[EN] CRYSTALLINE SOLID FORM OF (2S-5Z)-2-AMINO-7-(ETHANIMIDOYLAMINO)-2-METHYLHEPT-5-ENOIC ACID<br/>[FR] FORME CRISTALLINE SOLIDE DE L'ACIDE (2S-5Z)-2-AMINO-7-(ETHANIMIDOYLAMINO)-2-METHYLHEPT-5-ENOIQUE
申请人:PHARMACIA CORP
公开号:WO2004018412A1
公开(公告)日:2004-03-04
(2S,5Z)-2-amino-7-(ethanimidoylamino)-2-methylhept-5-enoic acid is crystallized as an anhydrous, stoichiometric 1.5 HCl salt and a scaleable crystallization method is disclosed. The salt form was characterized and the absolute configuration of the chiral center was confirmed as 'S'. (2S,5Z)-2-amino-7-(ethanimidoylamino)-2-methylhept-5enoic acid was high melting and appears acceptably non-hygroscopic for use in a pharmaceutical composition.
(2S,5Z)-2-氨基-7-(乙烯基氨基)-2-甲基庚-5-烯酸以无水、化学计量比为1.5的盐酸盐形式结晶,并披露了一种可扩展的结晶方法。盐的形式进行了表征,并确认手性中心的绝对构型为'S'。(2S,5Z)-2-氨基-7-(乙烯基氨基)-2-甲基庚-5-烯酸具有高熔点,看起来在制药组合物中具有可接受的不吸湿性。