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Herein, we report an energy\u2010transfer\u2010enabled strategy for the synthesis of 2\u2010substituted BCPs via strain\u2010release triplet carbene addition to bicyclo[1.1.0]butanes (BCBs). This method employs readily accessible diazoacetates and a diverse set of BCBs under mild blue\u2010light irradiation, providing direct access to 1,2,3\u2010trisubstituted BCPs. Key advantages include the modular installation of versatile bridge ester substituents, enabling downstream diversification, while retaining the bridgehead substituents from the BCB precursor. The synthetic utility is further demonstrated through the preparation of BCP analogues of bioactive fragments. Combined experimental and DFT studies support a mechanism involving photoinduced energy transfer to generate a triplet carbene, followed by stepwise addition across the highly strained C\u2500C \u03c3 bond of the BCB framework.\n                  <\/jats:p>","DOI":"10.1002\/anie.202518508","type":"journal-article","created":{"date-parts":[[2025,11,7]],"date-time":"2025-11-07T08:40:33Z","timestamp":1762504833000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":12,"title":["Modular Access to sp\n                    <sup>3<\/sup>\n                    \u2010Rich Bicyclo[1.1.1]pentane Bioisosteres via Energy\u2010Transfer\u2010Mediated Carbene Insertion"],"prefix":"10.1002","volume":"65","author":[{"given":"Liang","family":"Yi","sequence":"first","affiliation":[{"name":"KAUST Catalysis Center (KCC) King Abdullah University of Science and Technology (KAUST)  Thuwal 23955\u20106900 Saudi 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