Title:
METHOD FOR PREPARING NITROGEN-CONTAINING POLYCYCLIC FUSED RING COMPOUND, AND INTERMEDIATE AND USE OF COMPOUND
Document Type and Number:
WIPO Patent Application WO/2023/280073
Kind Code:
A1
Abstract:
A method for preparing a nitrogen-containing polycyclic fused ring compound, and an intermediate of the compound. By means of the preparation method, a compound of formula I and an intermediate thereof can be synthesized in a high-yield, low-cost and environmentally friendly manner, such that the compound of formula I can be produced on an industrial scale. In the preparation method, column chromatography separation and purification steps such as silica gel column chromatography are not used, and hydrogen is also not used as a hydrogenation or reduction agent, thereby significantly improving the production efficiency and safety. In addition, the preparation method achieves highly efficient utilization of position isomers IIIA and IIIB, and prevents the yield of a target product from being adversely influenced by discarding position isomer IIIA. The total yield of the method, in which the position isomer IIIA is used, can reach 9.4%, and is significantly higher than a yield of less than 4%, which is generated when the position isomer IIIB is used. When the two position isomers are applied to the preparation of compound I at the same time, the yield is increased by 3 times relative to that generated when position isomer IIIB is used alone.
Inventors:
ZHONG JUN (CN)
GAO QIN (CN)
CHEN MINCHUN (CN)
LIU YONGBO (CN)
WANG HAO (CN)
GAO QIN (CN)
CHEN MINCHUN (CN)
LIU YONGBO (CN)
WANG HAO (CN)
Application Number:
PCT/CN2022/103336
Publication Date:
January 12, 2023
Filing Date:
July 01, 2022
Export Citation:
Assignee:
APPLIED PHARMACEUTICAL SCIENCE INC (CN)
International Classes:
C07D471/14; C07D471/04; C07D519/00; C07F5/02
Domestic Patent References:
| WO2021023209A1 | 2021-02-11 | |||
| WO2021023209A1 | 2021-02-11 |
Foreign References:
| CN111465413A | 2020-07-28 | |||
| CN110964008A | 2020-04-07 | |||
| CN112574236A | 2021-03-30 | |||
| CN202110780873A | 2021-07-09 |
Other References:
CELL, vol. 42, no. 2, 1985, pages 581 - 588
MOL CELL ENDOCRINOL, vol. 322, no. 1-2, 2010, pages 2 - 7
J CLIN ONCOL, vol. 30, no. 2, 2012, pages 200 - 202
"RET Solvent Front Mutations Mediate Acquired Resistance to Selective RET Inhibition in RET-Driven Malignancies", JOURNAL OF THORACIC ONCOLOGY, vol. 15, no. 4, 2020, pages 541 - 549
MOL CELL ENDOCRINOL, vol. 322, no. 1-2, 2010, pages 2 - 7
J CLIN ONCOL, vol. 30, no. 2, 2012, pages 200 - 202
"RET Solvent Front Mutations Mediate Acquired Resistance to Selective RET Inhibition in RET-Driven Malignancies", JOURNAL OF THORACIC ONCOLOGY, vol. 15, no. 4, 2020, pages 541 - 549
Attorney, Agent or Firm:
BEIJING ORIGINTELLIGENCE IP LAW FIRM (CN)
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