L-Glufosinate Enzymatic Conversion for Stereoisomer Purity

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Solution Overview

Problem

Current commercial methods for producing glufosinate yield a racemic mixture of L- and D-glufosinate, with L-glufosinate being more potent, and there is a need for cost-effective methods to produce pure L-glufosinate or a mixture enriched for L-glufosinate.

Innovation Solution

A two-step process involving oxidative deamination of D-glufosinate to PPO using a mutant D-amino acid oxidase enzyme, followed by amination of PPO to L-glufosinate with a transaminase enzyme, utilizing amine donors, to achieve a substantial conversion of D-glufosinate to L-glufosinate.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Manufacturing precision

If current commercial chemical synthesis methods are used, then glufosinate can be produced, but only a racemic mixture of L- and D-glufosinate is obtained with reduced potency

Engineering Contradiction:
Improvestereoisomer purityVSAvoidproduction complexity
Core Design Contradiction:
Manufacturing precisionVSEase of manufacture

Solution Approach 1:

The synthesis process is divided into distinct enzymatic steps: first oxidative deamination of D-glufosinate to PPO using DAAO, then amination of PPO to L-glufosinate using transaminase. This segmentation allows each step to be optimized for stereoselectivity, achieving high L-glufosinate purity through controlled sequential transformations rather than attempting single-step synthesis.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

PPO (2-oxo-4-(hydroxy(methyl)phosphinoyl)butyric acid) serves as an intermediary compound in the synthesis pathway. The DAAO enzyme mediates the conversion of D-glufosinate to PPO, and the transaminase mediates the conversion of PPO to L-glufosinate. This intermediary approach enables stereoselective transformation through enzyme-catalyzed steps that would be difficult to achieve through direct chemical synthesis.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Manufacturing precision

If enzymatic methods with mutant DAAO are used, then L-glufosinate can be produced with high stereoselectivity, but enzyme development and optimization are required

Engineering Contradiction:
Improvestereoisomer purityVSAvoidenzyme system complexity
Core Design Contradiction:
Manufacturing precisionVSDevice complexity

Solution Approach 1:

The DAAO enzyme has been mutated to alter its kinetic parameters, specifically achieving an increased activity of about 3 µmol/min*mg or greater. The mutant DAAO comprises specific amino acid substitutions (F58K and M213S or N54V, F58Q, and M213S) that change the enzyme's catalytic efficiency and substrate specificity, enabling it to effectively drive the oxidative deamination reaction for high L-glufosinate production.

Inventive Principle:
Principle #35Parameter changes

3Productivity

If amine donors are used in the amination step, then L-glufosinate can be produced efficiently, but unreacted amine donor requires separation or reuse

Engineering Contradiction:
Improveconversion efficiencyVSAvoidamine donor recovery
Core Design Contradiction:
ProductivityVSLoss of substance

Solution Approach 1:

The patent addresses the handling of unreacted amine donor by providing options to either separate and recover it from the reaction mixture or reuse it in further rounds of reaction. This approach maximizes the utility of the amine donor substrate, reducing waste and improving the overall economics of the process by maintaining high conversion efficiency while minimizing material loss.

Inventive Principle:
Principle #34Discarding and recovering

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The method enables the production of a composition predominantly comprising L-glufosinate, with at least 70% conversion efficiency, allowing for effective use as a herbicide with reduced amounts.

Implementation Method 1

The first step involves the oxidative deamination of D-glufosinate to PPO (2-oxo-4-(hydroxy(methyl)phosphinoyl)butyric acid)

Methodology Applied
Scientific EffectOxidative deamination: Oxidation

Implementation Method 2

reacting D-glufosinate with a D-amino acid oxidase (DAAO) enzyme to form PPO

Methodology Applied
Scientific EffectEnzyme catalysis: Enzyme

Implementation Method 3

the method involves reacting D-glufosinate with a D-amino acid oxidase (DAAO) enzyme to form PPO (2-oxo-4-(hydroxy(methyl)phosphinoyl)butyric acid); followed by aminating the PPO to L-glufosinate by a transaminase (TA) enzyme, using an amine group from one or more amine donors

Methodology Applied
Scientific EffectTransamination:

Data Source

PatentEP3423585B1Methods for making l-glufosinate
Publication Date: 2026.04.08 BASF SE
  • EP3423585B1 patent drawingFigure 1
  • EP3423585B1 patent drawingFigure 2
  • EP3423585B1 patent drawing

AI summary

Methods for the production of L-glufosinate (also known as phosphinothricin or (S)-2-amino-4-(hydroxy(methyl)phosphonoyl)butanoic acid) are provided. The methods comprise a two-step process. The first step involves the oxidative deamination of D-glufosinate to PPO (2-oxo-4-(hydroxy(methyl)phosphinoyl)butyric acid). The second step involves the specific amination of PPO to L-glufosinate, using an amine group from one or more amine donors. By combining these two reactions, the proportion of L-glufosinate in a mixture of L-glufosinate and D-glufosinate can be substantially increased.