铜催化 1,7-烯炔的级联环化反应生成三氟甲基取代的 1'H-螺[氮杂环丁烷-2,4'-喹啉]-2'(3'H)-酮
Copper-Catalyzed Cascade Cyclization of 1,7-Enynes toward Trifluoromethyl-Substituted 1'H-Spiro[azirine-2,4'-quinolin]-2'(3'H)-ones.
机构信息
State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University , Lanzhou, 730000, P. R. China.
出版信息
Org Lett. 2017 Oct 6;19(19):5186-5189. doi: 10.1021/acs.orglett.7b02453. Epub 2017 Sep 21.
A novel method for the synthesis of trifluoromethyl-containing 1'H-spiro[azirine-2,4'-quinolin]-2'(3'H)-ones by a CF-radical-triggered tandem reaction of benzene-linked 1,7-enynes is described. This protocol utilizes 1-trifluoromethyl-1,2-benziodoxole as the trifluoromethylating reagent and TMSN as the aminating reagent. By this method, various potentially bioactive trifluoromethylated 1'H-spiro[azirine-2,4'-quinolin]-2'(3'H)-ones were facilely synthesized via a radical cascade process.
一种通过苯连接的 1,7-烯炔的 CF-自由基引发的串联反应合成含三氟甲基的 1'H-螺[氮丙啶-2,4'-喹啉]-2'(3'H)-酮的新方法被描述。该方案利用 1-三氟甲基-1,2-苯并碘杂环戊烯作为三氟甲基化试剂，TMSN 作为氨基化试剂。通过这种方法，通过自由基级联过程可以方便地合成各种潜在生物活性的三氟甲基化 1'H-螺[氮丙啶-2,4'-喹啉]-2'(3'H)-酮。
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