A method of preparing relugolix

By improving the synthetic route of regrugoli and employing steps such as inorganic base hydrolysis, amide condensation, and inorganic base cyclization, the problems of environmental pollution and high cost in existing technologies have been solved, and industrial production with high purity and high yield has been achieved.

CN122103163APending Publication Date: 2026-05-29SHANDONG ACADEMY OF PHARMACEUTICAL SCIENCES
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Patent Information

Application Number
CN202610126487.0
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2026-01-29
Publication Date
2026-05-29

AI Technical Summary

Technical Problem

Existing routes for synthesizing rilugoli suffer from serious environmental pollution, high production costs, and difficulty in removing impurities.

Method used

Relugoline was prepared from ethyl 2-[(2,6-difluorobenzyl)-propoxyamido]-4-(dimethylamino)methyl-5-(4-nitrophenyl)thiophene-3-carboxylate via inorganic base hydrolysis, amide condensation, inorganic base cyclization, 10% Pd/C catalytic hydrogenation, and finally condensation with methoxyaminophenyl carbonate amide phrase ester amide. The reaction route is shown in Figure 4.

Benefits of technology

It reduces production costs, minimizes the waste of organic solvents, simplifies operating procedures, and improves product purity and yield, making it suitable for industrial production.

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Abstract

The application discloses a preparation method of relugolix and belongs to the field of drug synthesis. The method uses 2-[(2,6-difluorobenzyl) n-propoxy amido]-4-(dimethylamino) methyl-5-(4-nitrophenyl) thiophene-3-carboxylic acid ethyl ester (formula II) as a starting material, and relugolix is prepared through the following steps: inorganic base hydrolysis, amide condensation, inorganic base cyclization, 10% Pd / C catalytic hydrogenation, and finally amide condensation with methoxyamino carbonic acid phenyl ester. The starting material used in the preparation method is cheap and easy to obtain, the reaction is mild, the operation is simple, the product has high purity and high yield, no biuret by-product is detected, and the method is suitable for industrial production.
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