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PROCESS FOR THE PREPARATION OF BENZOIMIDAZOL-2-YL PYRIMIDINE DERIVATIVES
专利权人:
JANSSEN PHARMACEUTICA N.V.
发明人:
CESCO-CANCIAN, SERGIO,GRIMM, JEFFREY, S
申请号:
NZ59974709
公开号:
NZ599747A
申请日:
2009.06.29
申请国别(地区):
NZ
年份:
2013
代理人:
摘要:
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.
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