PROCESS FOR THE PREPARATION OF BENZOIMIDAZOL-2-YL PYRIMIDINE DERIVATIVES

Disclosed herein is a crystalline hemi-tartrate salt of the compound of formula (I-A), namely [5-(4,6-dimethyl-1H-benzoimidazol-2-yl)-4-methyl-pyrimidin-2-yl]-[3-(1-methyl-piperidin-4-yl)-propyl]-amine. Also disclosed is a process of preparing the hemi-tartrate of compound of formula (I-A) comprisin...

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Bibliographic Details
Main Authors CESCO-CANCIAN, SERGIO, GRIMM, JEFFREY, S
Format Patent
LanguageEnglish
Published 28.03.2013
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:Disclosed herein is a crystalline hemi-tartrate salt of the compound of formula (I-A), namely [5-(4,6-dimethyl-1H-benzoimidazol-2-yl)-4-methyl-pyrimidin-2-yl]-[3-(1-methyl-piperidin-4-yl)-propyl]-amine. Also disclosed is a process of preparing the hemi-tartrate of compound of formula (I-A) comprising: Dissolving the compound of formula (I-A) in an organic solvent forming a solution; Heating said solution to a first temperature in the range of from about 35 DEGREE C to about reflux; Adding L-tartaric acid to form a tartrate solution; and Heating said tartrate solution to a second temperature in the range of from about 50 DEGREE C to about reflux to form a heated mixture. Further disclosed is a process for the recrystallization of a hemi-tartrate of compound of formula (I-A) comprising: Dissolving the hemi-tartrate of compound of formula (I-A) in a mixture of water and an organic solvent, or in a mixture of organic solvents; and Removing a sufficient amount of water to yield a mixture with a boiling point of between about 78 DEGREE C and about 80 DEGREE C.
Bibliography:Application Number: NZ20090599747