Title:
CHIRAL OR RACEMIC PYRIMIDODIAZEPANONE COMPOUND, AND PREPARATION METHOD THEREFOR AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2022/242558
Kind Code:
A1
Abstract:
The present invention belongs to the technical field of chiral compound synthesis, and specifically relates to a chiral or racemic pyrimidodiazepanone compound, and a preparation method therefor and the use thereof. The chiral or racemic pyrimidodiazepanone compound of the present invention or a pharmaceutically acceptable salt thereof has a structural formula as shown in formula (I). Further provided in the present invention is a preparation method for the pyrimidodiazepanone compound, the method specifically comprising using a pyrimidine-based allyl compound intermediate as a raw material; using an iridium complex generated by the action of an iridium compound and a phosphoramidite ligand as a catalyst; and performing a reaction under the action of a base to obtain the pyrimidodiazepanone compound. The chiral or racemic pyrimidodiazepanone compound of the present invention or the pharmaceutically acceptable salt thereof has a good inhibitory effect on the proteins GR, cofilin-1 and NF-κB, can reverse the apoptosis of PC12 cells caused by corticosterone in a depression state, and can be applied to the preparation of a medicament for preventing or treating depression or a lead compound thereof.
Inventors:
QIU LIQIN (CN)
JIANG XIAODING (CN)
QIAN XU (CN)
JIANG XIAODING (CN)
QIAN XU (CN)
Application Number:
PCT/CN2022/092681
Publication Date:
November 24, 2022
Filing Date:
May 13, 2022
Export Citation:
Assignee:
UNIV SUN YAT SEN (CN)
International Classes:
C07D487/04; A61K31/5513; A61P25/00
Domestic Patent References:
| WO2020089478A1 | 2020-05-07 | |||
| WO2010132015A1 | 2010-11-18 | |||
| WO2003080619A1 | 2003-10-02 | |||
| WO1986001798A1 | 1986-03-27 | |||
| WO2010106249A1 | 2010-09-23 | |||
| WO2005085210A1 | 2005-09-15 |
Foreign References:
| CN108358893A | 2018-08-03 | |||
| CN1656098A | 2005-08-17 |
Other References:
JIANG XIAODING, BENDU PAN, XU QIAN, HAO LIANG, YAQI ZHANG, BIN CHEN, XIAOBO HE, HOI SHAN CHAN, ALBERT S. C. CHAN, LIQIN QIU: "Enantioselective Construction of Pyrimidine-Fused Diazepinone Derivatives Bearing a Tertiary Stereogenic Center Enabled by Iridium-Catalysed Intramolecular Allylic Substitution", ADVANCED SYNTHESIS AND CATALYSIS, vol. 363, no. 13, 21 May 2021 (2021-05-21), pages 3227 - 3232, XP093005709, DOI: 10.1002/adsc.202100444
Attorney, Agent or Firm:
GUANGZHOU JUNCT INTELLECTUAL PROPERTY AGENCY FIRM (GENERAL PARTNERSHIP) (CN)
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