The novel synthesis of 3-aminopropyl dihydrogen phosphate(3-APPA; 3-Aminopropane phosphoric acid), and its applicability to the skin as a cosmetic raw material in terms of its efficacy and toxicology were presented. The phosphorylation of 3-amino-1 -propanol was carried out via cyclization into 6-mem- bered 2,6-oxaza-phosphoryl ring in the presence of phosphorous oxychloride and an organic base. The subsequent ring-opening hydrolysis and crystallization afforded the highly purified product in 90% isoloated yield. The method is much superior to the previous literature phosphorylation methods, as the procedure is simple and high- yielding. To confirm the efficacy of 3-APPA, several activities related to anti-aging capacity were measured. In-vitro human fibroblast, linear and 3-dimensional collagen matrix culture revealed that 3-APPA stimulated the proliferation of fibroblasts, and enhanced the synthesis of collagen, which showed 3-APPA’s potency for skin wrinkle reduction. The toxicological aspect of 3-APPA was also extensively examined. In vivo toxicity tests such as acute oral toxicity, eye irritation, human patch, and the repeat insult human patch test proved 3-APPA to be a safe material. Thus 3-APPA can be used as an effective anti-aging agent for various cosmetic formulations.