Application pharmaceuticals
Please find here a few examples of our nitriles mainly used as intermediates for pharmaceuticals for human and veterinary use:
Human medicine application:
| NITRALZ® | CAS No. | application area examples | end product examples |
|---|---|---|---|
4-Aminobenzonitrile | 873-74-5 | anti-migrane anti-atherosclerotic anticoagulant treatment of HIV anti-cancer anti-asthmatic | Dabigatran Frovatriptan Goxalapladib Rilpivirine |
2-Brombenzonitrile | 2042-37-7 | anti-hypertensive anti-epileptic | Irbesartan Perampanel |
4-Brombenzonitrile | 623-00-7 | analgesic ocular anti-inflammatory | Bromfenac |
2-Chlorbenzonitrile | 873-32-5 | anti-hypertensive analgesic hypnotic anesthetic | Sartanes
Ketamine Hydrochloride |
4-Chlorbenzonitrile | 623-03-0 | anti-allergic aromatase inhibitor | Lodoxamide Tromethamine |
2,3-Dichlorbenzonitrile | 6574-97-6 | anti-epileptic | Lamotrigine |
2,4-Dichlorbenzonitrile | 6574-98-7 | treatment of HIV | Dolutegravir |
Pivalonitrile | 630-18-2 | bronchodilator | Pirbuterol |
4-Tolunitrile | 104-85-8 | anti-histaminic hemostatic anti-ulcerative anti-neoplastic | Letrozole |
| 3-Acetylpyridine | 350-03-8 | anti-leukemia drug | Imatinib |
Veterinary medicine application:
| NITRALZ® | CAS No. | application area examples | end product examples |
|---|---|---|---|
Benzonitrile | 100-47-0 | antibacterial | Florfenicol, Robenacoxib |
n-Butyronitrile | 109-74-0 | anticoccidial | Amprolium |
4-Chlorbenzonitrile | 623-03-0 | contraceptive | Lotrifen |
3-Acetylpyridine | 350-03-8 | tyrosine-kinase inhibitor treatment of mast cell tumors | Masitinib |
Special solvents:
| NITRALZ® | CAS No. |
|---|---|
n-Butyronitrile | 109-74-0 |
Pivalonitrile | 630-18-2 |
4-Heptanone | 123-19-3 |
Did you know that …
Over 30 nitrile-containing pharmaceuticals are prescribed for a diverse variety of medicinal indications with more than 20 additional nitrile-containing leads in clinical development.
The nitrile group is quite robust and, in most cases, is not readily metabolized but passes through the body unchanged. The types of pharmaceuticals containing nitriles are diverse, from vildagliptin, an antidiabetic drug, to anastrozole, which is the gold standard in treating breast cancer. In many instances the nitrile mimics functionality present in substrates for enzymes, whereas in other cases the nitrile increases water solubility or decreases susceptibility to oxidative metabolism in the liver. The nitrile functional group is found in several drugs. (Fleming et al. 2010: 7902)
Fleming, Fraser F.; Lao, Lihua; Ravikumar, P.C; Funk, Lee and Shook, Brian C. (2010): Nitrile-Containing Pharmaceuticals. Efficacious Roles of the Nitrile Pharmacophor, in: Journal of Medicinal Chemistry. 53 (22), pp 7902-7917.
