WO2026123597 - SYNTHESIS METHOD FOR 6-(TERT-BUTOXYCARBONYL)-3,6-DIAZABICYCLO[3.1.1]HEPTANE
National phase entry is expected:
Publication Number
WO/2026/123597
Publication Date
18.06.2026
International Application No.
PCT/CN2025/096419
International Filing Date
22.05.2025
Title **
[English]
SYNTHESIS METHOD FOR 6-(TERT-BUTOXYCARBONYL)-3,6-DIAZABICYCLO[3.1.1]HEPTANE
[French]
PROCÉDÉ DE SYNTHÈSE DE 6-(TERT-BUTOXYCARBONYL)-3,6-DIAZABICYCLO[3.1.1]HEPTANE
[Chinese]
一种6-(叔丁氧羰基)-3,6-二氮杂双环[3.1.1]庚烷的合成方法
Applicants **
SHANGHAI BALMXY PHARMACEUTIC CO., LTD
Inventors
ZHANG, Jihan
WANG, Di
LI, Xiaotao
WU, Tianjun
Priority Data
202411840925.7
13.12.2024
CN
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CNIPA
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Chapter I
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Quotation for National Phase entry
| Country | Stages | Total | |
|---|---|---|---|
| China | Filing, Examination, Granting | 1577 | |
| EPO | Filing, Examination, Granting | 11551 | |
| Japan | Filing, Examination, Granting | 2000 | |
| South Korea | Filing, Examination, Granting | 1802 | |
| USA | Filing, Examination, Granting | 4740 |
Total:
21,670
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Abstract[English]
Provided in the present invention is a synthesis method for 6-(tert-butoxycarbonyl)-3,6-diazabicyclo[3.1.1]heptane. In the present invention, starting from N-benzyl-2,6-piperidinedione, a dibromide 1 is first formed, followed by formation of a bridged-ring intermediate 2 under alkaline conditions; subsequently, an intermediate 3 is obtained by performing debenzylation, and then two carbonyl groups are reduced to form a free amine 4; then, an amino group is subjected to Boc protection to obtain an intermediate 5, and further debenzylation is performed to form the target product. According to the synthesis method of the present invention, few impurities are produced, and the product is easy to purify and has high purity, so that the overall yield is improved, and the unit cost is effectively reduced, facilitating large-scale industrial production.[French]
La présente invention concerne un procédé de synthèse de 6-(tert-butoxycarbonyl)-3,6-diazabicyclo[3.1.1]heptane. Dans la présente invention, à partir de N-benzyl-2,6-pipéridinedione, on forme d’abord un dibromure 1, puis un intermédiaire 2 à cycle ponté est formé dans des conditions alcalines ; ensuite, un intermédiaire 3 est obtenu par débenzylation, puis deux groupes carbonyle sont réduits pour former une amine libre 4 ; ensuite, un groupe amino est soumis à une protection Boc pour obtenir un intermédiaire 5, et une débenzylation supplémentaire est effectuée afin de former le produit cible. Le procédé de synthèse fourni par la présente invention, produit peu d'impuretés, et le produit est facile à purifier et a une pureté élevée, de telle sorte que le rendement global est amélioré, et le coût unitaire est efficacement réduit, ce qui facilite la production industrielle à grande échelle.[Chinese]
本发明提供一种6-(叔丁氧羰基)-3,6-二氮杂双环[3.1.1]庚烷的合成方法，本发明从N-苄基-2,6-哌啶二酮出发，先形成二溴代物1，再在碱性条件下形成桥环中间体2，然后通过脱除苄基得到中间体3，而后还原双羰基形成游离胺4，然后对氨基进行Boc保护得到中间体5，再经脱苄基从而形成目标产物。本发明的合成方法产生的杂质少、产物易于纯化、纯度高，从而使得总收率提高，单位成本得到有效降低，有利于工艺化大规模生产。