An improved synthesis of 3-aminoestrone

Abstract An efficient Pd(0)-catalyzed protocol for the rapid and efficient preparation of 3-aminoestrone via 3-benzylaminoestrone from estrone–triflate is described. The three step synthesis proceeds with an overall yield of about 55% using X-Phos as optimal ligand for the Pd(0)-catalyzed Buchwald–Hartwig amination.