α-Methylfentanyl was initially discovered by a team at Janssen Pharmaceutica in the 1960s. In 1976, it began to appear mixed with “china white” heroin as an additive. It was first identified in the bodies of two drug overdose victims in Orange County, California, in December 1979, who appeared to have died from opiate overdose but tested negative for any known drugs of this type. Over the next year, there were 13 more deaths, and eventually the responsible agent was identified as α-methylfentanyl.
A bag of “China White” α-methylfentanyl.
α-Methylfentanyl was placed on the Schedule I list in September 1981, only two years after its appearance on the street, but already other analogs were being developed. Following the appearance of α-methylfentanyl on the market, over ten new analogs of fentanyl have been reported, starting with para-fluorofentanyl, followed by α-methylacetylfentanyl, then by the highly potent 3-methylfentanyl, and subsequently by many others such as β-hydroxyfentanyl, ohmefentanyl, β-hydroxythiofentanyl and β-hydroxy-4-methylfentanyl. The development of such a wide structural family of novel narcotic drugs was a major factor responsible for the implementation of the Federal Analog Act which for the first time attempted to control entire families of drugs based on their structural similarity rather than scheduling new drug analogs individually as each appeared.
In 1991, a group of Russian chemistry students discovered a simplified synthesis route which used phosgene instead of phenethylamine. Soon, abuse of the drug became widespread, causing a tenth of overdoses in the Moscow region. α-Methylfentanyl became notorious for low safety