A PROCESS FOR THE SYNTHESIS OF 4-((R)-2-{[6-((S)-3-METHOXY-PYRROL IDIN-1-YL)-2-PHENYL- PYRIMIDINE-4-CARBONYL]-AMINO}-3-PHOSPHONO-PR OPIONYL)-PIPERAZINE-1 -CARBOXYLIC ACID BUTYL ESTER

A PROCESS FOR THE SYNTHESIS OF 4-((R)-2-{[6-((S)-3-METHOXY-PYRROL IDIN-1-YL)-2-PHENYL- PYRIMIDINE-4-CARBONYL]-AMINO}-3-PHOSPHONO-PR OPIONYL)-PIPERAZINE-1 -CARBOXYLIC ACID BUTYL ESTER

The present invention relates to a process for the synthesis of 4-((R)-2-{[6-((S)-3-methoxy-pyrrolidin-1-yl)-2-phenyl-pyrimidin e-4-carbonyl]-amino}-3-phosphono-propionyl)-piperazine-1-carboxy lic acid butyl ester, or of a hydrochloride salt thereof; and to a crystalline form of 4-((R)-2-{[6-((S)-3-...

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Bibliographische Detailangaben
Hauptverfasser: CLAVEAU Romain, REBER Stefan, HALL Leanne, FEYEN Fabian, HUGHES Stephen, BLUMER Nicole
Format: Patent
Sprache:eng ; spa
Schlagworte:
ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM
CHEMISTRY
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
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Zusammenfassung:The present invention relates to a process for the synthesis of 4-((R)-2-{[6-((S)-3-methoxy-pyrrolidin-1-yl)-2-phenyl-pyrimidin e-4-carbonyl]-amino}-3-phosphono-propionyl)-piperazine-1-carboxy lic acid butyl ester, or of a hydrochloride salt thereof; and to a crystalline form of 4-((R)-2-{[6-((S)-3-methoxy-pyrrolidin-1-yl)-2-phenyl-pyrimidin e-4-carbonyl]-amino}-3-5 phosphono-propionyl)-piperazine-1-carboxylic acid butyl ester hydrochloride. Formula (I). La presente invención se refiere a un proceso para la síntesis de éster de butilo de ácido 4-((R)-2-{[6-((S)-3-metoxi-pirrolidin-1-i l)-2-fenil-pirimidin-4-carbonil]-amino}-3-fosfono-propionil)-pipe razin-1-carboxílico, o de una sal de clorhidrato del mismo; y a una forma cristalina de clorhidrato de éster de butilo de ácido 4-((R)-2-{[6-((S)-3-metoxi-pirrolidin-1-il)-2-fenil-pirimidin-4-c arbonil]-amino}-3-fosfono-propionil)-piperazin-1-carboxílico. Fórmula (I). (ver Fórmula).