In the book, methods for the synthesis of derivatives with a quinoline core are described, which were used in practical medicine in the 21st century. The evolution of the chemistry of medicinal substances is reflected, a modern synthesis strategy for pharmacologically valuable compounds is considered, the methodology of searching for effective medicines among them is highlighted. The main material of the book, the syntheses of potential medicinal substances, is systematized according to the classes and structural groups of chemical compounds. Modern data on the effect of biologically active substances are preseted. The book will be useful for researchers engaged in the field of fine organic synthesis of pharmaceutical chemistry and pharmacology, will also be useful to graduate students and teachers of chemical, pharmaceutical, biological and medical faculties of universities.