Abstract: A process for the preparation of a chiral compound, in particular posaconazole, wherein the process comprises mixing and reacting the compounds of formula (I) Y3—NH2; of formula (IIa) 0=C?N—Y0 and/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).

Abstract: 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.

Abstract: 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 PGF2?-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.

Abstract: This invention relates to processes and intermediates for the stereoselective alkylation of carbonyl groups. The invention in particular allows the stereoselective preparation of the antidepressant drug escitalopram. It has been found that boric or boronic acid derivatives are useful bridging elements for the attachment of a chiral group to a compound containing a carbonyl group to be alkylated. The said borates and boronates are thus useful in a process for the asymmetric alkylation of a carbonyl group in a compound containing a carbonyl group and an anchor group capable of reacting with a boric or boronic acid derivative. The asymmetric alkylation can be carried out by admixing the compound containing a carbonyl group to be alkylated and the anchor group capable of reacting with a boric or boronic acid derivative with a boric or boronic acid derivative, adding a chiral alcohol, and adding an organometallic compound. After the alkylation reaction, the borate and boronate can be easily removed by hydrolysis.

Abstract: The present invention relates to a method for the production of organic compounds, in particular sodium (6R,7R)-7-[(Z)-2-(5-amino-[1,2,4]thiadiazol-3-yl)-2-hydroxyimino-acetylamino]-8-oxo-3-[(E)-(R)-1?-(5-methyl-2-oxo-[1,3]-dioxol-4-ylmethoxycarbonyl)-2-oxo-[1,3?]bipyrrolidinyl-3-ylidenemethyl]-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylate (ceftobiprole medocaril), and compounds of the general formula (1) and of the general formula (2), the compounds themselves and intermediates in the production according to the invention.

Abstract: The present invention relates to a method for the production of organic compounds, in particular sodium (6R,7R)-7-[(Z)-2-(5-amino-[1,2,4]thiadiazol-3-yl)-2-hydroxyimino-acetylamino]-8-oxo-3-[(E)-(R)-1?-(5-methyl-2-oxo-[1,3]-dioxol-4-ylmethoxycarbonyl)-2-oxo-[1,3?]bipyrrolidinyl-3-ylidenemethyl]-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylate (ceftobiprole medocaril), and compounds of the general formula (1) and of the general formula (2), the compounds themselves and intermediates in the production according to the invention.

Abstract: 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 crystallisation of the product obtained the chromatography to obtain pure bimatoprost.

Abstract: The present invention relates to acid addition salts of aripiprazole, a process for preparing said acid addition salts and their use to prepare or purify aripiprazole in the form of a free base or in the form of a pharmaceutically acceptable salt.

Abstract: This invention relates to processes and intermediates for the stereoselective alkylation of carbonyl groups. The invention in particular allows the stereoselective preparation of the antidepressant drug escitalopram. It has been found that boric or boronic acid derivatives are useful bridging elements for the attachment of a chiral group to a compound containing a carbonyl group to be alkylated. The said borates and boronates are thus useful in a process for the asymmetric alkylation of a carbonyl group in a compound containing a carbonyl group and an anchor group capable of reacting with a boric or boronic acid derivative. The asymmetric alkylation can be carried out by admixing the compound containing a carbonyl group to be alkylated and the anchor group capable of reacting with a boric or boronic acid derivative with a boric or boronic acid derivative, adding a chiral alcohol, and adding an organometallic compound. After the alkylation reaction, the borate and boronate can be easily removed by hydrolysis.

Abstract: This invention provides processes for preparing cefepime, including crystalline intermediates of Formula V.

Abstract: The present invention provides a new method for preparation and crystallization of hydrochlorides, hydrobromides or hydroiodides of pharmaceutical compounds or their intermediates in which the base or its acid addition salt is reacted in a solvent with a Trialkylsilylhalogenide.

Abstract: 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 PGF2?-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.

Abstract: A process for the production of intermediates having a formula IA that can be used for the synthesis of cephalosporins, such as cefepime of formula V. The intermediates of formula IA are produced by desilyation of a compound of formula II wherein R4 is a silyl-protecting group, with a protic solvent to obtain a compound of formula III, and reacting the compound of formula III with an organic base of formula IV wherein R2 and R3 together represent a C4-alkylene group, and with the adjacent nitrogen atom form a saturated 5-membered heterocycle, and R1 represents a methyl group, to obtain the compound of formula 1A.

Abstract: The present invention relates to acid addition salts of aripiprazole, a process for preparing said acid addition salts and their use to prepare or purify aripiprazole in the form of a free base or in the form of a pharmaceutically acceptable salt.

Abstract: The invention belongs to the field of organic chemistry and relates to a new process for the purification of olanzapine comprising preparation of acid addition salts of olanzapine and transformation thereof into a pharmaceutically acceptable pure and discoloured final product. The present invention also relates to new processes for the preparation of pure olanzapine.

Abstract: The invention relates to a new process for the production of intermediates for the synthesis of caephalosporin of formula (I) wherein R1, R2 and R3, independently of one another, are alkyl, alkenyl, aryl, hydroxy(C1-6)alkyl, carbamoyl-(C1-6)alkyl, amino-(C1-6)alkyl, acylamino-(C1-6)alkyl or carboxy(C1-6)alkyl, or wherein R2 and R3 together with the adjacent nitrogen atom, form an alicyclic 5- to 8-membered heterocyclic ring, and R1 signifies alkyl, alkenyl or aryl. The process according to the invention is notable in that the formation of undesired by-products, especially ?2-analogous compounds of formula (I), is greatly reduced.

Abstract: This invention provides processes for preparing cefepime, including crystalline intermediates of Formula V.

Abstract: A process for the purification of cefixime via a novel tert-octylamine salt of a cefixime intermediate of formula V which may be crystalline and which may be produced in a one-pot reaction from 7-amino-3-vinyl-ceph-3-em-4-carboxylic acid.

Abstract: A process for the purification of cefixime via a novel tert.octylamine salt of a cefixime intermediate which may be crystalline and which may be produced in a one pot reaction from 7-amino-3-vinyl-ceph-3-em-4-carboxylic acid.

Abstract: Cefdinir in the form of a salt with dicyclohexylamine, a process for its production and its use in the purification of impure cefdinir.