PROCESS FOR PREPARING HIGH PURITY DEGREE LAROTRECTINIB

The present invention relates to a Larotrectinib synthesis process with a 3-O- sulfonylated impurity content lower than 0.10% by weight. A further object of the invention is the compound 3-O-sulfo-Larotrectinib ((3S)-N-[5-[(2R)-2- (2, 5 -Difluorophenyl)- 1- pyrrolidinyl] pyrazole [1,5- a] pyrimidine...

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Bibliographic Details
Main Authors NOVO, Barbara, FUSARI, Matteo, BONANOMI, Jacopo, TRABACE, Simona, BERTOLINI, Giorgio, SADA, Mara, DE FIORE, Stella
Format Patent
LanguageEnglish
French
Published 25.08.2022
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
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Summary:The present invention relates to a Larotrectinib synthesis process with a 3-O- sulfonylated impurity content lower than 0.10% by weight. A further object of the invention is the compound 3-O-sulfo-Larotrectinib ((3S)-N-[5-[(2R)-2- (2, 5 -Difluorophenyl)- 1- pyrrolidinyl] pyrazole [1,5- a] pyrimidine-3-yl]-3 -hydroxy sulphonyloxy-1- pyrrolidinecarboxamide), hereinafter referred to as S-Larotrectinib, useful as an analytical standard to evaluate the purity of Larotrectinib. La présente invention concerne un procédé de synthèse de Larotrectinib ayant une teneur en impuretés 3-O-sulfonylées inférieure à 0,10 % en poids. Un autre objet de l'invention est le composé 3-O-sulfo-Larotrectinib ((3S)-N-[5-[(2R)-2-(2, 5-difluorophényl)-1-pyrrolidinyl]pyrazole [1,5- a]pyrimidine-3-yl]-3-hydroxy sulphonyloxy-1-pyrrolidinecarboxamide), ci-après désigné S-Larotrectinib, utile en tant que base analytique pour évaluer la pureté du Larotrectinib.
Bibliography:Application Number: WO2022IB51461