Epothilone Fragment Fermentation and Chemical Conversion

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Solution Overview

Problem

There is a continuing need for more efficient methods to prepare epothilones and their derivatives, which are promising anticancer agents, as existing methods are not cost-effective for commercial development.

Innovation Solution

The development of new methods involving fermentation of organisms to obtain epothilone fragments, which are then chemically converted into epothilones, reducing manufacturing costs and facilitating their therapeutic use.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of manufacture

If fermentation methods are used to obtain epothilone fragments, then manufacturing cost is reduced, but process complexity increases due to combining biological and chemical steps

Engineering Contradiction:
Improvemanufacturing costVSAvoidprocess complexity
Core Design Contradiction:
Ease of manufactureVSDevice complexity

Solution Approach 1:

The epothilone molecule is divided into fragments that can be produced by fermentation, which are then chemically converted into the final product. This segmentation allows the complex synthesis to be broken into manageable biological and chemical stages, reducing overall manufacturing cost while maintaining controllable process complexity.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent combines fermentation processes with chemical conversion steps in a hybrid manufacturing approach. By merging biological fragment production with subsequent chemical synthesis, the method achieves cost reduction through fermentation while completing the molecular structure through established chemical procedures.

Inventive Principle:
Principle #5Merging (Combining)

2Device complexity

If existing preparation methods are used for epothilones, then process simplicity is maintained, but manufacturing cost remains high for commercial development

Engineering Contradiction:
Improveprocess simplicityVSAvoidmanufacturing cost
Core Design Contradiction:
Device complexityVSEase of manufacture

Solution Approach 1:

Fermentation-produced fragments serve as intermediary substances that bridge the gap between simple biological processes and the complex epothilone molecule. These intermediaries can be obtained through relatively simple fermentation, then converted through chemical steps to produce the final therapeutic agent at reduced cost.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Manufacturing precision

If total chemical synthesis is used for epothilones, then manufacturing precision can be controlled, but productivity is reduced due to high cost and complexity

Engineering Contradiction:
Improvesynthesis controlVSAvoidmanufacturing efficiency
Core Design Contradiction:
Manufacturing precisionVSProductivity

Solution Approach 1:

The fermentation process performs preliminary action by producing key molecular fragments before the chemical conversion stage. This preliminary biological synthesis reduces the burden on subsequent chemical steps, allowing for better overall control and improved manufacturing efficiency compared to complete chemical synthesis.

Inventive Principle:
Principle #10Preliminary action

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

These methods significantly lower the cost of producing epothilones, making them more viable as therapeutic agents by enhancing the efficiency of their preparation and commercial development.

Implementation Method 1

one or more fragments of the epothilone molecule are obtained through fermentation of organisms

Methodology Applied
Scientific EffectFermentation: Fermentation

Data Source

PatentUS8030503B2Process for the preparation of epothilones
Publication Date: 2011.10.04 KOSAN BIOSCIENCES INC
  • US8030503B2 patent drawing
  • US8030503B2 patent drawing
  • US8030503B2 patent drawing

AI summary

Intermediates in the preparation of epothilones and epothilone analogs are provided along with synthetic methods useful in the synthesis of epothilone compounds.