Abstract: The invention relates to the methods for preparation of olanzapine polymorphic Form I. The invention also provides new mixed solvates of olanzapine, which are valuable intermediates used in the preparation of pure olanzapine polymorphic Form I.
Abstract: The present invention is a process for the preparation of 17?-hydroxy-7?-methyl-19-nor-17?-pregn-5(10)-en-20-yn-3-one (17?-ethynyl-17?-hydroxy-7?-methyl-5(10)-estren-3-one, tibolone) of formula 1, which comprises hydrolysis of 17?-ethynyl-17?-hydroxy-7?-methyl-5(10)-estrene 3,3-cyclic ketals of formula 2, where groups R1, R2, R3 and R4 are hydrogen atoms or alkyl groups, or R1 and R3, taken together with the carbon atoms within the dioxolane ring to which they are attached, form an alicyclic ring fused to the dioxolane ring, with R2 and R4 being hydrogen atoms, or R1 and R3 together with the carbon atoms to which they are attached form an aromatic ring fused to the dioxolane ring, where R2 and R4, taken together, form a chemical bond within said aromatic ring.
Type:
Application
Filed:
October 1, 2003
Publication date:
May 25, 2006
Applicant:
Institut Farmaceutyczny
Inventors:
Jacek Martynow, Andrzej Kutner, Wieslaw Szelejewski, Wanda Wojciechowska, Hanna Fitak
Abstract: The invention relates to the methods for preparation of olanzapine polymorphic Form I. The invention also provides new mixed solvates of olanzapine, which are valuable intermediates used in the preparation of pure olanzapine polymorphic Form I.