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ChemicalBook CAS DataBase List Leuprorelin acetate

Leuprorelin acetate synthesis

1synthesis methods

Leuprolide acetate is a commonly used hormone anticancer drug. It is the acetate salt of leuprolide, a synthetic nonapeptide analog of gonadotropin-releasing hormone (LHRH, a decapeptide). It belongs to LH-RH. Antagonist, LHRH is produced by the hypothalamus, which can induce the anterior pituitary to release gonadotropins and follicle-stimulating hormone (FSH) and luteinizing hormone (LH). A method for preparing leuprorelin acetate - pGlu-His(Trt)-Trp-Ser(tBu)-Tyr(tBu)-D-Leu-Leu-Arg(Pbf)-Pro-OH and Ethylamine synthesis reaction.

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Yield: 38.6%

Reaction Conditions:

with methanesulfonic acid;methyl-phenyl-thioether;ethane-1,2-dithiol for 1 h;Ambient temperature;

References:

Fukuda, Tsunehiko;Wakimasu, Mitsuhiro;Kobayashi, Shigeru;Fujino, Masahiko [Chemical and pharmaceutical bulletin,1982,vol. 30,# 8,p. 2825 - 2835]

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