Molecular Formula | C66H83N17O13 |
Molar Mass | 1322.47 |
Density | 1.49±0.1 g/cm3(Predicted) |
pKa | 9.82±0.15(Predicted) |
Physical and Chemical Properties | Nafarelin Monoacetate: C66883N17O13? C2H4O2. Crystallization, melting point 188~190 deg C. [Α] D25-27.4 °(C = 0.9, acetic acid). |
Use | Nafarelin is used to treat endometriosis, inflammation, and cysts. Its effect is mainly through inhibiting the hypothalamus-pituitary-ovarian axis, causing The low estrogen state in the body causes ectopic endometrial atrophy. In addition, nafarelin can also be used to treat central precocious puberty. Endometriosis is an estrogen-dependent disease in which ovarian hormones are necessary for ectopic endometrial growth. It is an analog of gonadotropin-releasing hormone (GnRH). It is used to treat endometriosis, which can eliminate pain and reduce endometrial damage. |
Production method | N-acetyl -2-cyanoglycine ethyl ester is reacted with 2-bromomethylnaphthalene in ethanol, and then acidic hydrolysis to obtain compound (I). (I) Acetylation first, then methanol to form an ester to form a compound (II). (II) D-configuration (III) was obtained by separation, and then hydrolyzed with 6mol/L hydrochloric acid to obtain compound (IV). (Ⅳ) Transformed into N-tert-butoxycarbonyl derivative (V), nafarelin was synthesized on diphenylmethylamine resin by solid phase method. |