Semisynthesis of RPR 121056A, a major metabolite of irinotecan (CPT-11)

Autor:	Laurent P. Rivory, Jean-Dominique Bourzat, Marc Vuilhorgne, Alain Commercon, Jacques Robert
Rok vydání:	1996
Předmět:	Chemistry Stereochemistry Metabolite Organic Chemistry Cleavage (embryo) Biochemistry Semisynthesis In vitro Irinotecan chemistry.chemical_compound Hydrogenolysis Drug Discovery medicine Cytotoxicity medicine.drug
Zdroj:	Tetrahedron Letters. 37:6327-6330
ISSN:	0040-4039
DOI:	10.1016/0040-4039(96)01387-1
Popis:	The semisynthesis of RPR 121056A ( 4 0, a major metabolite of irinotecan (CPT-11, 2 ), is reported starting from SN-38 ( 3 ) and an appropriate side-chain precusor, and using a 2-step sequence. This semisynthesis is based on the 10-O-acylation of SN-38 with the conveniently protected carbamoylchloride derivative 10 followed by cleavage of the benzylic protecting groups by hydrogenolysis. Preliminary in vitro results show that RPR 121056A displays no cytotoxicity.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::d144c668f765e0b61740b602a6c8d324 https://doi.org/10.1016/0040-4039(96)01387-1 Zobrazit plný text záznamu Full Text from ScienceDirect