The development of a safe and effective active pharmaceutical ingredient (API) to be used for addressing a disease is of the utmost importance in the pharmaceutical industry. Oftentimes, the synthetic pathway required for API development involves the genesis of a chiral compound. Asymmetric syntheses are popular routes for generating these kinds of compounds; these reaction routes require a high level of attention for efficient and successful syntheses. Process analytical technology (PAT) provides significant advantages for monitoring, controlling, and assessing synthetic processes directly and in real time. In this review, PAT applications for investigating and improving asymmetric synthetic reactions are discussed. The totality of this effort provides a comprehensive and thorough repository of recent work which has advanced the pharmaceutical field for generating chiral compounds for industrial applications. Display omitted •The generation of safe and effective APIs is crucial in the pharmaceutical industry.•Asymmetric synthetic reactions are commonly used during API development.•PAT provides numerous advantages for monitoring syntheses in real time.•This review covers work since 2012 which uses PAT for monitoring asymmetric reactions.