The leaders of health care organizations are grappling with rising expenses and surging demands for health services. In response, they are increasingly embracing artificial intelligence (AI) technologies to improve patient care delivery, alleviate operational burdens, and efficiently improve health care safety and quality. In this paper, we map the current literature and synthesize insights on the role of leadership in driving AI transformation within health care organizations. We conducted a comprehensive search across several databases, including MEDLINE (via Ovid), PsycINFO (via Ovid), CINAHL (via EBSCO), Business Source Premier (via EBSCO), and Canadian Business & Current Affairs (via ProQuest), spanning articles published from 2015 to June 2023 discussing AI transformation within the health care sector. Specifically, we focused on empirical studies with a particular emphasis on leadership. We used an inductive, thematic analysis approach to qualitatively map the evidence. The findings were reported in accordance with the PRISMA-ScR (Preferred Reporting Items for Systematic Reviews and Meta-Analysis extension for Scoping Reviews) guidelines. A comprehensive review of 2813 unique abstracts led to the retrieval of 97 full-text articles, with 22 included for detailed assessment. Our literature mapping reveals that successful AI integration within healthcare organizations requires leadership engagement across technological, strategic, operational, and organizational domains. Leaders must demonstrate a blend of technical expertise, adaptive strategies, and strong interpersonal skills to navigate the dynamic healthcare landscape shaped by complex regulatory, technological, and organizational factors. In conclusion, leading AI transformation in healthcare requires a multidimensional approach, with leadership across technological, strategic, operational, and organizational domains. Organizations should implement a comprehensive leadership development strategy, including targeted training and cross-functional collaboration, to equip leaders with the skills needed for AI integration. Additionally, when upskilling or recruiting AI talent, priority should be given to individuals with a strong mix of technical expertise, adaptive capacity, and interpersonal acumen, enabling them to navigate the unique complexities of the healthcare environment.