Phosphorus trichloride and phosphorus oxychloride as reagents in the pharmaceutical industry
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Phosphorus trichloride (PCl3) and phosphorus oxychloride (POCl3) are raw materials used on a large scale during the synthesis of pharmaceuticals. They are used for both the production of Active Pharmaceutical Ingredients (API) and intermediates of those substances.
The active ingredients are substances that act on the human body, causing a certain therapeutic effect. Their small amounts are contained in tablets, capsules, gels and powders or they are suspended in other materials, pharmaceutically inert to the human organism. High reactivity of phosphorus trichloride and phosphorus oxychloride translates into great opportunities to use these chemical compounds in the pharmaceutical industry, making them popular as raw materials in the manufacture of medicines. Below we present examples of using PCl3 and POCl3 in the pharmaceutical industry.
PCl3 and POCl3 as substrate materials in the synthesis of
drugs.
The first example of PCl3 application is to use it as a
reagent - a substance used for the synthesis of drugs based on derivatives of
sulphonamides. The distinguished representatives among this group of medicines
are:
·
chlorthalidone - a diuretic
medicine used in diseases such as hypertension, diabetes insipidus, or liver
and kidney failure,
·
sulfadiazine - used in the burn
treatment . The substance is also used for anti-microbial prevention of entire
body, using the process that stops the production of folic acid in bacterial
cells. Moreover, the combination of pyrimethamine and sulfadiazine is used to
counteract toxoplasmosis, which is a human and animal parasitic disease caused
by protozoa infestation.
Both PCl3 and POCl3 are used as substrates in
the synthesis of derivatives of amino methylene-bis-phosphoric acids They are
modern medicines inhibiting bone resorption. For this reason, these
pharmaceuticals are used in the treatment of osteoporosis and neoplastic
diseases of bones. One of the active substances obtained in such reactions is
1-Hydroxy-2-(1H-imidazole-1-yl)ethylidene]-bisphosphonic acid, known as
zoledronic acid, which is capable of deposition in bones. It stimulates the
osteoblasts to form the bone tissue and inhibits bone calcification. It is
mainly used to treat fractures and during bone surgery to prevent bone
complications.
Potential applications of trichloride and phosphorus
oxychloride in the synthesis of pharmaceuticals
There are many scientific publications and patents, indicating the
possible use of PCl3 and POCl3 in pharmacology. These
publications indicate the high potential of the substances, and their
constantly increasing presence in the sector of pharmaceutical research may
indicate the widening area of their potential usage in the pharmacy.
According to the mentioned scientific studies, PCl3 may
be used as a starting material in the complex process of synthesis of a drug
called Tenofovir. It is an organic compound from the group of phosphonates,
used in the treatment of hepatitis B and to prevent the symptoms of
immunodeficiency caused by virus type 1 (HIV 1), being the virus causing
acquired immune deficiency syndrome (AIDS). On the other hand POCl3
may have a potential use in the synthesis of vitamins, as it is used in one of
the methods for the synthesis of vitamin B6 derivatives.
In addition, phosphorus oxychloride may be used as a reagent in the
phosphorylation reaction, which attaches phosphate residue to a nucleophilic
atom of any chemical compound. In the reaction with nucleosides, nucleotides
may be formed, e.g. guanosine derivatives, such as GMP (guanosine-5’-
monophosphate), which is one of RNA monomers and its salts: disodium (E627),
dipotassium (E628), calcium (E629) used as flavour enhancers in the food
industry.
Another use of POCl3 is its optional application in the
reaction with N-Phenylanthranilic acid in order to obtain 9-chloro-acridine. In
further reactions it forms derivatives, which are considered as potential drugs
with properties of stopping the formation of tumours in the human body.
Phosphorus oxychloride may be also used for the production of Abiraterone,
which is the active substance used in the treatment of prostate cancer.
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