The present invention relates to zofenopril calcium form A substantially free of other forms of zofenopril calcium and to zofenopril calcium having a chemical purity of more than 98.5%. The present invention also relates to methods of preparing such zofenopril calcium. It further relates to compositions comprising such zofenopril calcium. Zofenopril calcium, (4S)-1-[(2S)-3-benzoylthio-2-methylpropionyl]-4-(phenylthio)-L-proline calcium salt, has the following structure:
[EN] NOVEL CRYSTALLINE FORMS<br/>[FR] NOUVELLES FORMES CRISTALLINES
申请人:GENERICS UK LTD
公开号:WO2009106894A1
公开(公告)日:2009-09-03
The present invention relates to two novel crystalline forms of zofenopril calcium, to processes for their preparation and their use in pharmaceutical compositions.
[EN] NOVEL CRYSTALLINE FORM<br/>[FR] NOUVELLE FORME CRISTALLINE
申请人:GENERICS UK LTD
公开号:WO2009022168A1
公开(公告)日:2009-02-19
The present invention relates to a novel anhydrous crystalline form of zofenopril calcium of formula (I), chemically known as (4S)-1-[(2S)-3-(benzoylthio)-2-methylpropionyl]-4-(phenylthio)-L-proline calcium salt or hemi-calcium salt. The present invention further relates to a process for the preparation of the new crystalline form of zofenopril calcium, its use in pharmaceutical compositions and the use of the new crystalline form and compositions in the treatment of hypertension and various other diseases.
The present invention relates to a novel crystalline form of zofenopril calcium of formula (I), chemically known as (4S)-1-[(2S)-3-(benzoylthio)-2-methylpropionyl]-4-(phenylthio)-L-proline calcium salt. The present invention further relates to a process for the preparation of the new crystalline form of zofenopril calcium and its use in pharmaceutical preparations.
Process for the preparation of zofenopril calcium salt
申请人:MENARI RICERCHE S.P.A.
公开号:US20020156293A1
公开(公告)日:2002-10-24
A process for the preparation of polymorph A of zofenopril calcium salt in substantially pure form, which comprises: 1) reaction of S(-)-3-benzoylthio-2-methylpropanoic acid chloride with cis-4-phenylthio-L-proline in water at pH ranging from 9.0 to 9.5 and recovery of zofenopril in the acidic form; b) salification of acid zofenopril with a potassium salt in alcoholic solution, and recovery of the resulting potassium salt; c) conversion of the potassium salt to the calcium salt by addition of zofenopril potassium salt aqueous solution to a CaCl
2
aqueous solution at a temperature of 70-90° C. with simultaneous seeding to promote the precipitation of polymorph A.