Abstract: The present invention relates to a process for the preparation of statins by means of a Julia-Kocienski reaction between an aldehyde and a sulfone derivative in the presence of an alkaline metal alkoxy base. The resulting derivatives are suitable as building blocks for statin type compounds such as cerivastatin, fluvastatin, pitavastatin and rosuvastatin.

Abstract: The present invention relates to a process for the preparation of a 1-methyl-1H-tetrazole-5-thio derivative comprising reaction of a halomethyl substrate with 1-methyl-H-tetrazole-5-thiol to obtain a thio-ether compound, and oxidizing the thio-ether compound to the corresponding sulfone. In case of a chiral halomethyl substrate, the resulting chiral diol sulfone derivative is suitable as a building block for statin type compounds.

Abstract: The present invention relates to a mutant prokaryotic penicillin G acylase derived from a wild-type penicillin G acylase characterized in that the mutant is having an amino acid substitution at one or more amino acid positions selected from the group consisting of amino acid positions A3, A77, A90, A144 A192, B24, B109, B148, B313, B460 and B488 according to the amino acid numbering of the Escherichia coli penicillin G acylase having the amino acid sequence depicted in SEQ ID No: 1.

Abstract: Cefodroxil monohydrate is formed by a processing which includes a) bringing an aqueous solution of cefadroxil monohydrate to a pH of between 7 to 9 with a suitable titrant; b) lowering the pH to a value of between 5 and 6.5 to obtain a suspension of cefadroxil monohydrate in crystal form; and c) isolating the cefadroxil monohydrate in crystal form from the suspension obtained in step b). The cefadroxil monohydrate thereby obtained exhibits a CIE b value of below 6, and advantageously a CIE b value of below 12 when stored at a temperature of 25° C. for at least 1 month.

Abstract: The invention relates to salts of acids with 2-propyl esters of general formula (2) The invention also relates to a method for the preparation of salts of acids with compounds of general formula (2) and to the use thereof in the preparation of atorvastatin.

Abstract: The present invention describes a process for the synthesis of a semi-synthetic ?-lactam compound from a nucleus and a side chain selected from the group consisting of D-phenylglycine and D-dihydro-phenylglycine in the form of a side chain ester and an enzyme catalyzing the coupling of the side chain ester to the nucleus characterized in that the side chain ester is not isolated as a solid intermediate.

Abstract: The invention relates to compounds of general formula (3) wherein R4 is allyl, 2-butyl, cyclohexyl, 3-methyl-2-butyl or 4-methyl-2-pentyl, a method for the preparation of compounds of general formula (3) and their use in the preparation of atorvastatin.

Abstract: The present invention relates to a salt of a carboxylic acid with a diamine such as 2,2?-(ethylenedioxy)diethyl amine, 3,3?-(ethylenedioxy)dipropyl amine and 2,2?-oxybis(ethylamine) and a method of preparing such salts. Preferably the carboxylic acid is a fermentation product such as clavulanic acid, mycophenolic acid or pravastatin.

Abstract: The present invention relates to a process for the preparation of cefadroxil in crystal form, comprising a) adding an aqueous solution of cefadroxil to a crystallization vessel and a titrant to keep a pH in the crystallization vessel of between 7 to 9; and b) lowering the pH in the crystallization vessel to a value of between 5 and 6.5 to obtain a suspension of the ?-lactam compound in crystal form. The invention further relates to cefadroxil in crystal form obtainable by the process according to the present invention. The invention also relates to cefadroxil in crystal form with a CIE b value of below 12 when stored at a temperature of 25° C. for at least 1 month.

Abstract: The present invention relates to 5-substituted hydantoins, a process for the preparation of 5-substituted hydantoins and the use of 5-substituted hydantoins in the preparation of enantiomerically enriched ?-amino acids. Furthermore, the present invention relates to the preparation of pharmaceutically active products such as perindopril and ramipril using the novel 5-substituted hydantoins.

Abstract: The present invention relates to a method for the production of atorvastatin having decreased levels of impurity (3) by means of a pH-controlling step.

Abstract: The present invention relates to a method for the production of atorvastatin having decreased levels of impurities of general formulae (3) and (4) by means of a concentrating step.

Abstract: The present invention relates to a method for the purification of cyclopeptides of general formula (3) by means of a silicate.

Abstract: The present invention provides a method for the preparation of mycophenolate mofetil wherein mycophenolic acid or an amine salt of mycophenolic acid is esterified with 2-morpholinoethanol, the resulting mixture is extracted into water at a pH-value between 1.0 and 3.0, and mycophenolate mofetil is back-extracted in a water-immiscible solvent at a pH-value between 3.0 and 5.0.

Abstract: The present invention relates to a process for the preparation of octahydrocyclopenta[b]pyrrole-2-carboxylic acid and esters thereof of general formula (1) in the presence of a cobalt and/or nickel comprising catalyst and to the use of compounds of general formula (1) in the synthesis of ramipril.