Application of 2-hydroxy-3-trifluoromethylpyridine in insecticides and antagonists and in the preparation of other pharm

2-Hydroxy-3-trifluoromethylpyridine is a widely used organic intermediate, not only for the synthesis of nicotinic insecticides, antagonist TRPV1, anti-androgen A52, but also for the synthesis of various drugs. 2-Hydroxy-3-trifluoromethylpyridine's physical and chemical information is shown as follows:

Physicochemical information of 2-hydroxy-3-trifluoromethylpyridine

Structural formula        

CAS# 22245-83-6

Appearance

White to off-white powder

Melting point

150-153℃

Boiling point

224℃

Flash point

89℃

Molecular formula

C6H4F3NO

Molecular weight

163.10

Solubility

Soluble in water, ethanol, ethyl acetate and other solvents

3-TRIFLUOROMETHYLPYRIDINE

The quality specification of the product is shown as follows:

Quality specification of 2-hydroxy-3-trifluoromethylpyridine

CAS#

2927-71-1

Appearance

Off-white solid

Purity ≥98%

Monohybrid ≤1%

1. Packaging and storage properties

1.1 Package: Fluorinated bottle, aluminum foil bag and cardboard drum

1.2 Storage: Keep the container airtight and store in a dry, ventilated and cool place.

2. Exposure hazard and control

2.1 Causes skin irritation and causes severe eye irritation.

2.2 Handle in a well-ventilated place. Wear suitable protective gear. Prevent dust from spreading. Wash hands thoroughly after handling.

3. Emergency treatment

3.1 First aid measures

Inhalation: Move the victim to fresh air, keep breathing open and rest. If feeling unwell seek medical attention/consultation.   

Skin contact: Immediately remove/remove all contaminated clothing. Wash gently with plenty of soap and water. If skin irritation or rash occurs: Seek medical attention/consultation.

Eye contact: Wash carefully with water for several minutes. If convenient and easy to do, remove contact lenses. Continue washing. If eye irritation: Seek medical attention/consultation.

Ingestion: If discomfort occurs, seek medical attention/consultation. Rinse mouth.   

Emergency responder protection: Rescuers need to wear personal protective equipment, such as rubber gloves and airtight goggles.

3.2 Fire Fighting Measures

Suitable extinguishing agents: dry powder, foam, fog water, carbon dioxide   

Special hazards: Caution, burning or high temperature may decompose to produce toxic smoke.

Specific method: Extinguish the fire from upwind, choose the suitable fire extinguishing method according to the surrounding environment.   

Non-relevant personnel should evacuate to a safe place.

Once the surrounding area is on fire: If safe, remove removable containers.

Special protective gear for firefighters: Always wear personal protective equipment when extinguishing a fire.

4. Application

4.1 For the preparation of nicotine-based insecticide imidacloprid compositions.

4.2 For the preparation of TRPV1 antagonist with significant analgesic effect.

4.3 Novel synthesis of anti-androgen A52 for the treatment of prostate cancer.

4.4 Compositions for the preparation of histoproteinase S inhibitors [7]. These derivatives can be used for the treatment of histone S-related diseases such as atherosclerosis, obesity, inflammatory and immune diseases such as rheumatoid in the use of drugs for arthritis, psoriasis, cancer and chronic pain, such as neuropathic pain.

4.5 Novel compounds for the preparation of inhibitors of transfected (RET) kinase rearrangements for the treatment of gastrointestinal sensitivities, diseases associated with RET dysfunction and abdominal diseases treatment including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea, functional esophageal disease, functional gastroduodenal disease, inflammatory bowel disease such as non-small cell lung cancer, hepatocellular carcinoma, colorectal cancer The following are examples of the IBS categories.