Carl Djerassi was inducted into the Inventors Hall of Fame in 1978 for his discovery of oral contraceptives (U.S. Patent number 2,744,122; filed November 22, 1951). He considered his two years at Syntex (1949-1951) "among the most productive ones of my chemical career," since less than half a year after his synthesis of cortisone, he synthesized the first oral contraceptive.

In 1921, Ludwig Haberlandt, an Austrian endocrinologist, proposed that extracts of corpus luteum (Latin for "yellow body"), which produces progesterone, a steroid hormone involved in the female menstrual cycle and the embryogenesis in the body of humans and other species, could be useful for birth control. It was only weakly active when taken orally, so daily injections were needed. Paul Ehrlich established relationships between biological activity and chemical structure that enabled scientists to predict which drugs might be useful.

Using these principles as guidelines, Djerassi, George Rosenkranz, and their team sought to modify the progesterone molecule to form an orally active substance with its biochemical properties. On October 15, 1951, Luis Miramontes, their young undergraduate chemistry student, synthesized 19-nor-17alpha-ethynyltestosterone (generic norethisterone). Several weeks later, the team filed their patent application for this compound that became one of the first ovulation-inhibiting ingredients of oral contraceptives. Djerassi reported their results at the April, 1952, American Chemical Society meeting in Milwaukee, Wisconsin, and they published their article three years later in the Journal of the American Chemical Society. After clinical studies by Gregory Pincus and others, the U.S. Food and Drug Administration (FDA) approved the use of norethindrone, now one of the world's most widely used steroid contraceptives. According to Djerassi, if these drugs had been discovered two decades later, they would not have been approved because of more stringent FDA regulations.

In view of the pill's extensive use, considerable clinical research on possible side effects made it the most intensively studied drug in modern medicine. By the close of the 1960's, evidence of an increased risk for strokes, cardiovascular disease, and blood clots were ignored but were later exaggerated. The risks were reduced considerably by decreasing the amounts of the progestin and estrogen components, and the pill was found to reduce the risk of ovarian and endometrial cancers. For healthy young women, the benefits of the pill more than outweigh any risks, making it the most effective and probably the safest contraceptive.

An ardent feminist since his third marriage, Djerassi has described himself as the pill's mother and Gregory Pincus, who "fertilized" norethindrone, as the pill's father.

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