Natural compounds, such as polyketides, are considered a treasure trove of pharmaceuticals, having paved the way for saving millions of lives and improving public health. However, their complex structures have made it extremely difficult to synthesize them efficiently in pharmacologically useful quantities. We have successfully synthesized bastimolide A, a potent antimalarial candidate, in scalable and environmentally friendly manner. Our synthetic route can produce bastimolide A in 21 steps with an overall yield of 15.4% by using chiral Brønsted acid-catalyzed enantio- and diastereoselective allylborations as key steps. This "efficient and scalable" synthetic route significantly will advance the understanding of bastimolide A's biological properties and the feasibility of its future pharmaceutical development.
