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Herein, we describe a visible-light-mediated multicomponent coupling of azabicyclo[1.1.0]butanes (ABBs), alkenes, and N-activating electrophiles, which provides a general and modular strategy for the rapid assembly of pharmaceutically interesting yet synthetically challenging azetidine-containing spirocycles in a single step. This practical protocol features a broad substrate scope, high functional group compatibility, operational simplicity, scalability, and excellent chemoselectivity and regioselectivity. Its versatility is demonstrated by the late-stage modification of pharmaceutically relevant molecules, diverse downstream derivatizations, and the synthesis of bioisosteric analogues of bioactive molecules.<\/jats:p>","DOI":"10.1021\/acs.orglett.6c04136","type":"journal-article","created":{"date-parts":[[2026,10,5]],"date-time":"2026-10-05T08:02:08Z","timestamp":1791187328000},"page":"13116-13122","source":"Crossref","is-referenced-by-count":0,"title":["Visible-Light-Mediated Multicomponent Strain-Release-Driven\nSynthesis of Highly Functionalized Spiroazetidines"],"prefix":"10.1021","volume":"28","author":[{"given":"Kaiqiang","family":"Tian","sequence":"first","affiliation":[{"name":"China Pharmaceutical University , , , ,","place":["Nanjing, China, 210009"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Huimin","family":"Dong","sequence":"additional","affiliation":[{"name":"China Pharmaceutical University , , , ,","place":["Nanjing, China, 210009"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ye","family":"Wu","sequence":"additional","affiliation":[{"name":"China Pharmaceutical University , , , ,","place":["Nanjing, China, 210009"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-7042-2397","authenticated-orcid":true,"given":"Bo","family":"Zhang","sequence":"additional","affiliation":[{"name":"China Pharmaceutical University , , , ,","place":["Nanjing, China, 210009"]}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"316","published-online":{"date-parts":[[2026,10,5]]},"reference":[{"key":"2026101608464699400_cit1a","doi-asserted-by":"publisher","first-page":"3673","DOI":"10.1016\/j.bmcl.2014.06.081","article-title":"The Use of Spirocyclic\nScaffolds in Drug Discovery","volume":"24","author":"Zheng","year":"2014","journal-title":"Bioorg. 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