Vito Nv

Janssen Pharmaceutica Nv

Janssen Pharmaceuticals, Inc.

Janssen R&d Ireland

Vlaamse Instelling Voor Technologisch Onderzoek (vito)

Vlaamse Instelling Voor Technologisch Onderzoek

Dominic Ormerod

Andras Horvath

Dominique Paul Michel Depré

Anita Buekenhoudt

Yamini Satyawali

Karolien Vanbroekhoven

Claudia Matassa

Veronique Cerpentier

Helmut Elslander

Pieter Vandezande

Matthieu Dorbec

Wim Porto-Carrero

A method and a device are disclosed for converting at least one reactant into a reaction product and separating the at least one reactant. The device includes a vessel with a vessel inner volume and a confinement, submerged in the vessel inner volume, that provides a confinement inner volume in fluid connection with the vessel inner volume. First and seconds fluids, with a respective, higher first density and a lower, second density form respective lower and upper phases in the vessel inner volume. A third fluid with a third density higher than that of the second fluid forms a lower layer in the confinement inner volume, relative to an upper layer formed by the second fluid. The third fluid may be the same as or different from, and is physically separated from, the first fluid. At least one of the first, second, and third fluids is at most partly miscible with the other two, but preferably immiscible. The at least one reactant and the reaction product have different affinities for at least two of the first, second, and third fluids, and at least one of the first and third fluid contains a fourth phase which is a solid or semi solid and is capable of promoting the conversion.

Device and method for converting and separating at least one reactant and a reaction product thereof

A method for producing a chiral amine may include performing a transamination reaction of a prochiral amino acceptor and an amino donor in a first solution in the presence of a transaminase, thereby forming a chiral amine and a co-product in the first solution. The amino donor is a high molecular weight (HMW) amino donor. In some examples, the molecular weight of the HMW amino donor is at least 150 g/mol. In some examples, the amino donor is affixed on a support, the total molecular weight of the amino donor and the support being at least 150 g/mol.

Method for producing chiral amines

A membrane based separation method is for the separation or enrichment of one or more unsaturated compounds from mixtures of chemically similar organic compounds having a different degree of unsaturation, using a membrane, such as an inorganic membrane, functionalized with a metal, such as silver. An inorganic membrane, preferably modified or grafted with an organic functional group, is further functionalized with a metal, such as silver, for use in the membrane based separation methods.

Separation of unsaturated organic compounds

A membrane based process separates amines or organic acids from a solution containing at least one amine or at least one organic acid according to their hydrophobic properties. The more hydrophobic amine or organic acid passes the hydrophobic membrane into an acidic aqueous solution, thus selectively removing the amine or organic acid from the first solution. The process is particularly suitable to obtain chiral amines in high yield. A transaminase-catalyzed transamination of an amino donor and amino acceptor is combined with a hydrophobic membrane separation of the produced chiral amine. The selective removal of the chiral amine from the reaction mixture promotes the further transformation of the amino acceptor into the product chiral amine.

Process for the separation of organic compounds

Provided herein are processes for carrying out a chemical reaction of a substrate in a diluted reaction mixture. The processes include conducting the reaction mixture having reaction product and solvent to a filtration membrane which is permeable to the solvent but impermeable to the reaction product. Solvent which permeates the filtration membrane for dilution of the substrate feed is recycled.

Reaction process with membrane separation

Disclosed is a process for carrying out a cyclization reaction, a polymerization reaction, an enzymatic reaction showing substrate inhibition, an enzymatic reaction showing product inhibition, a reaction showing precipitation of the substrate or of a reactant, the process comprising the steps of

Dilute chemical reaction process with membrane separation step

A process for preparing [(1R,2R)-4-oxo-1,2-cyclopentanedicarboxylic acid II, by the resolution of racemic 4-oxo-1,2-cyclopentanedicarboxylic acid (V), said process comprising:

Processes and intermediates for preparing a macrocyclic protease inhibitor of HCV

Disclosed is a process for the preparation of a cinchonidine salt of formula (IV) via an aqueous solution of a racemic 4-hydroxy-1,2-cyclopentanedicarboxylic acid, which is subjected to cyclization without removing water, by the addition of a water-miscible organic solvent to the aqueous solution and, again without removing water, adding cinchonidine to the aqueous-organic solvent solution so as to obtain the cinchonidine salt of the lactone acid. The cinchonidine salt is allowd to crystallize so as to obtain the enantiomerically purified crystalline lactone acid cinchonidine salt (IV). The enantiomerically pure salt is an intermediate in the synthesis of HCV inhibitor compound of formula (I). 

The present invention relates to the cinchonidine salt useful in the preparation of intermediates for preparing a macrocyclic HCV inhibitor, as well as processes involving this salt.

Processes and intermediates for preparing a macrocyclic protease inhibitor of hcv

The present invention relates to synthesis procedures and intermediates of a compound of formula: and the salts thereof.

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Hoogstraten, Belgium

Dominic Ormerod