Introduce of Leuprolide acetate 74381-53-6

- 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.

Basic Information

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

PSA: 466.34000

LogP: 3.44730

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 [1]

Synthetic resolution

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.


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