Buserelin CAS 57982-77-1

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Buserelin, GnRH analogue. Usually presented as a white or off white solid powder, the molecular formula of Busherelin is C60H86N16O13, with a molecular weight of 1239.424, CAS 57982-77-1, and an accurate mass of 1238.656006. Low solubility in water, manifested as slightly soluble in water. This means that when conducting chemical reactions, it is necessary to consider the selection of solvents and reaction conditions to ensure that Buscherelin can effectively participate in the reaction. In addition, the solubility of Buscherelin in dilute acids is also low, which further limits its application in certain chemical reactions. The predicted acidity coefficient (pKa) is 9.82 ± 0.15. The acidity coefficient is an important parameter that describes the acidity and alkalinity of a substance, reflecting its ability to dissociate hydrogen ions in solution. Buscherelin has a high pKa value, indicating its stability under neutral or alkaline conditions, while it may be prone to dissociation or degradation under acidic conditions. It has multiple functions and application values and plays an important role in the medical field. Its mechanism of action in treating osteoporosis, male breast development, prostate cancer, breast cancer and regulating endocrine function has made it a drug of great concern. It also needs to further study and explore the application value of Busherelin in other fields to make greater contributions to the development of medicine.

Buserelin is a drug with multiple medical applications, and its functions are extensive and important.

Treating osteoporosis

 

As an important drug, it has significant therapeutic effects on osteoporosis. Osteoporosis is a common bone disease characterized by thinning and weakening of bones, making it prone to fractures. Busherelin effectively improves symptoms in patients with osteoporosis by promoting bone growth and increasing bone density. Its main component, estradiol, is an important hormone in the human body that plays a crucial role in female puberty and fertility. Estradiol can stimulate endometrial hyperplasia, maintain a normal menstrual cycle, and also promote bone growth and increase bone density. For people with osteoporosis, Buscherelin can effectively promote bone growth, increase bone density, and thus improve bone health.

Treatment of male breast development disorders&Treat prostate and breast cancer cancer

 

In addition to treating osteoporosis, it can also be used to treat male breast development. Male breast development syndrome is a common male breast disease characterized by symptoms such as breast enlargement and pain. Busherelin effectively improves the symptoms of male breast development by regulating hormone levels, inhibiting the growth of breast ducts and milk secretion. Estradiol, as the main component of Busherelin, has an inhibitory effect on the growth and secretion of breast ducts and can help restore normal breast tissue structure.

It also has certain application value in the treatment of prostate cancer and breast cancer. As a gonadotropin-releasing hormone analogue, it produces an anti estrogenic effect by inhibiting the secretion of luteinizing hormone and follicle stimulating hormone in the anterior pituitary gland, reducing serum testosterone levels. This mechanism makes it an effective drug for the treatment of prostate cancer and breast cancer. In the treatment of prostate cancer, Busherelincan reduce testosterone levels, thereby inhibiting tumor growth and spread. In the treatment of breast cancer, it can prevent the recurrence of breast cancer in postmenopausal women and improve the treatment effect.

Treatment of endometriosis& Regulating endocrine function

 

 

In addition, it can also be used to treat endometriosis. Endometriosis is a common gynecological disease characterized by the growth of endometrial tissue outside the uterine cavity. Busherelin inhibits the secretion of luteinizing hormone and follicle stimulating hormone in the anterior pituitary gland, lowers serum hormone levels, and thus inhibits the growth and development of ectopic endometrium. This mechanism of action makes Busherelin an effective drug for treating endometriosis, which can alleviate symptoms such as dysmenorrhea and infertility in patients, and improve their quality of life.

In addition to the specific applications mentioned above, it also has the function of regulating endocrine function. As a hormonal drug, Buserellin can affect the secretion and metabolism of various hormones in the human body, thereby regulating the balance of the endocrine system. For example, Busherelin can affect the function of endocrine glands such as the adrenal gland and thyroid gland, and regulate the secretion levels of related hormones. This regulatory effect is of great significance for maintaining the balance and stability of the human endocrine system.

Buserelin is an important pharmaceutical intermediate mainly used in the manufacture of certain antibacterial drugs. It belongs to peptide hormones and has characteristics such as strong biological activity and long-lasting efficacy. The synthesis of Buscherelin involves multiple steps, including condensation, hydroxylation, methylation, diazotization, and other reactions.

Synthesis steps

1. Synthesis of Aminophenol

Firstly, the condensation reaction between aniline and acetaldehyde is carried out under acidic conditions to produce aminophenol. The chemical equation for this step is as follows:

C₆H₅NH₂+CH₃CHO → C₆H₅NHCH₂OH (under acidic conditions)

This reaction is usually carried out under the catalysis of hydrochloric acid or sulfuric acid, and the reaction temperature is controlled between room temperature and boiling. After the reaction is completed, aminophenol is separated by distillation or extraction methods.

2. Synthesis of 2-hydroxyaniline

Next, the hydroxylation reaction between aminophenol and formaldehyde is carried out under alkaline conditions to generate 2-hydroxyaniline. The chemical equation for this step is as follows:

C₆H₅NHCH₂OH+HCHO → C₆H₆(OH)NHCH₂OH (under alkaline conditions)

This reaction is usually carried out in an alkaline solution of sodium hydroxide or potassium hydroxide, and the reaction temperature is controlled between room temperature and 60 ℃. After the reaction is completed, 2-hydroxyaniline is separated by acidification, extraction and other methods.

3. Synthesis of 2-methyl-4-nitroaniline

Then, 2-hydroxyaniline is methylated with dimethyl sulfate under alkaline conditions to produce 2-methyl-4-nitroaniline. The chemical equation for this step is as follows:

C₆H₆(OH)NHCH₂OH+(CH₃)₂SO₄ → C₆H₇N(CH₃)+H₂O+SO₂ (under alkaline conditions)

This reaction is usually carried out in an alkaline solution of sodium hydroxide or potassium hydroxide, and the reaction temperature is controlled between room temperature and 80 ℃. After the reaction is completed, 2-methyl-4-nitroaniline is separated by extraction, crystallization and other methods.

4. Synthesis of Buscherelin

Finally, 2-methyl-4-nitroaniline was subjected to diazotization reaction with sodium nitrite under acidic conditions to generate Buscherelin. The chemical equation for this step is as follows:

C₆H₇N(CH₃)+NaNO₂+HCl → C₆H₇N(CH₃)NO+NaCl+H₂O (under acidic conditions)

This reaction is usually carried out in acidic solutions of hydrochloric acid or sulfuric acid, and the reaction temperature is controlled between 0-5 ℃. After the reaction is completed, Busnerelin is separated by extraction, crystallization, and other methods.

Through the above four steps, we can synthesize the important drug intermediate of Busnerelin. Each step involves specific chemical reactions and conditions, which require strict control to ensure the quality and purity of the Buserelin . Meanwhile, due to the involvement of some toxic and harmful chemicals in these reactions, necessary safety and environmental protection measures need to be taken during the experimental process to ensure the safety of experimental personnel and the sustainability of the environment.

Buserelin is an artificially synthesized gonadotropin-releasing hormone (GnRH, also known as LHRH) analogue, belonging to the first generation of GnRH agonists. Since its inception in the 1970s, it has become an important drug for the treatment of hormone dependent cancers (such as prostate cancer, breast cancer), endometriosis, hysteromyoma, and controlled ovarian hyperstimulation in assisted reproductive technology (ART). In the 1960s, scientists gradually revealed the mechanism by which the hypothalamus regulates the release of luteinizing hormone (LH) and follicle stimulating hormone (FSH) from the anterior pituitary gland by secreting gonadotropin-releasing hormone (GnRH). GnRH is a peptide hormone whose structure was independently identified by the team of Andrew Schally and Roger Guillemin in 1971, and for this, it was awarded the 1977 Nobel Prize in Physiology or Medicine. The half-life of natural GnRH (pGlu His Trp Ser Tyr Gly Leu Arg Pro Gly NH ₂) is extremely short (only 2-4 minutes), and it is easily degraded by enzymes, which limits its therapeutic application. Therefore, scientists began to search for more stable GnRH analogs to enhance their efficacy and prolong their duration of action. In the early 1970s, a team of scientists from Hoechst AG (now part of Sanofi) in Germany began systematic research on GnRH analogs. They found that the 6th glycine (Gly ⁶) and 10th glycinamide (Gly-NH ₂) of GnRH are key sites for enzyme degradation. Through amino acid substitution and modification, the research team found that:

• The 6th Gly → D-amino acid (such as D-Ser, D-Leu, D-Trp) can enhance enzyme stability.
• Gly-NH ₂ → ethylamide (- NH Et) at position 10 can enhance receptor affinity.

After multiple rounds of optimization, the Hoechst team synthesized Buserelin (originally codenamed HOE-766) in 1975, with the following structure:
[pGlu-His-Trp-Ser-Tyr-D-Ser(tBu)-Leu-Arg-Pro-NHEt]
Key embellishments:

• The 6th D-serine (D-Ser ⁶): resists enzymatic degradation and prolongs half-life.
• Tert butyl modification (tBu): enhances hydrophobicity and improves membrane penetration.
• C-terminal ethylamide (Pro NHEt): enhances GnRH receptor binding.

These changes increase the biological activity of Buserelin by 50-100 times compared to natural GnRH, and extend its half-life to about 1 hour (subcutaneous injection).

Buserelin is a synthetic GnRH analog with significant therapeutic applications in the management of various reproductive and non - reproductive disorders. Its unique mechanism of action, which involves initial stimulation followed by desensitization of the pituitary gland, allows for the suppression of the HPG axis and the regulation of sex hormone production. Buserelin has proven to be effective in the treatment of endometriosis, prostate cancer, and in assisted reproductive technologies. However, like all drugs, it has a safety profile with potential side effects and drug interactions. Healthcare providers should carefully consider the benefits and risks of buserelin therapy and monitor patients closely during treatment to ensure optimal outcomes. Further research is ongoing to explore new applications of buserelin and to improve its safety and efficacy in clinical practice.

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