OSR: Fuel For Thought · 2010-07-07 16:00

A new paper published in the June 2010 issue of the energy industry journal Fuel — Aqueous mercury precipitation with the synthetic dithiolate, BDTH2 — provides a comprehensive description of the chemical properties and manner of synthesis of the chelator developed for the purpose of toxic waste remediation that has been marketed since 2008 as a “dietary supplement” under the trade name OSR#1.

Co-authors Lisa Y. Blue, Partha Jana and David A. Atwood, are affiliated with the Department of Chemistry of the University of Kentucky; Blue and Atwood are also affiliated with Merloc LLC, a start-up company which has licensed the University of Kentucky’s patents for multidentate sulfur-containing ligands for binding heavy metals for waste management and environmental cleanup applications.

Boyd Haley, Ph.D., University of Kentucky Professor Emeritus, former head of the University’s Department of Chemistry, and a prominent, long-time proponent of the hypothesis that autism is a conseqence of vaccine-mediated mercury poisoning, has licensed the same patents from the University, which in 2007 described the purpose of their license to Haley as “development of water soluble chelators.”

Until early 2008, Prof. Haley made numerous public references to his development of a “new chelator,” and his intention to submit it to the U.S. Food & Drug Administration’s Investigational New Drug approval process. However, in early 2008 he discontinued referring to it as a chelator, and filed a notice of intent “to introduce a new dietary ingredient for use as an antioxidant… into interstate commerce.” He has since dubbed the product “OSR,” has steadfastly referred to it as an “antioxidant,” and has refused to publicly discuss its action as a chelator. In spite of an FDA notice indicating that he had failed to establish the OSR and its components have “any established use as a food for human beings,” and that he had failed to demonstrate that OSR could reasonably be expected to be safe, Prof. Haley has aggressively promoted OSR, focusing largely on the market consisting of parents of autistic children.

OSR#1 is now the subject of a recent warning letter from the FDA, indicating that it is not a “dietary ingredient,” but an inadequately tested, inadequately labeled, unapproved drug, with toxic effects demonstrated in Prof. Haley’s own unpublished studies.

Aqueous mercury precipitation with the synthetic dithiolate, BDTH2 requires a solid grounding in chemistry to be fully understood. The following excerpts nonetheless provide both the lay and professional reader a far more straightforward description of Prof. Haley’s drug than anything provided by Prof. Haley himself, his business associates, or the network of “alternative health care practitioners” who are sharing in the profits from its sale.

Excerpts & Commentary

(All emphasis and subtitles added)

Blue, Lisa Y., Partha Jana, and David A. Atwood
Aqueous mercury precipitation with the synthetic dithiolate, BDTH2
Fuel, Vol. 89, No. 6 (June 2010): 1326-1330.
http://dx.doi.org/10.1016/j.fuel.2009.10.031

Abstract

“BDTH2, 1,3-benzenediamidoethanethiol (common name) and closely related derivatives were specifically designed to become insoluble after the formation of linear, covalent bonds to aqueous mercury. BDTH2 (IUPAC nomenclature, N,N′-bis(2-mercaptoethyl)isophthalamide) emerged as the preeminent reagent for the complete precipitation of mercury from water after several years of studies with a wide range of compounds having one, two, three, and four thiol groups. BDTH2 does not become inactive through oxidation to disulfide and can be applied to mercury-containing water as acidic, basic, and ethanolic solutions. The BDT–Hg precipitate is extremely stable and leaches low-ppm levels of mercury only under extremely acidic and basic conditions. BDTH2 is also effective in the aqueous precipitation of other soft, divalent metals, such as copper, cadmium, lead, and the main group elements, arsenic and selenium. The insolubility of the BDT–M compounds can be attributed to the presence of strong, non-polar, covalent M–S bonding within a water-insoluble organic framework. BDTH2 has no known biological toxicity and is being sold as a nutritional supplement under the trade name OSR-1. This review describes the chemistry, precipitation, and leaching studies of BDTH2 with mercury.”

This is what Prof. Haley’s “dietary supplement” was designed to do:

“BDTH2 represents an inexpensive, very effective means of precipitating soft metals from water and produces solids that will not release the metal after disposal.”
“After discovering that the problems associated with [common commercial metal precipitation] reagents made them relatively ineffective, we began a systematic search for thiol-containing compounds capable of removal [of] soft heavy metals, and in particular, mercury, from water. This entailed the syntheses of new bidentate, tridentate and tetradentate thiols having the following general properties:
(1) stoichiometric precipitation of Hg(II) to low ppb levels,
(2) covalent Hg–S bonding,
(3) insolubility and stability of metal compounds under acidic and basic conditions,
(4) absence of disulfide formation,
(5) thermal stability,
(6) ease of preparation,
(7) low cost,
(8) no biological toxicity.”
“This approach met with some success in the preparation of a wide range of new thiol compounds, including BDTH2 and tetradentate thiols potentially capable of forming tetrahedral mercury compounds. BDTH2 emerged as the ideal reagent for aqueous Hg(II) removal (BDTH2 is the abbreviation derived from the common name 1,3-Benzene Diamido ethane Thiol; the IUPAC nomenclature is N,N0-bis(2-mercaptoethyl)isophthalamide).”
“BDTH2 is effective in precipitating mercury through the formation of covalent Hg–S bonds under a variety of laboratory conditions, from gold mining effluent, from soils and for low ppb field samples from a former chlor-alkali facility. BDTH2 is also effective in precipitating other divalent metals such as Fe, Cu, Cd, and Pb, metal removal from acid mine drainage, for the prevention of metal leaching from coal and sulfide minerals and for the removal of lead from lead-battery recycling effluent.”

This is how Prof. Haley’s “dietary supplement” is synthesized:

“This general procedure can be scaled to prepare smaller or larger amounts of BDTH2. Triethylamine (TEA; 52 mL, 38 g, 375.53 mmol) in chloroform (100 mL) is added slowly to a stirring solution of cysteamine hydrochloride (21.20 g, 186.6 mmol) in chloroform (200 mL) in a 3 L round-bottom flask with a nitrogen stream passed over the mouth of the vessel. The reaction mixture is stirred magnetically with a 1 in. Teflon stir bar. Isophthaloyl dichloride (12.48 g, 61.48 mmol) in chloroform (100 mL) is then added to the solution and allowed to stir for 12 h. At the end of the reaction time, the solution is clear violet in color. The chloroform solution is washed with a 10% HCl solution (500 mL x 2, VWR) in a 2 L separatory funnel. The chloroform layer is transferred to a 1 L Erlenmeyer flask and dried by stirring over sodium sulfate (Na2SO4) for 1 h and filtered. Nitrogen is passed over the solution to evaporate the solvent and induce precipitation of the product. The product is allowed to dry further, open to air, for one day before characterization by melting point, IR, 1H NMR and MS. Yield without optimization: 12.51 g (72%).”

This is what it costs Prof. Haley to manufacture the active ingredient of his “dietary supplement” in small quantities:

“The cost of BDTH2 using laboratory reagents is less than $0.25/g. BDTH2 will be inexpensive when produced in large quantities.”

(According to several retailer websites, 30 100mg capsules of OSR — that is, 3 grams of OSR — cost from $60, or $20/gram, to $105, or $35/gram — a markup of 8,000% to 14,000%. The cost of developing the chelator was largely shouldered by the University of Kentucky. Even factoring in the cost of fillers, capsules, packaging, marketing, business and legal expenses, these figures point to a profit potential that equals or exceeds that enjoyed by mainstream drug manufacturers — all without the fuss and expense involved in conducting proper clinical trials on adult human beings prior to putting the substance on the market for consumption by disabled children. According to Dr. Jerry Kartzinel, over one million capsules of OSR have been sold to date. The profits from the sales of this inadequately tested, unapproved new drug are shared by Prof. Haley, his business associates, and the cadre of doctors, dentists and online retailers who serve as his marketing team.)

This is the extent to which those involved in the promotion and sale of BDTH2/OSR#1 have documented its alleged “non-toxicity”:

“For information regarding the commercial use of BDTH2, now being marketed under the Tradename ‘‘B9”, contact: Inquiries@MerlocLLC.com. Another significant advantage of BDT by comparison to other mercury treatment technologies is that it is non-toxic. This has been demonstrated in animal toxicity (acute oral, subchronic oral, in utero) and mutagenicity studies. Indeed, BDTH2 is currently being sold by CTI Science, Inc. under the Tradename OSR#1 as a nutritional supplement.”

(Both the authors and Prof. Boyd Haley have a powerful economic interest in characterizing their product as “benign,” with no potential for adverse effects if consumed by human beings. However, although the authors cite 46 references in this paper, none are provided to support their assertion that BDTH2/OSR#1 is “non-toxic.” Although it is likely that they have had privileged access to the unpublished animal toxicity and mutagenicity studies commissioned by Prof. Haley — that is, those cited in the FDA’s June 17, 2008 opinion letter and June 17, 2010 warning letter as indicative of toxicity — they do not provide citations for those studies, or for any other studies that might substantiate this claim.)

Due to copyright regulations, I am unable to provide unrestricted access to the full-text article. Readers are welcome to request a copy for their own, non-commercial use via the comments entry form.


All articles about OSR on Neurodiversity Weblog:

Haley’s Chelator: For Cats Or For Kids? (April 26, 2008)
A Fine White Powder (August 1, 2008)
The Industrial Treatment (August 8, 2008)
An Inquiry Emerges (August 14, 2008)
FDA To Haley: OSR#1 A Misbranded, Mislabeled, Unsafe Drug (June 24, 2010)
OSR: Fuel For Thought (July 7, 2010)
OSR: A Bevy Of Adverse Events (July 12, 2010)
OSR: The Littlest Consumers (July 14, 2010)

Articles about OSR in The Chicago Tribune:

OSR#1: Industrial chemical or autism treatment? (January 17, 2010)
FDA warns maker of product used as alternative autism treatment (June 23, 2010)
Supplement seller says FDA may be ‘confused’ (July 12, 2010)

Comments


  1. “This general procedure can be scaled to prepare smaller or larger amounts of BDTH2. Triethylamine (TEA; 52 mL, 38 g, 375.53 mmol) in chloroform (100 mL) is added slowly to a stirring solution of cysteamine hydrochloride (21.20 g, 186.6 mmol) in chloroform (200 mL) in a 3 L round-bottom flask with a nitrogen stream passed over the mouth of the vessel…."

    This is the process that produces what a former chemistry professor asserts is a mere “combination” of dietary ingredients?

    — Sullivan    2010-07-07 18:55    #

  2. But of course! The first time I read the recipe, I thought it sounded like something out of The Moosewood Cookbook. ;-)

    — Kathleen Seidel    2010-07-07 19:13    #

  3. Thanks for putting all this chemical information so clearly and in so accessible a location. This is indeed a frightening story.

    — Broken Link    2010-07-08 11:28    #

  4. It is just stunning that this is being fed to children – who have no say in the matter – with essentially no quality control and nothing like the safety studies that ought to be required. I hope this is put to a stop.

    — isles    2010-07-09 13:18    #

  5. Triethylamine (one of the precursor materials) is fairly nasty stuff. It is used to immobilize fruit flies for study and has a significant inhalation toxicity. 1 part per million was considered lethal via inhalation.

    This begs the question of how clean OSR is. How well are the constituents removed from the final product. The paper notes a yield of only 72%.

    — Sullivan    2010-07-09 13:23    #

  6. You write very well, almost like you are an author that is getting paid to produce these articles, Hmmm who might your employers be, which Pharmaceutical company’s payroll are you on?

    — t swherman    2010-07-30 10:21    #

  7. Mwahahahaha — no — but thanks for the compliment.

    — Kathleen Seidel    2010-07-30 12:10    #

Add a comment


Name
E-mail
http://
Message
  Enter links as text in quotes, colon, URL
Example: "Google":http://google.com
Textile Help