Abstract: Synthesis methods for the preparation of intermediates which are suitable for the preparation of statin derivatives, and especially to synthesis methods for the intermediate of formula (VI) wherein Ra? and Rc? are each independently of the other hydrogen or hydroxy-protecting group, or together are a bridging hydroxy-protecting group; and Rb is a carboxy-protecting group.

Abstract: Synthesis methods for the preparation of intermediates which are suitable for the preparation of statin derivatives, and especially to synthesis methods for the intermediate of formula (VI) wherein Ra? and Rc? are each independently of the other hydrogen or hydroxy-protecting group, or together are a bridging hydroxy-protecting group; and Rb is a carboxy-protecting group.

Abstract: The invention relates to novel synthesis methods for the preparation of the intermediates, which are suitable for the preparation of statin derivatives, especially to novel synthesis methods of the intermediate of formula VI wherein Ra? and Rc? are each independently of the other hydrogen or a hydroxy-protecting group or together are a bridging hydroxy-protecting group, and Rb is a carboxy-protecting group, which methods are carried out by conversion of the intermediate of formula XVI wherein Ra? and Rc? are each independently of the other hydrogen or a hydroxy-protecting group, R* and R** are each independently of the other hydrogen or an amide-protecting group, and Rb is a carboxy-protecting group; which methods proceed to further new intermediates and methods for their preparation

Abstract: A crystalline form of sertraline hydrochloride was found, referred to hereinafter as polymorphic form CSC2 having a dissolution rate which surprisingly will increase rate of absorption of a drug. Furthermore, different crystalline forms of sertraline hydrochloride alcohol solvates, crystalline forms of sertraline hydrochloride hydrates, referred to hereinafter as polymorphic form CSC1, a process for the preparation of the amorphous form of sertraline hydrochloride, and different processes for the preparation of polymorphic forms I, II, V, and T1 are disclosed.

Abstract: An improved process for the preparation of sertraline hydrochloride polymorphic form II is described, which process comprises seeding a solution of sertraline free amine in a ketone with some crystals of polymorphic form II and addition of hydrogen chloride, and wherein the solution is heated before addition of the hydrogen chloride. According to the present process, the metastable form II may be obtained in a reliable way with good yield and high purity with respect to other polymorphic forms as well as preparative residues such as educts or solvents.

Abstract: A cystalline form of sertraline hydrochloride was found, referred to hereinafter as polymorphic form CSC2 having a dissolution rate which surprisingly will increase rate of absorption of a drug. Furthermore, different crystalline forms of sertraline hydrochloride alcohol solvates, crystalline forms of sertraline hydrochloride hydrates, referred to hereinafter as polymorphic form CSC1, a process for the preparation of the amorphous form of sertraline hydrochloride, and different processes for the preparation of polymorphic forms I, II, V, and T1 are disclosed.

Abstract: The invention relates to novel synthesis methods for the preparation of the intermediates, which are suitable for the preparation of statin derivatives, especially to novel synthesis methods of the intermediate of formula VI wherein Ra′ and Rc′ are each independently of the other hydrogen or a hydroxy-protecting group or together are a bridging hydroxy-protecting group, and Rb is a carboxy-protecting group, which methods are carried out by conversion of the intermediate of formula XVI wherein Ra′ and Rc′ are each independently of the other hydrogen or a hydroxy-protecting group, R* and R** are each independently of the other hydrogen or an amide-protecting group, and Rb is a carboxy-protecting group; which methods proceed to further new intermediates and methods for their preparation.

Abstract: The present invention relates to a process for the preparation of compounds of formula (1), in which R1, R2 and R3 independently of one another are hydrogen, halogen , trifluoromethyl of or C1-C4alkoxy, wherein a compound of formula (2), in which R1, R2 and R3 are as defined in formula (1), is reacted with methlyamine in the presence of a non-alcoholic solvent and, if desired, in the presence of a sulfonic acid catalyst to give the compound of formula (2) and, if desired, is subject to purification by recrystallization.

Abstract: A crystalline form of sertraline hydrochloride was found, referred to hereinafter as polymorphic form CSC2 having a dissolution rate which surprisingly will increase rate of absorption of a drug.

Abstract: Described is a process for the preparation of compounds of formula (1a) which comprises reacting an isomeric mixture consisting of from 75 to 95% of compound of formula (2a) and from 5 to 25% of a compound of formula (2b) with methylamine, in a suitable solvent, to form a sertraline-imine isomeric mixture consisting of from 75 to 95% of formula (1a) and from 5 to 25% of formula (1b)(A1), or reacting an isomeric mixture consisting of from 75 to 95% of a compound of formula (2a) and from 5 to 25% of a compound of formula (2b) with methylamine, in a suitable solvent, using suitable methods of isolation to form an enriched sertraline-imine isomeric mixture, consisting of >99% of a compound of formula (1a) and <1% of a compound of formula (1b)(A2); and then subjecting the sertraline-imine isomeric mixture obtained according to reaction route (A1) or (A2), in a suitable solvent, to recrystallisation (B), in accordance with scheme (I) wherein in formula (1a), R1, R2 and R3 are each independently of the others

Abstract: Radiation-sensitive compositions comprising a substance which forms acid under the action of actinic radiation and polymers based on combination of different repeating units derived from hydroxy styrene and hydroxy-vinylcyclohexane derivatives wherein a portion of the hydroxyl groups are replaced with either acid-labile acetal or ketal protecting groups and where a portion of the repeating groups comprise two crosslinked species connected via the protecting groups.

Abstract: Polymers based on combination of different repeating units derived from hydroxy styrene and hydroxyvinylcyclohexane derivatives wherein a portion of the hydroxyl groups are replaced with either acid-labile acetal or ketal protecting groups and where a portion of the repeating groups comprise two crosslinked species connected via the protecting groups.

Abstract: A process for the preparation of phenolic resins having acid-labile acetal or ketal protecting groups by reacting a phenolic resin with an enol ether in the presence of an acidic catalyst and subsequently treating the reaction mixture with a basic anion exchanger gives heat-resistant polymers which, in combination with acid photogenerators, produce radiation-sensitive compositions of high processing stability with a greatly improved shelf life.