Fursultiamine hydrochloride
[CAS# 2105-43-3]

Identification

• Classification: Pharmaceutical intermediate >> API intermediate
• Name: Fursultiamine hydrochloride
• Synonyms: N-[(4-amino-2-methylpyrimidin-5-yl)methyl]-N-[(E)-5-hydroxy-3-(oxolan-2-ylmethyldisulfanyl)pent-2-en-2-yl]formamide hydrochloride
• Molecular Formula: C₁₇H₂₇ClN₄O₃S₂
• Molecular Weight: 435.00
• CAS Registry Number: 2105-43-3
• EC Number: 218-278-9
• SMILES: CC1=NC=C(C(=N1)N)CN(C=O)/C(=C(\CCO)/SSCC2CCCO2)/C.Cl

Properties

• Boiling point: 645.1 ºC (760 mmHg), Calc.
• Flash point: 343.9 ºC, Calc.

Safety Data

• Hazard Symbols: GHS07 Warning
• Hazard Statements: H302-H315-H319-H335
• Precautionary Statements: P280-P305+P351+P338

Discovory and Applicatios

Fursultiamine hydrochloride is a synthetic compound that belongs to the class of thiamine derivatives. It is a prodrug of thiamine, commonly known as vitamin B1, and is used in the treatment of thiamine deficiency. The substance is an ester of thiamine and is converted into active thiamine in the body after administration. Fursultiamine hydrochloride is primarily used in the medical field, especially in areas where thiamine deficiency is prevalent, such as in certain neurological disorders and conditions related to malnutrition.

The discovery of fursultiamine hydrochloride is part of the ongoing effort to improve the bioavailability and therapeutic efficacy of essential vitamins and their derivatives. The development of prodrugs like fursultiamine hydrochloride helps overcome the limitations of the parent compound, in this case, thiamine, which can have poor absorption when taken orally. By modifying the structure of thiamine, fursultiamine hydrochloride allows for better absorption in the gastrointestinal tract and more efficient conversion to the active form of thiamine within the body.

In terms of its applications, fursultiamine hydrochloride is primarily used to address and treat thiamine deficiency, which can lead to a variety of health issues. Thiamine deficiency is often associated with conditions such as beriberi, Wernicke-Korsakoff syndrome, and other neurological disorders. These conditions are particularly common in regions where diets are deficient in thiamine, or in individuals who have poor nutritional intake or suffer from alcoholism, which impairs thiamine absorption and metabolism.

Fursultiamine hydrochloride is commonly administered orally in the form of tablets or capsules, but it can also be used intravenously or intramuscularly in clinical settings, depending on the severity of thiamine deficiency and the patient's medical needs. Once ingested or administered, fursultiamine is hydrolyzed in the body to release thiamine, which is then utilized in various metabolic processes, including the conversion of carbohydrates into energy, and the maintenance of proper nerve function.

In addition to its use in treating thiamine deficiency, fursultiamine hydrochloride has also been explored in the context of other health conditions where thiamine plays a role. This includes research into its potential effects in conditions like diabetes, heart disease, and certain types of neuropathy, where thiamine supplementation may offer therapeutic benefits. However, the primary use of fursultiamine hydrochloride remains in the treatment of thiamine deficiency-related diseases.

Fursultiamine hydrochloride is generally considered safe for use when administered according to medical guidelines, with minimal side effects. However, like any drug, it should be used under medical supervision, especially in individuals with allergies or sensitivities to thiamine or related compounds. Overdosage is rare but can lead to symptoms associated with thiamine toxicity, such as headaches, irritability, or more severe reactions in extreme cases.

The compound has been studied in various clinical settings, particularly in regions where thiamine deficiency is a known public health issue. Its use in treating neurological and cardiovascular conditions related to thiamine deficiency has been well documented, and it remains a valuable tool in the medical management of these disorders.