar'是基团(i)或(ii); R为酰基,Ar”为被R,R.sup.1,R.sup.2或R.sup中的任何一个取代多达三倍的苯基,吡咯基,呋喃基或硫代苯基。 .3。化合物(I)可用作合成具有抗肿瘤活性的六氢areno(e)环丙(c)吲哚-4-的中间体。

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