Bayer Aktiengesellschaft

Hermann Schutt

Michael Preiss

The present invention relates to an improved process for the preparation of 1-desoxynojirimycin. 1-Desoxynojirimycin can be reacted by alkylation on the nitrogen atom to give various saccharase inhibitors which are used therapeutically in the treatment of diabetes mellitus.

Enzymatic deacylation of acyl-aminosorboses

The invention relates to a process for the stereo-selective resolution of DL-phenylglycine derivatives by hydrolyzing the ester or amide groups of N-acyl-L-phenylglycine esters or amides in N-acyl-DL-phenylglycine esters or amides by the action of enzymes, separating the N-acyl-D-phenylglycine esters or amides from the N-acyl-L-phenylglycines and then, if appropriate, subjecting the ester or amide groups of the D-enantiomers and the acyl groups to acid hydrolysis, characterized in that enzyme which are bonded to carriers are allowed to act on the N-acyl-DL-phenylglycine esters or amides in an inert two-phase mixture consisting of water-immiscible organic solvent and water.

Stereoselective resolution of phenylglycine derivatives with enzyme

The invention relates to a process for the preparation of the highly pure enzyme kallikrein from organ extracts, in particular from swine pancreas extracts, the accompanying proteolytic activity of the swine pancreas extract being separated off by chromatography on ion exchangers and the highly pure enzyme kallikrein being obtained by chromatography on support materials with a kallikrein-trypsin inhibitor (basic pancreatic trypsin inhibitor=BPTI) covalently bonded in a particular manner.

Process for the preparation of the highly pure enzyme kallikrein from

The invention relates to optically pure heterocyclic amino acid compounds of the Formula I, as described hereinabove as well as a process for their preparation involving subject D, L-compounds to the action of a proteolytic enzyme. The compounds obtained are useful, inter alia, as intermediates for the manufacture of cephalosporins or penicillins.

Optically pure heterocyclic aminoacid compounds, a process for their use

The invention relates to a new enzymatic process for the stereoselective resolution of a DL-phenylglycine derivative comprising hydrolyzing an ester or amide group on an N-acyl-L-phenylglycine ester or amide in an N-acyl-DL-phenylglycine ester or amide in solution by the action of an enzyme bonded to a carrier, separating the N-acyl-D-phenylglycine ester or amide from the N-acyl-L-phenylglycine and then, if desired, hydrolyzing under acid conditions, the ester or amide group of the D-enantiomer and the acyl group. D-Phenylglycine and D-4-hydroxyphenylglycine are used as starting substances for the preparation of semisynthetic antibiotics of the penicillin series. L-Phenylglycine is a starting substance for L-aspartyl-L-phenylglycine methyl ester, which is used as a sweetener.

Stereoselective resolution of phenylglycine derivatives and

The kallikrein-trypsin inhibitor is obtained from animal organs by proteolytic digestion of the organ at an elevated temperature and recovery of kallikrein-trypsin inhibitor by selective adsorption thereof on carrier-bound trypsin and subsequent desorption.

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Wuppertal, Germany

Hermann Schutt