W. R. Grace Co.-conn.

W. R. Grace Co.

Robert J Kupper

Akiva T Gross

Alan B Chmurny

Rowena L Roberts

Jennifer M Quirk

Charles G Carter

Felek Jachimowicz

Christer L Hakansson

Synthesis of phenylserine ester (a) via benzaldehyde and glycine ester using serine hydroxymethyltransferase; and (b) via methyl benzoylacetate. Synthesis of hydroxy-aspartame or derivative by enzymatic coupling of phenylserine or derivative with aspartic acid or derivative. Hydrogenation of the coupled product to give as final product aspartame or analog with related processes and products.

Process for preparing as partyl-phenylalanine dipeptides

A hydroxy-carboxylate ester is converted to an amino-acid-amide by replacement of the --OH group with --N.sub.3, via, e.g., CH.sub.3 SO.sub.2 Cl and NaN.sub.3 ; reacting with amine to convert the ester to amide; and hydrogenating --N.sub.3 to --NH.sub.2. The present process alleviates the conventional use of blocking-deblocking procedures.

Preparation of amino acid derivatives

A process of forming 2-bromo-2-nitro-1,3-propanediol by contacting a 5-nitro-1,3-dioxane with bromine under alkaline conditions and hydrolyzing the brominated product.

Novel process for the preparation of bronopol

A process to decolorize and stabilize nitro compounds by contacting the nitro compound with an alkaline earth metal hypochlorite particulate material.

Decolorization

Aspartyl-beta substituted phenylalanine dipeptides

Formylating the amino nitrogen of an alkali metal salt of an amino carboxylic acid, by reacting the salt with an alkyl formate in an alkanol solvent. In one embodiment, the alkyl formate is added to the reaction as such; in another embodiment, the alkyl formate is formed in situ by reaction of carbon monoxide with the alkanol solvent in the presence of the alkali metal salt of the amino carboxylic acid. The process provides a new class of compounds, the alkali metal salts of N-formyl-aspartic acids.

N-formylation of amino carboxylates with alkyl formates

Synthesis of phenylserine ester (a) via benzaldehyde and glycine ester using serine hydroxymethyltransferase; and (b) via methyl benzoylacetate. Synthesis of hydroxy-aspertame or derivative by enzymatic coupling of phenylserine or derivative with aspertic acid or derivative. Hydrogenation of the coupled product to give as final product aspertame or analog with related processes and products.

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Mt. Airy, MD, United States of America

Robert J Kupper