PROCESS FOR THE PREPARATION OF LEDIPASVIR AND INTERMEDIATES THEREOF

The present invention relates to process for preparation of ledipasvir of formula 1 and its novel intermediates. The process involves reaction of compound of formula 2 with compound of formula 3 to yield a compound of formula 4, deprotection of compound of formula 4 to yield compound of formula 5 an...

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Main Authors AGRAWAL, Manoj, Kunjabihari, JAIN, Adinath, Murlidhar, DESHMUKH, Swapnil, Sudhakar, SINGH, Girij, Pal, GODBOLE, Himanshu, Madhav
Format Patent
LanguageEnglish
French
Published 10.08.2017
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary:The present invention relates to process for preparation of ledipasvir of formula 1 and its novel intermediates. The process involves reaction of compound of formula 2 with compound of formula 3 to yield a compound of formula 4, deprotection of compound of formula 4 to yield compound of formula 5 and conversion of compound of formula 5 to Ledipasvir wherein PG is an amine protecting group provided that amino protecting group is not carbomethyloxy (-COOCH3) group; X and Y are leaving groups. La présente invention concerne un procédé de préparation de lédipasvir de formule 1 et de ses nouveaux intermédiaires. Le procédé implique la réaction d'un composé de formule 2 avec un composé de formule 3 pour obtenir un composé de formule 4, la déprotection du composé de formule 4 pour donner un composé de formule 5 et la conversion du composé de formule 5 en Lédipasvir où PG désigne un groupe protecteur d'amine, à condition que le groupe protecteur d'amino ne soit pas un carbométhyloxy (-COOCH3) ; X et Y sont des groupes partants.
Bibliography:Application Number: WO2017IB50464