Tiopronin Powder CAS 1953-02-2

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Tiopronin powder, the chemical name of the core component (tiopronin) is n - (2-mercaptopropionyl) glycine, and the other name is viola. It is a white crystalline powder with a sulphur odour. Soluble in water or ethanol, very slightly soluble in chloroform or ether; Soluble in dilute alkali solution. Tiopronin is a sulfhydryl-containing drug with similar properties to penicillamine, which can protect liver tissues and cells. Animal experiments show that tiopronin can prevent liver damage caused by carbon tetrachloride, methionine, and acetaminophen by providing sulfhydryl groups, and inhibiting the accumulation of triglycerides in chronic liver injury. Tiopronin can reduce the activity of apps in hepatocyte mitochondria, so as to protect the structure of liver mitochondria and improve liver function. In addition, tiopronin can also scavenge free radicals through the reversible combination of sulfhydryl and free radicals.

Tiopronin powder is a novel glycine derivative containing free thiol groups, widely used as a hepatoprotective drug in clinical practice. Its applications include liver diseases, adjuvant therapy of radiotherapy and chemotherapy, ophthalmic diseases, skin diseases, and prevention of urinary system stones.

Liver Disease Treatment: Core Indications and Mechanisms of Action

 

1. Viral hepatitis and drug-induced liver injury
By providing free thiol groups, stable compounds are formed by binding with free radicals, thereby clearing oxygen free radicals and protecting the structure of liver cell membranes and mitochondria. It can reduce the activity of mitochondrial ATPase in liver cells, decrease energy consumption, and promote liver cell repair. Clinical studies have shown that for patients with acute viral hepatitis, sulpiride significantly reduces serum transaminase levels and improves symptoms such as fatigue and decreased appetite; The effective rate of drug-induced liver injury (such as liver damage caused by anti tuberculosis drugs and anti epileptic drugs) is over 85%, which can shorten the course of the disease and reduce the risk of liver fibrosis.

2. Alcoholic fatty liver and non-alcoholic fatty liver disease (NAFLD)
By inhibiting the accumulation of triglycerides in liver cells, lipid metabolism disorders can be improved.

 

Animal experiments have shown that it can reduce the degree of hepatic steatosis induced by high-fat diet in rats, decrease hepatocyte ballooning and inflammatory cell infiltration. In clinical applications, for patients with alcoholic fatty liver, the combination of sulpiride and abstinence therapy can significantly reduce serum gamma glutamyltransferase (GGT) levels and improve liver ultrasound imaging; For NAFLD patients, it can assist in weight loss and improve insulin resistance.
3. Early intervention for liver cirrhosis
By inhibiting the activation of hepatic stellate cells and reducing collagen synthesis, the progression of liver cirrhosis can be delayed. For patients with compensatory cirrhosis, long-term use of sulpiride can reduce portal vein pressure and lower the risk of esophageal and gastric variceal bleeding. In addition, it can also improve the nutritional status of patients with cirrhosis and increase serum albumin levels.

Chemotherapy adjuvant therapy: multi-target protective effect

 

1. Reduce bone marrow suppression
By stabilizing the bone marrow cell membrane, the rate of bone marrow chromosomal aberrations caused by radiotherapy and chemotherapy can be reduced. Clinical data shows that for cancer patients receiving cisplatin chemotherapy, the combined use of sulpiride can reduce the incidence of leukopenia from 62% to 35%, and the incidence of thrombocytopenia from 48% to 22%. The mechanism may be related to the repairing effect of thiol groups on DNA damage.
2. Accelerate liver cell recovery
Chemotherapy and radiotherapy often lead to elevated liver transaminase levels, which promote liver cell regeneration and shorten the time for liver function recovery.

 

For liver cancer patients receiving hepatic artery embolization chemotherapy, postoperative use of sulpiride can restore normal serum ALT levels within 7 days, while the control group requires more than 14 days.

3. Preventing secondary tumors
Reducing the risk of DNA mutations by eliminating free radicals generated by radiotherapy and chemotherapy. Animal experiments have shown that it can reduce the incidence of lung cancer in mice after radiotherapy, and its mechanism may be related to the inhibition of the release of inflammatory factors such as IL-6 and TNF - α.

Ophthalmic disease treatment: breakthrough application of senile cataract

 

1. Inhibit lens protein degeneration
By binding to the disulfide bond between thiol groups and lens proteins, protein cross-linking polymerization is prevented, thereby delaying the progression of cataracts. Clinical studies have shown that for early-stage elderly cataract patients, the combination of local use of sulpiride eye drops (0.1%) and oral preparations (0.2g/day) resulted in a 68% improvement in visual acuity after 6 months, compared to only 32% in the control group.
2. Improve vitreous opacity
It can reduce abnormal cross-linking of vitreous collagen fibers and promote the absorption of turbid substances. For patients with diabetes vitreous hemorrhage, the combination of tiopronin and vitrectomy can reduce the incidence of postoperative retinal detachment and improve the success rate of surgery.

Prevention of urinary system stones: specific treatment for cystine stones

 

1. Dissolve cystine stones
By forming soluble complexes with cysteine, its solubility in urine is increased. For patients with recurrent cysteine stones, long-term use of sulpiride (0.5g/day) can reduce the recurrence rate of stones from 80% to 25% without affecting renal function.
2. Adjust the pH value of urine
Can alkalize urine and inhibit the formation of uric acid stones. For patients with hyperuricemia, the combined use of sulpiride and potassium citrate can maintain urine pH between 6.2-6.8 and reduce the risk of uric acid stone formation by 60%.

Skin disease treatment: unique advantages of anti-inflammatory and anti allergic effects

 

1. Chronic eczema and neurodermatitis
Relieve skin itching and inflammation by inhibiting histamine release and 5-hydroxytryptamine (5-HT) receptor activity. For patients with chronic eczema, the combination of local use of Thioprine cream (2%) and oral preparation (0.1g/day) resulted in a 58% reduction in itching score and a 42% reduction in skin lesion area after 4 weeks, with better efficacy than topical corticosteroids alone.
2. Acne and rosacea
Can regulate sebaceous gland secretion and inhibit the growth of Propionibacterium acnes. For patients with moderate acne, oral administration of thioprine (0.2g/day) combined with topical application of tiopronin powder resulted in a 73% reduction in inflammatory lesions and a 61% reduction in non inflammatory lesions after 8 weeks, with a lower incidence of adverse reactions compared to treatment with antibiotics alone.

Melting point 93-98 ° C, Boiling point 418.3 ± 30.0 ° C (predicted), Density 1.249 (estimate), Refractive index 1.5216 (estimated), Storage condition: insert atmosphere, 2-8 ° C, Form solid, Acidity coefficient (PKA) 3.36 ± 0.10 (predicted).

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Synthetic method of the powder of tiopronin:

1. Propionic acid is first chlorinated with thionyl chloride and then brominated to obtain α- Bromopropionyl chloride. Glycine is dissolved in 2mol / L sodium hydroxide and added dropwise at the same time α- Bromopropionyl chloride and sodium hydroxide solution to obtain n-( α- Bromopropionyl) glycine. After reacting with sodium disulphide, it is reduced with zinc powder to obtain tiopronin.

2. Or mix glycine with water, add 2 - bromopropionyl chloride and sodium carbonate solution dropwise under certain conditions, and add and stir. Thiobenzoic acid is added, and sodium hydroxide solution is added dropwise. After the reaction, it is filtered to remove a small amount of insoluble matter, and the filtrate is acidified. The obtained solid is washed and dried, then concentrated ammonia is added to the aqueous sodium carbonate solution, stirred, washed, filtered, acidified with hydrochloric acid, concentrated under reduced pressure, and dissolved by adding a hot mixture of ethyl acetate and ethanol (1:1). After treatment, tiopronin was obtained

3. 2-chloropropionic acid and sulfoxide chloride can also be refluxed together to obtain 2-chloropropionyl chloride. Mix glycine, sodium carbonate, and an appropriate amount of water. Under the cooling of the ice salt bath and vigorous stirring, drop the aqueous solution of 2 - Chloropropionyl chloride and sodium carbonate and stir. It is acidified with hydrochloric acid and extracted with ethyl acetate. The treated material is dissolved in sodium carbonate aqueous solution and dropped into sodium disulphide solution for reaction. Tiopronin is also obtained after sulfuric acid acidification, filtration, and zinc powder treatment in the filtrate.

Using inexpensive and readily available 2-bromopropionic acid as the starting material, tiopronin can be prepared through steps such as chlorination, condensation, nucleophilic substitution, and deprotection.

1. Chlorination:

React 2-bromopropionic acid with anhydrous ferrous chloride (FeCl₂) or carbon tetrachloride (CCl4) to undergo a chlorination reaction to produce 2-chloropropionic acid.

BrCH₂CH₂COOH+Cl₂ → ClCH₂CH₂COOH+HBr

2. Condensation:

Treat 2-chloropropionic acid with an alkali (such as sodium hydroxide) to undergo a dehydration reaction, producing acrylic acid.

ClCH₂CH₂COOH+NaOH → CH₂=CHCOOH+NaCl+H₂O

3. Nucleophilic Substitution:

Acrylic acid reacts with 2-thioethylamine (or 2-thiopropylamine) under alkaline conditions to undergo a nucleophilic substitution reaction, resulting in the formation of thiopronin.

CH₂=CHCOOH+HSCH₂CH₂NH₂ → CH₂=CHCOOCH₂CH₂CH₂SCH₂CH₂NH₂

4. Deprotection:

React the synthesized tiopronin powder with sodium hydroxide or other suitable deprotection reagents to remove the protective group and obtain the final product of tiopronin.

CH₂=CHCOOCH₂CH₂SCH₂CH₂NH₂+NaOH → CH₂=CHCOOH+H₂S+NaOCH₂CH₂NH₂

The total yield is 35.7%. The substitution reaction and deprotection reaction are completed using the "one pot method", which shortens the production cycle and improves the reaction yield compared to the original process. At the same time, it reduces the discharge of "three wastes" and reduces production costs. Through the above steps, 2-bromopropionic acid can be used as the starting material to successfully synthesize tiopronin through reactions such as chlorination, condensation, nucleophilic substitution, and deprotection. Please note that in practical operations, factors such as reaction conditions, solvent selection, and purification and separation steps may need to be considered.

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