Chemical Milestone

Ever since the almost magical therapeutic properties of cortisone were recognized in 1948, one of the most extensive research programs in medical history has been aimed at finding a real supply of the new wonder drug. The only known way of producing it is through an intricate chemical process of 30-odd steps starting with cattle bile. And the yield is so small that several dozen head of cattle are needed to produce one average daily dose for one patient. But last week Harvard's Professor Robert B. Woodward announced that he had reached the first milestone on the road to making synthetic cortisone from simple chemicals.

Like other steroid hormones (e.g., testosterone, androsterone, progesterone), cortisone is a tough chemical customer. Its molecules are built around the steroid nucleus" (TIME, Jan. 29) which has three six-atom carbon rings and one five-atom ring in the proper spatial arrangement. To build such a molecule from scratch was considered so difficult that few chemists ever hoped to accomplish it.

Woodward started out with orthoto-luidine, an oily liquid extracted from coal tar, whose molecule has one six-carbon ring and one methyl (CH3) group. Step by step he attached more atoms, carefully choosing his reactions so that the atoms would fall in the proper places. After some 20 laboratory steps, his 22 Ibs. of original raw materials were reduced to 1/28 oz. of a genuine steroid. The compound's molecule has the steroid nucleus with an oxygen atom attached at one end and a carbome-thoxy (C02CH3) group at the other.

Chemist Woodward emphasized the fact that his new substance is not yet cortisone. He must add another oxygen atom in the proper spot, and must exchange his carbomethoxy group for a dihydroxyacetone sidechain. In the process it will also be necessary to alter the double bonds that now join some of the atoms in his steroid (see diagram). But Chemist Woodward's cautious colleagues agree that the toughest part of the job seems to be over.

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