WO2026050923 - METHOD FOR SYNTHESIZING KEY INTERMEDIATE OF JAK KINASE INHIBITOR
National phase entry:
Publication Number
WO/2026/050923
Publication Date
12.03.2026
International Application No.
PCT/CN2024/116846
International Filing Date
04.09.2024
Title **
[English]
METHOD FOR SYNTHESIZING KEY INTERMEDIATE OF JAK KINASE INHIBITOR
[French]
PROCÉDÉ DE SYNTHÈSE D'UN INTERMÉDIAIRE CLÉ D'INHIBITEUR DE KINASE JAK
[Chinese]
一种JAK激酶抑制剂关键中间体的合成方法
Applicants **
SHANGHAI ZAIQI BIO-TECH CO., LTD
Inventors
LI, Tao
YANG, Minhui
XIONG, Sheng
HUANG, Chengwei
ZENG, Guohua
XU, Guodong
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International Searching Authority |
CNIPA
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The Standard Agent's Assignment
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Legal Entity
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Chapter I
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Send the Letters Patent by Courier
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Quotation for National Phase entry
| Country | Stages | Total | |
|---|---|---|---|
| China | Filing, Examination, Granting | 1505 | |
| EPO | Filing, Examination, Granting | 11796 | |
| Japan | Filing, Examination, Granting | 1914 | |
| South Korea | Filing, Examination, Granting | 1427 | |
| USA | Filing, Examination, Granting | 4740 |
Total:
21,382
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Abstract[English]
NHCbz to obtain intermediate 2; and finally, performing palladium-on-carbon catalyzed hydrogenation, followed by salt formation with methanesulfonic acid to obtain the product tert-butyl (3aR,5S,6aS)-5-(methylamino)hexahydrocyclopenta[c]pyrrole-2(1H)-carboxylate methanesulfonate. The method reduces raw material costs, has a simple and reliable process with easy industrialization, and provides a new reaction route for the synthesis of tert-butyl (3aR,5S,6aS)-5-(methylamino)hexahydrocyclopenta[c]pyrrole-2(1H)-carboxylate methanesulfonate.[French]
NHCbz pour obtenir un intermédiaire 2 ; et enfin, effectuer une hydrogénation catalysée au palladium sur carbone, suivie d'une formation de sel avec de l'acide méthanesulfonique pour obtenir le produit méthanesulfonate de tert-butyl (3aR,5S,6aS)-5-(méthylamino)hexahydrocyclopenta[c]pyrrole-2(1H)-carboxylate. Le procédé permet de réduire les coûts de matière première, a un procédé simple et fiable avec une industrialisation facile, et fournit une nouvelle voie de réaction pour la synthèse de méthanesulfonate de tert-butyl(3aR,5S,6aS)-5-(méthylamino)hexahydrocyclopenta[c]pyrrole-2(1H)-carboxylate.[Chinese]
NHCbz发生光延反应，得到中间体2；最后钯碳催化氢化，然后甲酸磺酸成盐得到(3aR, 5S,6aS)-5-甲胺基六氢环戊并[c]吡咯-2(1H)-甲酸叔丁酯甲磺酸盐产品。该方法降低了原料成本，工艺简单可靠、易于工业化生产，为(3aR,5S, 6aS)-5-(甲胺基)六氢环戊并[c]吡咯-2(1H)-甲酸叔丁酯甲磺酸盐的合成提供了一条新反应路径。