WO2026056878 - PREPARATION METHOD FOR PYRIDAZINONE COMPOUND OF THYROID HORMONE ANALOG AND INTERMEDIATE THEREOF
National phase entry is expected:
Publication Number
WO/2026/056878
Publication Date
19.03.2026
International Application No.
PCT/CN2025/120215
International Filing Date
10.09.2025
Title **
[English]
PREPARATION METHOD FOR PYRIDAZINONE COMPOUND OF THYROID HORMONE ANALOG AND INTERMEDIATE THEREOF
[French]
PROCÉDÉ DE PRÉPARATION D'UN COMPOSÉ DE PYRIDAZINONE D'ANALOGUE D'HORMONE THYROÏDIENNE ET INTERMÉDIAIRE DE CELUI-CI
[Chinese]
一种甲状腺激素类似物的哒嗪酮化合物及其中间体的制备方法
Applicants **
ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD.
SHANGHAI SYNCORES TECHNOLOGIES, INC.
Inventors
MOU, Peng
SUN, Ye
ZHAI, Qisong
Priority Data
202411266158.3
10.09.2024
CN
Application details
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International Searching Authority |
CNIPA
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| Recordal of a Change of the Applicant's Name/Address |
Change of Applicant's Name and Address
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| Type of Assignment |
The Standard Agent's Assignment
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| Applicant's Legal Status |
Legal Entity
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| Entry into National Phase under |
Chapter I
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| Patent Delivery |
Send the Letters Patent by Courier
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| 译文 |
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Quotation for National Phase entry
| Country | Stages | Total | |
|---|---|---|---|
| China | Filing, Examination, Granting | 1779 | |
| EPO | Filing, Examination, Granting | 12570 | |
| Japan | Filing, Examination, Granting | 2215 | |
| South Korea | Filing, Examination, Granting | 2265 | |
| USA | Filing, Examination, Granting | 4740 |
Total:
23,569
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Abstract[English]
The present invention provides a preparation method for Resmetirom and an intermediate I thereof. In the method, by means of a continuous process, there is no need to separate the intermediate and perform post-reaction work-up, thereby saving a plurality of procedures and operation time; and the work-up is simple and efficient, and the use of a highly polluting reagent pyridine is avoided. Moreover, by adjusting a material feeding order, the reaction can be promoted and the color of a product can be effectively improved. The entire process is simple to operate and cost-effective, uses a green and environmentally friendly reagent, and is suitable for large-scale industrial production.[French]
La présente invention concerne un procédé de préparation de resmétirom et d'un intermédiaire I de celui-ci. Le procédé utilise un traitement en continu, sans la nécessité de séparer l'intermédiaire et d'effectuer un traitement post-réaction, ce qui permet d'économiser plusieurs procédures et de réduire le temps de fonctionnement ; le traitement est simple et efficace sans avoir besoin d'utiliser une pyridine réactive hautement polluante. De plus, l'ajustement de l'ordre d'alimentation en matériau permet de favoriser la réaction et d'améliorer de manière efficace la couleur du produit. L'ensemble du procédé est simple à mettre en œuvre et économique, utilise un réactif écologique et respectueux de l'environnement, et est approprié pour une production industrielle à grande échelle.[Chinese]
本发明提供一种瑞司美替罗及其中间体I的制备方法，该方法通过连续工艺，无需分离中间体，也无需反应后处理，节省多个工序及工时，后处理简单有效，并且避免使用高污染试剂吡啶，同时通过调整加料顺序，能促进反应进行且能有效改善产品的颜色，整个工艺操作简便，成本优势，试剂绿色环保，适用于工业化大生产。