Abstract: The present invention relates to a crystalline form of an intermediate for cefoperazone of formula (1) and to a process for the preparation thereof by enzymatic condensation of a 3?-thiosubstituted ?-lactam nucleus with a phenylglycine derivative.

Abstract: The invention relates to a method for synthesizing a peptide by enzymatically preparing an ester or thioester from (i) an N-terminal protected amino acid or an N-terminal protected peptide where either can have a protected C-terminal ester group and (ii) an alcohol represented by the formula HO—CX2—Z or a thiol represented by the formula HS—CX2—Z, each X independently representing a halogen atom or a hydrogen atom; and Z represents an electron withdrawing group comprising at least one sp3-hybridized carbon comprising at least two substituents comprising a heteroatom directly attached to the at least one sp3-hybridized carbon or at least one sp2-hybridized carbon comprising one or two substituents comprising a heteroatom directly attached to the at least one sp2-hybridized carbon, and enzymatically coupling the prepared ester or thioester with an optionally C-terminal protected amino acid or with an optionally C-terminal protected peptide in a medium comprising 2 wt. % water or less.

Abstract: The present invention relates to a process for the preparation of 3?-thiosubstituted cephalosporins by enzymatic condensation of a nucleus with a phenylglycine derivative. Furthermore the present invention relates to a crystalline form of a compound of general formula (1) wherein R2 is OH and X is S and R1 is a radical of formula (2a) with R3 is CH3.

Abstract: The invention relates to a method for preparing an optionally N-protected amino acid C-terminal ester or an optionally N-protected peptide C-terminal ester, comprising transesterifying the C-terminal t-alkyl ester of the amino acid or the C-terminal t-alkyl ester of the peptide with an alcohol (other than the t-alcohol corresponding to the t-alkyl group of the ester) in the presence of a hydrolytic enzyme (E.C. 3). The invention further relates to a method for preparing a peptide comprising coupling an activated, N-protected, amino acid C-terminal ester or an optionally N-protected peptide C-terminal ester with an optionally C-terminal protected amino acid or an optionally C-terminal protected peptide via a peptide bond, in the presence of an enzyme catalysing peptidic bond formation.

Abstract: Method for enzymatically synthesising a peptide, comprising enzymatically preparing an ester or a thioester from (i) an N-terminal protected amino acid, an N-terminal protected amino acid C-terminal ester, an N-terminal protected peptide, or an N-terminal protected peptide C-terminal ester and (ii) an alcohol represented by the formula HO—CX2—Z respectively a thiol represented by the formula HS—CX2—Z, each X independently representing a halogen atom or a hydrogen atom; and Z being selected from the group of sp3-hybridised carbons comprising at least two substituents comprising a heteroatom directly attached to the sp3-hybridised carbon and sp2-hybridised carbons comprising one or two substituents comprising a heteroatom directly attached to the sp2-hybridised carbon, the preparation of the ester or thioester being carried out in a reaction medium comprising 2 wt.

Abstract: The present invention relates to a method for selective conjugation of bioactive moieties to a polymer or polymerisable compound. The method is more specifically related to the selective conjugation of bioactive moieties to a pendant carboxylic acid, ester or thioester group in which the pendant group is part of a polymer or a polymerisable compound, wherein the method comprises contacting the polymer or polymerisable compound with a hydrolytic enzyme to catalyse the conjugation between the bioactive moiety and the pendant carboxylic acid, ester or thioester group. The conjugation of the bioactive moieties may occur prior to, during or after polymerization of the polymerisable compound. The conjugation of the bioactive moieties may also occur after the polymer is given a form.

Abstract: The present invention relates to a method for selectively hydrolysing a pendant ester bond formed by an unsubstituted or substituted hydrocarbon group—optionally comprising one or more heteroatoms—and a pendant carboxylate moiety, which carboxylate moiety is part of a polymer or a polymerisable compound, which polymer or polymerisable compound comprises at least one other hydrolysable group, wherein the method comprises contacting the polymer or polymerisable compound with a hydrolytic enzyme.

Abstract: The invention relates to a method for preparing an optionally N-protected amino acid C-terminal ester or an optionally N-protected peptide C-terminal ester, comprising transesterifying the C-terminal t-alkyl ester of the amino acid or the C-terminal t-alkyl ester of the peptide with an alcohol (other than the t-alcohol corresponding to the t-alkyl group of the ester) in the presence of a hydrolytic enzyme (E.C. 3). The invention further relates to a method for preparing a peptide comprising coupling an activated, N-protected, amino acid C-terminal ester or an optionally N-protected peptide C-terminal ester with an optionally C-terminal protected amino acid or an optionally C-terminal protected peptide via a peptide bond, in the presence of an enzyme catalysing peptidic bond formation.