Steviol is a diterpene first isolated from the plant Stevia rebaudiana in 1931.

[3] The aglycon is prepared by enzymatic hydrolysis, since upon acid treatment steviol will undergo Wagner-Meerwein rearrangement to the very stable isosteviol.

In Stevia rebaudiana, the biosynthesis of steviol is confined to green tissues.

The precursors of steviol are synthesized via the non-mevalonate pathway located in plant cell plastids, which produces isopentenyl pyrophosphate (IPP) and dimethylallyl pyrophosphate (DMAPP).

GPDP is made into a cyclic compound, copalyl diphosphate (CDP), by CDP synthase, after which kaurene is produced by another cyclization catalyzed by kaurene synthase.