Product information

 

Tegafur Basic information

Antineoplastic Chemical Properties Application Production methods

Product Name:	Tegafur
Synonyms:	TEGAFUR;1-(tetrahydrofuran-2-yl)-5-fluoro-uraci;1-(tetrahydrofuran-2-yl)-5-fluorouracil;3h)-pyrimidinedione,5-fluoro-1-(tetrahydro-2-furanyl)-4(1h;5-fluoro-1-(tetrahydro-2-furanyl)-2,4-pyrimidinedione;5-fluoro-1-(tetrahydro-2-furyl)-uraci;5-fluoro-1-(tetrahydro-3-furyl)uracil;5-fluoro-1-(tetrahydrofuran-2-yl)uracil
CAS:	17902-23-7
MF:	C8H9FN2O3
MW:	200.17
EINECS:	241-846-2
Product Categories:	Active Pharmaceutical Ingredients;Pyridines, Pyrimidines, Purines and Pteredines;Antitumors for Research and Experimental Use;Biochemistry;Chemical Reagents for Pharmacology Research;Nucleosides and their analogs;Nucleosides, Nucleotides & Related Reagents;Intermediates & Fine Chemicals;Pharmaceuticals;API;Inhibitors
Mol File:	17902-23-7.mol

Tegafur Chemical Properties

mp	171-173 °C(lit.)
storage temp.	2-8°C
Merck	9112
CAS DataBase Reference	17902-23-7(CAS DataBase Reference)

Safety Information

Hazard Codes	T
Risk Statements	23/24/25
Safety Statements	22-36/37/39-45
RIDADR	UN 2811 6.1/PG 2
WGK Germany	3
RTECS	YR0450000

MSDS Information

Provider	Language
5-Fluoro-1-(tetrahydro-2-furanyl)-2,4(1H,3H)-pyrimidinedione	English
SigmaAldrich	English

Tegafur Usage And Synthesis

Antineoplastic	Tegafur is a anticancer drug.it is a fluorouracil derivative, in vitro it has no anti-tumor effect, after it goes into the human body ,by the role of the liver drug metabolism enzymes and microsomal enzymes P-450 in the liver, its tetrahydrofuran ring is taken off, fluorouracil (5-FU)is gradually released to produce cytotoxicity. Variety of tumor inhibition is similar to 5-FU, its mechanism of inhibition is inhibiting thymidine synthetase, blocking deoxy thymidylate converting to pyrimidine nucleotide, thereby interfering and blocking the synthesis of DNA, RNA and protein .  Tegafur index of chemotherapy is twice of 5-FU and toxicity is 1/6 ~ 1/5 of 5-FU ,there is cross-resistance between 5-FU and the product,it belongs to cycle-specific drugs, tegafur belongs to the time-dependent cytostatic, preferable absorption after oral , Tmax is 2h, it slowly releases 5-FU in vivo, blood level is not very high, it can maintain a longer time, so it has a low toxicity in vivo.the Intravenous infusion is better than the one-time injection. After the drug going into the body, it is evenly distributed in the liver, small intestine, spleen, lung, kidney and brain, liver and kidney having the highest concentrations. T1 / 2 is 5 ~ 18.6h. Inhibition of DNA, RNA synthesis can maintain 12 ~ 20h. After 24h, the content of each tissue is significantly reduced. It is Mainly excreted in the urine and respiratory tract , within 24h after administration, 23% is by the urine excretion of the prototype , 55% is excreted from the respiratory tract in the form of CO2. This product is highly fat-soluble, widely distributed, easily through the blood-brain barrier, its cerebrospinal fluid concentration is higher than 5-FU.  This product is effective against a variety of solid tumors, it is primarily used for the treatment of digestive system cancers, tegafur has a effective rate of 30% to 33% on gastric cancer ,it has a certain effect on colon cancer, colorectal cancer, lung cancer, primary and metastatic liver cancer, pancreatic cancer , cholangiocarcinoma, gallbladder cancer, prostate cancer, kidney cancer, bladder cancer . It can also be used to treat breast cancer, head and neck squamous cell carcinoma, lung cancer and liver cancer. It is Also used as a radiation sensitizer before and after surgery treatment to prevent cancer recurrence, proliferation and metastasis. Overall, the efficacy of this product is a little better than 5-FU.  The above information is edited by the Chemicalbook of Tian Ye.
Chemical Properties	White crystalline powder. Melting point 164-165 ℃, soluble in water, ethanol, dimethylformamide, insoluble in ether, benzene. Odorless, bitter taste.
Application	this product is a derivative of 5-fluorouracil, the role and application of the product is the same as 5-fluorouracil, but it has less toxicity and its chemotherapy index is high. After the activion by the liver in vivo ,it becomes 5-fluorouracil to play a role in cancer. It is effective on Gastric cancer, colon cancer, colorectal cancer, pancreatic cancer and breast cancer, lung cancer.
Production methods	After condensatio from 5-fluorouracil and 2-acetoxy tetrahydrofurann, the product is obtained. The yield rate of this method is only15%. Another method is using 5-fluorouracil, hexamethyl silazane and trimethylchlorosilane as starting materials to produce tegafur.
Chemical Properties	White Crystalline Powder
Usage	Used as an antineoplastic

 

 

Company information

 Henan sunlake enterprise corporation is located in Henan Province , The central plain of China , Which enjoys favorable geogeaphical position and convenient transportion, The com[any was established in june. 1998 , until now having more than 18 years experience in manufacturing & exporting chemical raw material .

  Sunlake is a professional manufacturer engaged in producing and selling chemicals,including Organic & inorganic chemicals , pigments & Dyestuffs ,  Water treatment chemicals , Food & FEED additives and others . these products have been being well exported to europe , southeast Asia , the Middle East ,  Africa , South America and some other countries and areas.

    We sincerely welcome foreign friends to visit our plant for cooperation. With the idea of "quality first,credit priority, Excellent service", We are highly acknowledged by customers for good quality and competitive price. More importantly , the company has a strong R & D team, who are professional engineers and scholars with Ph. D. .So we are confident to serve you  better with our high - quality products and professional team.

    We are taking great efforts to provide our customers with demanded goods and professional services, and continuously improve our core ability of competition and get the momentum for sustainable development, and finally make us being a reliable and professional wupplier in international market.

    We  welcome any serious inquiries from all customers of the world, and sincerely hope to cooperate.