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We report a copper-promoted three-component difluoroalkylative alkynylation of [3.1.1]propellane with terminal alkynes and bromodifluoroacetates, enabling simultaneous installation of a gem-difluoro group and a versatile alkyne handle at the bridgehead. This one-step transformation provides modular access to difunctionalized BCHep scaffolds under mild conditions with broad functional group tolerance and offers opportunities for late-stage diversification of complex molecules.<\/jats:p>","DOI":"10.1021\/acs.joc.6c01371","type":"journal-article","created":{"date-parts":[[2026,8,22]],"date-time":"2026-08-22T20:48:38Z","timestamp":1787431718000},"page":"12113-12119","source":"Crossref","is-referenced-by-count":0,"title":["Three-Component\nDifluoroalkylative Alkynylation of\n[3.1.1]Propellane Enables Modular Bicyclo[3.1.1]heptane Synthesis"],"prefix":"10.1021","volume":"91","author":[{"given":"Pan","family":"Huang","sequence":"first","affiliation":[{"name":"Yangzhou University , , Siwangting Road 180 , ,","place":["Yangzhou, China, 225002"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Huifang","family":"Ma","sequence":"additional","affiliation":[{"name":"Yangzhou University , , Siwangting Road 180 , ,","place":["Yangzhou, China, 225002"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Lianmin","family":"Yang","sequence":"additional","affiliation":[{"name":"Guangxi University of Science and Technology , , Liushi Road 257 , , ,","place":["Liuzhou, Guangxi, China, 545006"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Shuli","family":"Wang","sequence":"additional","affiliation":[{"name":"Yangzhou University , , Siwangting Road 180 , ,","place":["Yangzhou, China, 225002"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Shuwei","family":"Zhang","sequence":"additional","affiliation":[{"name":"Yangzhou University , , Siwangting Road 180 , ,","place":["Yangzhou, China, 225002"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Duo","family":"Zhang","sequence":"additional","affiliation":[{"name":"Guangxi University of Science and Technology , , Liushi Road 257 , , ,","place":["Liuzhou, Guangxi, China, 545006"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-4487-1820","authenticated-orcid":true,"given":"Guodong","family":"Zhang","sequence":"additional","affiliation":[{"name":"Guangxi University of Science and Technology , , Liushi Road 257 , , ,","place":["Liuzhou, Guangxi, China, 545006"]}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"316","published-online":{"date-parts":[[2026,8,21]]},"reference":[{"issue":"11","key":"2026090408101723600_cit1","doi-asserted-by":"publisher","first-page":"2839","DOI":"10.1039\/C8OB02812E","article-title":"Saturated\nBioisosteres of Benzene: Where to Go Next?","volume":"17","author":"Mykhailiuk","year":"2019","journal-title":"Org. 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