Synthesis ( IF 2.2 ) Pub Date : 2018-08-20 , DOI: 10.1055/s-0037-1610237 Sergey Ryabukhin 1, 2 , Kostiantyn Melnykov 1, 2 , Dmitriy Granat 1 , Dmitriy Volochnyuk 1, 3 , Oleksandr Grygorenko 1, 2
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Abstract
An approach for the multigram synthesis of 3,3-difluorocyclobutyl-substituted building blocks (including carboxylic acid, amines, alcohols, azide, trifluoroborate ketone) is described. It is shown that, in most cases, ethyl 3,3-difluorocyclobutanecarboxylate is a convenient common synthetic intermediate to obtain the target derivatives. For preparation of 3,3-difluorocyclobutanol or -cyclobutanone, an alternative pathway via reaction of dichloroketene and tert-butyl or benzyl vinyl ether should be applied.
An approach for the multigram synthesis of 3,3-difluorocyclobutyl-substituted building blocks (including carboxylic acid, amines, alcohols, azide, trifluoroborate ketone) is described. It is shown that, in most cases, ethyl 3,3-difluorocyclobutanecarboxylate is a convenient common synthetic intermediate to obtain the target derivatives. For preparation of 3,3-difluorocyclobutanol or -cyclobutanone, an alternative pathway via reaction of dichloroketene and tert-butyl or benzyl vinyl ether should be applied.
中文翻译：
C4 / C5 3,3-二氟环丁基取代的结构单元的多重图合成
摘要
描述了一种3,3-二氟环丁基取代的结构单元（包括羧酸，胺，醇，叠氮化物，三氟硼酸酯）的多谱图合成方法。结果表明，在大多数情况下，3,3-二氟环丁烷甲酸乙酯是获得目标衍生物的方便的常用合成中间体。为了制备3，3-二氟环丁醇或-环丁酮，应采用通过二氯乙烯酮与叔丁基或苄基乙烯基醚反应的替代途径。
描述了一种3,3-二氟环丁基取代的结构单元（包括羧酸，胺，醇，叠氮化物，三氟硼酸酯）的多谱图合成方法。结果表明，在大多数情况下，3,3-二氟环丁烷甲酸乙酯是获得目标衍生物的方便的常用合成中间体。为了制备3，3-二氟环丁醇或-环丁酮，应采用通过二氯乙烯酮与叔丁基或苄基乙烯基醚反应的替代途径。
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