Sandoz Ag

Meda Ab

Meda Pharma Gmbh & Co. Kg

Dominic De Souza

Martin Albert

Hubert Sturm

Joerg Salchenegger

Andreas Berger

Abhinay C Pise

Sachin Bhuta

Martin Langner

Kerstin Knepper

Michael Oberhuber

Helmut Schwab

Thorsten Wilhelm

Shreerang V Joshi

Dattatraya N Chavan

Daniel Luschnig

Shashikant D Metkar

Ferdinand Zepeck

Hans-Peter Spitzenstaetter

Werner Hasselwander

Ajna Lukic

Aljaz Kajtna

Waander Riethorst

Borut Gabriel

Peter Remler

Doris Osl

Anja Lukic

Alja Kajtna

Jörg Salchenegger

Hans-Peter SPITZENSTÄTTER

The present disclosure is directed to an improved process to convert crude ascomycin to purified pimecrolimus. Crude ascomycin is chlorinated with triphenylphosphine and N-chlorosuccinimide (NCS) to yield crude pimecrolimus, which is then purified further by HPLC and subsequent crystallization. The processes of the present disclosure enable the removal of close homologs of pimecrolimus by high-pressure liquid chromatography without prior purification of the ascomycin starting material. This improvement may make the conversion of ascomycin to pimecrolimus industrially applicable and less expensive.

Process to convert technical ascomycin into purified pimecrolimus

The present invention relates to a process for the preparation of a hydrogen chloride (HCl) salt of a compound of formula (I) wherein Yand Yare independently F or Cl, preferably F, said compound of formula (I) containing the cis-isomer and the trans-isomer, wherein the process comprises (1) providing the compound of formula (I) comprised in a first suitable solvent; and (2) treating the compound of formula (I) comprised in the first suitable solvent with HCl comprised in a second suitable solvent to obtain the HCl salt of the compound of formula (I). 

Purification of posaconazole and of posaconazole intermediates

The present invention relates to a process for the preparation of a chiral compound according to formula (V) wherein Ris preferably an alkyl residue preferably having from 1 to 6 carbon atoms, in particular to a process for the preparation of a chiral compound the crystalline chiral compounds as such, and their use for the preparation of an antifungal agent, in particular posaconazole. 

Process for the preparation of chiral hydrazides

The present invention relates to process for the preparation of a chiral compound of formula (IX) or a salt thereof, wherein Yand Yare independently F or Cl, preferably F, the crystalline compound of formula (IX) as such, and its use for the preparation of an antifungal agent. 

Preparation of posaconazole intermediates

A process for the preparation of a chiral compound, in particular posaconazole, wherein the process comprises mixing and reacting the compounds of formula (I) Y&#x2014;NH; of formula (IIa) 0=C&#x2550;N&#x2014;Yand/or of formula (IIb) and of formula (III) in a solvent in any order to obtain a reaction mixture containing a chiral compound of formula (IV) and/or formula (V). 

Process for the preparation of chiral triazolones

The present invention relates to a process for the purification of crude bimatoprost to obtain pure bimatoprost comprising a chromatography, preferably a chromatography using an achiral stationary phase and an eluent comprising an alcohol and an apolar solvent; and crystallization of the product obtained the chromatography to obtain pure bimatoprost.

Process for the production of bimatoprost

The present invention relates to the use of a compound having the formula (II) for the preparation of a compound having the formula (V). Methods of preparing the compound having the formula (V) using the compound having the formula (II) are also described. Individual reaction steps as well as intermediates are additionally claimed. 

Method for the preparation of rivoraxaban

The present invention relates to processes for the preparation of 5-methyl-3-nitromethyl-hexanoic acid ester and its salts. Also disclosed are processes for the preparation of 5-methyl-3-nitromethyl-hexanoic acid salt and a process for the preparation of 3-(aminomethyl)-5-methylhexanoic acid. (S)-5-Methyl-3-nitromethyl-hexanoic acid or (R)-5-methyl-3-nitromethyl-hexanoic acid in enantioenriched form or enantiopure form as well as salts thereof, (S)-5-methyl-3-nitromethyl-hexanoic acid ester or (R)-5-methyl-3-nitromethyl-hexanoic acid ester in enantioenriched form or enantiopure form and a compound, namely Formula (XIII), in racemic form, enantioenriched form or enantiopure form are also disclosed. 

Process for the stereoselective enzymatic hydrolysis of 5-methyl-3-nitromethyl-hexanoic acid ester

The present invention relates to an improved process for the production of prostaglandins and prostaglandin analogs. In particular, this invention relates to the production of prostaglandins of the PGF-series, including latanoprost, travoprost, and bimatoprost, which are active pharmaceutical ingredients used for the reduction of elevated intra-ocular pressure in patients with glaucoma and ocular hypertension.

Process for the production of prostaglandins and prostaglandin analogs

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Kundl, Austria

Dominic De Souza