A STABLE POLYMORPH OF THE SALT OF (2R)-4-OXO-4-[3-(TRIFIUOROMETHYL)-5,6- DIHYDRO[L,2,4]TRIAZOLO[4,3-A]PYRAZIN-7(8H)-YL]-L-(2,4,54RIFLUOROPHENYL)BUTAN-2-AMINE WITH L-TARTARIC ACID

A stable polymorph (Form Z1) of the salt of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro [152,4]triazolo[4,3-α]pyrazin-7(8H)-yl]-1-(2s4,5-trifluorophenyl)butan-2-amine (sitagliptin) with L-tartaric acid, of formula 1, which is a very suitable form of the active pharmaceutical ingredient of medicina...

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Main Authors LUKAS KREJCIK, KAMAL JARRAH, PETR LEHNERT, ONDREJ DAMMER, JINDRICH RICHTER
Format Patent
LanguageEnglish
Portuguese
Published 19.11.2018
Subjects
ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:A stable polymorph (Form Z1) of the salt of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro [152,4]triazolo[4,3-α]pyrazin-7(8H)-yl]-1-(2s4,5-trifluorophenyl)butan-2-amine (sitagliptin) with L-tartaric acid, of formula 1, which is a very suitable form of the active pharmaceutical ingredient of medicinal products intended especially for treatment of diabetes type 2. A method of preparation of the stable polymorph (Form Z1) of the salt of sitagliptin with L-tartaric acid, as well as its use for the preparation of a pharmaceutical composition.
Bibliography:Application Number: PT20140815215T