Menarini Ricerche S.p.a.

Menarini Richerche S.p.a.

Raffaello Giorgi

Carlo Mannucci

Antonio Giachetti

Anita Falezza

Carlo Alberto Maggi

Danilo Giannotti

Cristina Di Bugno

Monocyclic compounds with four bifunctional residues having NK-2 antagonist action

A process for the preparation of polymorph A of zofenopril calcium salt in substantially pure form, which comprises: a) reaction of S(&minus;)-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 a zofenopril potassium salt aqueous solution to a CaCl aqueous solution at a temperature of 70-90&deg; C. with simultaneous seeding to promote the precipitation of polymorph A.

Process for the preparation of zofenopril calcium salt

A process for the preparation of polymorph A of zofenopril calcium salt in substantially pure form, which comprises: 1) reaction of S(&minus;)-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 poyassium 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 aqueous solution at a temperature of 70-90&deg; C. with simultaneous seeding to promote the precipitation of polymorph A.

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Pomezia, Italy

Raffaello Giorgi