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New process for the synthesis of strontium ranelate and its hydrates.
专利权人:
LES LABORATOIRES SERVIER
发明人:
VAYSSE-LUDOT LUCILE,LECOUVE JEAN-PIERRE,LANGLOIS PASCAL
申请号:
AP2008004617
公开号:
AP2400A
申请日:
2008.09.15
申请国别(地区):
AP
年份:
2012
代理人:
摘要:
Synthesizing strontium ranelate compounds (I) and their hydrates, comprises: reacting 3-cyano thiophene compound (II) with soda or potash, in water or mixture of water and organic solvent at 0-100[deg] C, to give a salt of 5-(bis-carboxymethyl-amino)-3-carboxymethyl-4-cyano-thiophene-2-carboxylic acid (III); and reacting strontium chloride with mixture of water and organic solvent at 0-100[deg] C to give (I), after the isolation. Process for synthesizing strontium ranelate compounds of formula (I) and its hydrates, comprises: reacting 3-cyano thiophene compound of formula (II) with soda or potash, in water or mixture of water and organic solvent at 0-100[deg] C, to give a salt of 5-(bis-carboxymethyl-amino)-3-carboxymethyl-4-cyano-thiophene-2-carboxylic acid of formula (III); and reacting strontium chloride with mixture of water and organic solvent at 0-100[deg] C to give (I), after the isolation. R, R1 : 1-6C alkyl, preferably CH 3; and A : Na or K. An independent claim is included for a potassium salt of 5-(bis-carboxymethyl-amino)-3-carboxymethyl-4-cyano-thiophene-2-carboxylic acid of formula (IIIb). [Image] [Image] [Image] ACTIVITY : Osteopathic. MECHANISM OF ACTION : None given.
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