- Sep 30, 2017 -
Leuprolide (chemical formula: C61H88N16O14), for gonadotropin drugs, fluffy solid, clinically used in endometriosis; accompanied by menorrhagia, lower abdominal pain, low back pain and anemia and other uterine fibroids; Premenopausal breast cancer, and estrogen receptor-positive patients; prostate cancer; central precocious puberty.
Chinese name: leuprolide
Alias: leuprolide, Na Na Tong, leuprolide acetate
English name: Leuprorelin, Enanton
CAS Number: 53714-56-0
Molecular formula: C61H88N16O14
Molecular weight: 1269.45000
Accurate quality: 1268.67000
Physical and chemical properties
Appearance and properties: fluffy solid
Optical rotation: -31.7 °
Density: 1.44 g / cm3
Melting point: 131ºC
Boiling point: 473.6ºC at 760 mmHg
Flash point: 255.2ºC 
Phenol and phosgene reaction to produce phenyl chloroformate, and then tert-butanol reaction, the formation of tert-butoxyphenyl phenyl ester, followed by hydrazine reaction, and then nitrosation to produce tert-butyl azide, and then react with leucine , The leucine side chain was obtained.
The proline side chain can also be obtained.
The serine is reacted with benzyl chloride to protect the hydroxyl group and react with t-butyl azide to give the serine side chain. Similar to serine, side chains of tyrosine and histidine can be obtained. Tert-butyl azide and tryptophan, and then reacted with 2,4,6-trimethoxybenzenesulfonyl chloride to give the tryptophan side chain. Tert-butyl azanoate and arginine, and then p-toluenesulfonyl chloride reaction, to obtain arginine side chain. After the above-mentioned side chain is obtained, the peptide is further reacted with ethylamine, followed by reaction with ethylamine, and then deprotecting or hydrogenolysis to remove the support base.