Synthetic organic chemistry - Evil versus Good

Fatal doses of heroin, fentanyl and carfentanil
The world hardly needs a more efficient way to make fentanyl. The last thing the world needs is a list of analogs and the procedures to make them so strong they make fentanyl look like bubble gum. Sadly a published paper gives us both.
Replacing the hydrogen atom (red circle) in fentanyl with what is called a carbomethoxy group (blue circle), you now have carfentanil, which is 20 times more potent than fentanyl and 1000 times more than morphine.
A lethal dose of fentanyl is about one milligram, so a lethal dose of carfentanil would be 50 micrograms. One poppy seed weighs about 0.3 milligrams. So a lethal dose of carfentanil would be approximately one-sixth the weight of a poppy seed.
But even carfentanil isn't even the most potent fentanyl analog out there. That 'honor' belongs to a derivative called ohmefentanyl. Two simple modifications ... the addition of one methyl group and one hydroxyl group (blue circles)— makes the molecule 6.3 times more potent than carfentanil, 126 times more than fentanyl, and 6,300 times more than morphine.

The estimated lethal dose of ohmefentanyl is 0.16 micrograms, which means that one poppy seed's worth (300 micrograms) of ohmefentanyl is enough to kill 1900 people. One ounce (28 grams, 28,000,000 micrograms) would be enough to kill 175 million people.
But organic synthesis has also been responsible for Taxol, a very important cancer drug that treats ovarian and other cancers. The natural source, the bark of the Pacific yew tree could never provide enough of the drug. But chemists figured out a way to make it. Without this important advance, a drug that has saved many thousands of lives would not be available today.

Such is the power of synthetic organic chemistry.
Carfentanil, new player in the opioid war: Elephant tranquilizer
A 10 milligram dose of the animal tranquilizer carfentanil is powerful enough to sedate, even kill, a 15,000-pound African elephant. If diluted sufficiently, a dose of the same size — the fraction of the weight of a paper clip — could also send 500 humans to the morgue. A dose as small as 20 micrograms would be fatal to humans.

Carfentanil is an analog of fentanyl. It is 10,000 times more potent than morphine and 5000 times more potent than pharmaceutical grade (100% pure) heroin, making it one of the most potent known and the most potent commercially used opioid. Carfentanil was first synthesized in 1974. Heroin cut with carfentanil offers a harder-hitting, longer-lasting high and allows dealers a very cheap shortcut to increase their supplies.

Border agents had to don hazmat suits to deal with a one kilogram package of carfentanil
Mounties announced charges against Joshua Wrenn, 24, who was on the receiving end of a one kilogram package of carfentanil shipped from China. The Canadian Border Services Agency and the Royal Canadian Mounted Police said they found the drug hidden in a box labeled as printer accessories. They charged Wrenn with one count of importing a controlled substance and one count of possession for the purpose of trafficking.

The package, authorities said, could have produced 50 million doses.

Joshua Wrenn

Authories display 1 Kg of salt to show how much carfentanil was seized.
Yesterday CNN reported a spike in overdoses in Cincinnati. In New Jersey 29 people overdosed between Tuesday and Thursday in Camden. In Indiana, 13 people overdosed Tuesday in Jennings County alone. In Kentucky 12 people overdosed Wednesday in Montgomery County.

Heroin contaminated with carfentanil was also reported in Florida causing a massive spike in overdoses there.
Like fentanyl, carfentanil can be absorbed through the skin or inhaled, and contact with even a grain could be enough to require medical attention in humans.

Carfentanil is readily available on-line from any number of Chinese suppliers.

Global 'Darkweb' Fentanyl/Carfentanil operation busted in Kelowna
RCMP in Kelowna have uncovered a sophisticated drug-trafficking ring that depended on the dark web and Bitcoin to traffic fentanyl and carfentanil around the world. A 35-year-old man and a 28-year-old woman were arrested after a year-long investigation. Kelowna RCMP worked with authorities from across Canada, the U.S. and Australia on the investigation, dubbed "Project E-Neophile." Upwards of 25 packages suspected of containing fentanyl or carfentanil, destined for Canadian, American, European and Australian cities, were intercepted.
Police also seized two guns, $68,000 US in the digital currency Bitcoin, 120 grams of fentanyl and carfentanil and more than three kilograms of unknown cutting agents.
The powerful opioid carfentanil has claimed another 5 lives in the Minneapolis area.

A 52-year-old inmate, identified as Larance Curtis McMorris is the fourth confirmed death in Milwaukee County from carfentanil.

Carfentanil has killed four people in Maryland in recent weeks. In Alberta there have been 21 deaths in the first three months of 2017 directly attributed to Carfentanil.
Two Sarasota men are behind bars, facing felony drug charges after they sold cops more than 67 grams of Carfentanil. Undercover detectives had coordinated several drug transactions between Michael Sandusky, 23, and Michael White, 28. Detectives later learned what they thought was heroin was actually Carfentanil
Two deadly drugs behind an epidemic of fatalities in the US are now spreading onto British streets, the UK’s National Crime Agency (NCA) has warned. Police believe a spate of deaths in the north of England has been caused by heroin laced with fentanyl and carfentanil. Public Health England has issued a drugs alert in a sign of how concerned police and medical authorities are becoming.

 Four people died in the Barnsley area of South Yorkshire, on April 14 and two men died the day after in Leeds and Normanton in West Yorkshire. Since these six deaths, there have been similar fatalities recorded by Humberside and Cleveland Police.
On Tuesday, public health officials confirmed the first cases of overdose deaths from carfentanil in New Hampshire.
Maryland officials said that three people have died of overdoses of the synthetic drug carfentanil. One day after announcing Wisconsin's first death attributed to carfentanil the county's medical examiner said the drug is to blame for two more deaths in Milwaukee. In Illinois carfentanil has killed two in Sangamon County in the past two weeks. Carfentanil was found near the scene of a pair of fatal drug overdoses in Colorado. In Minnesota authorities said that carfentanil is to blame for five recent overdose deaths. In South Carolina another two deaths have recently been confirmed.
Throughout the U.S., carfentanil is being found in cocaine, counterfeit pills, methamphetamine, heroin and other drugs. It can also be found in liquid form.

The situation is the same in Canada. Carfentanil was seized during a drug bust in Hinton. Inmates have been overdosing at Drumheller Institution from carfentanil. Carfentanil has been detected in Port Alberni and the Alberni Valley. It has appeared in drugs seized north of Toronto in Richmond Hill.
Last September, the U.S. Drug Enforcement Agency issued a warning to law enforcement about carfentanil. Those warnings are proving frighteningly accurate.

Carfentanil is 100 times deadlier than fentanyl, which is 50 times deadlier than heroin.
Carfentanil is marketed under the brand name Wildnil. For years, the drug rested on the shelves of zoologists and veterinarians specializing in large animals. It's a uniquely powerful sedative. There is and never has been any human use for carfentanil.

Carfentanil is being created in clandestine laboratories in China, which has no controls on the drug. Several months ago the Associated Press found a dozen Chinese businesses that said they would export carfentanil for as little as $2,750 per kilogram. One kilogram is sufficient for 50 million doses. The U.S. Department of Defense identified it years ago as a potential weapon in the hands of enemy nations.
In Akron, Ohio, medical examiner Dr. Lisa Kohler has seen over 50 people die from carfentanil since July. Most US emergency doctors had never heard of carfentanil before it showed up in Ohio. It is 10,000 times more potent than morphine, and a grain of it, 20 micrograms, can kill a human. It was aerosolized by Russian special forces in 2002 when Chechen rebels took hostages in a Moscow theater, where it killed over 100 hostages along with the terrorists.

Police in Canada will begin carrying naloxone, not to aid overdose victims, but for officers that come in contact with it. Public health teams across North America are distributing naloxone kits. But there’s one problem; carfentanil is so toxic, naloxone might not work. Police Lieutenant Rick Edwards says his officers are “giving 4–8 doses of naloxone just to get a response.”
1) Fentanyl and carfentanil are being cut into powder cocaine — a drug used by individuals who don’t fit the usual mold of a typical addict.

2) Some first responders are reporting the need to use 10–16 milligrams of naloxone. A typical heroin overdose dosage is 2 milligrams.

3) Doctors can't wait for naloxone to work. In the past people who overdosed on heroin would wake up after a dose of naloxone within minutes. Now those minutes could mean death if Carfentanil is involved. Ventilations are required, and possibly chest compressions as well.

4) Carfentanil causes cardiovascular collapse, (failure of circulation) in addition to hypoventilation (breathing at an abnormally slow rate) and hypoxia, (deficiency in the amount of oxygen reaching tissues) necessitating advanced life support.

5) Residue is dangerous. Personal protective equipment is required around drug paraphernalia.

Russian soldiers carry hostages from the Dubrovka theatre, October 2002
See ----->
See ----->

Carfentanil $2,750 US per kilogram in China
Carfentanil had been detected in the deaths of two men in their 30s, one in the Edmonton area and the other in Calgary. Carfentanil is an analog of the synthetic opioid fentanyl, which is being increasingly cut into the illicit drug supply. Fentanyl was detected in 60 per cent of 488 illicit-drug overdose deaths in B.C. in the first eight months of 2016.

Carfentanil is 100 times deadlier than fentanyl, 10,000 times deadlier than morphine. “An amount as small as a grain of sand could be lethal,” the government of Alberta said.
Carfentanil was responsible for two overdoses in Winnipeg late last month, according to firefighters in that city. In Hamilton County, Ohio there were more than 96 heroin overdoses and three deaths in under a week in late August. In nearby East Liverpool, the Ohio police department shared a photo of two adults who had overdosed in their car with a four-year-old child in the back.
In Ohio’s Cuyahoga County there were 14 opioid related overdoses in the first week of September, two of which were directly related to carfentanil.
In 2014, US authorities seized 3.7kg of fentanyl. This year, until mid-July, they have seized 134.1kg. Fentanyl is the most frequently seized synthetic opioid, US Customs reports. In China carfentanil is not a controlled substance and it can be manufactured legally and sold openly online.

"We can supply carfentanil . for sure" a saleswoman from Jilin Tely Import and Export Co said. "And it's one of our hot sales product."
Carfentanil Bust in Miami-Dade highlights growing crisis

Carfentanil seizure in Vancouver in August
Miami-Dade police narcotics detectives and FBI agents on Friday raided the home of a carfentanil dealer. The FBI’s Technical Hazards Response Unit donned Hazmat suits to search the dealer’s South Miami-Dade home. Users have injected, ingested or snorted the drug with no such protection.

Carfentanil has been detected in the bodies of at least 107 people who died of overdoses this year, according to data by the Miami-Dade Medical Examiner’s Office. That number is considered low as lab results are still pending from others. The U.S. DEA issued a public warning in September. “Carfentanil is surfacing in more and more communities. We see it on the streets, often disguised as heroin. It is crazy dangerous.”
Across South Florida, opioids — heroin, fentanyl and its synthetic cousins — have been increasingly detected in the bodies of hundreds of overdose victims in the past two years. Many users believe they are taking heroin, and don’t realize it has been cut with fentanyl, carfentanil or other very cheaply made synthetics. Cartfentanil cases did not begin showing up in Miami-Dade until around July.

Ingesting just a few granules of carfentanil can be lethal. It can also be readily absorbed through the skin. It is by far the most deadly of the opiates available on the street. At the present time there are no restrictions on the drug in China, it's point of manufacture.