Steroids contraceptive synthesis development

The 1950s and 1960s saw the development of orally active progestins based on the synthesis of steroids that lack the C19-angular methyl substituent (19-norsteroids). The commercial production of these compounds for the regulation of menstmal disorders began in 1957, and for oral contraception in 1960. 

Dr. Bill Coleman, for several chemical steps in Syntex s synthesis of the oral contraceptive chlormadinone. With Haldor Christensen, sodium dispersion chemistry led to a superior process for the manufacture of the Eh Lilly herbicide, diphenamid. We devised novel patented chemistry, with the inspiration of Dr. Martin Hultquist, for the manufacture of DDQ. The list could go on and on, but the essence is that in Arapahoe we became chemical process development chemists. We learned that there were no such chemists as steroid chemists, organometallic chemists, heterocyclic chemists, and so on. There are only process development chemists, capable of synthesizing anything. Being scientists in a small company we also learned to accommodate other disciplines and business requirements in creating our chemical processes. 

As indicated earlier, plant products can be useful as starting materials for the semisynthetic preparation of other drugs. An important example in this regard is the Mexican yam, which produces a steroid precursor (diosgenin) vital to the synthesis of steroidal hormones used in oral contraceptives (i.e., progesterone). The availability of diosgenin eliminates numerous expensive steps in the organic synthesis of the basic steroid molecule. It was this discovery that contributed to the development of the pharmaceutical company Syntex (now a subsidiary of Hoffman LaRoche) and the development of the first birth control pill. 

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