Title:
NOVEL METHOD FOR PRODUCING RUCAPARIB THAT IS PARP INHIBITOR AND INTERMEDIATE THEREOF
Document Type and Number:
WIPO Patent Application WO/2023/013974
Kind Code:
A1
Abstract:
The present invention relates to a method for producing novel rucaparib which can achieve an excellent synthesis yield and reproducibility. More particularly, the present invention relates to: a novel production method for synthesizing rucaparib by first synthesizing an indole skeleton to which substituents have been introduced to positions 2, 3, 4, and 6, and then performing a heptagonal lactam ring formation reaction between the substituents introduced to positions 3 and 4; and a novel intermediate which can be used in the production thereof.
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Inventors:
CHEON CHEOL-HONG (KR)
PARK JINJAE (KR)
PARK JINJAE (KR)
Application Number:
PCT/KR2022/011115
Publication Date:
February 09, 2023
Filing Date:
July 28, 2022
Export Citation:
Assignee:
UNIV KOREA RES & BUS FOUND (KR)
International Classes:
C07D209/10; A61K31/55; A61P35/00; C07C221/00; C07C225/16; C07C255/30; C07C255/32; C07D487/04
Domestic Patent References:
| WO2019020508A1 | 2019-01-31 |
Foreign References:
| CN108409626A | 2018-08-17 | |||
| US20200331916A1 | 2020-10-22 | |||
| CN109824677A | 2019-05-31 | |||
| KR20070051340A | 2007-05-17 |
Other References:
XIE ZHOULING; ZHOU YOULI; ZHAO WEI; JIAO HE; CHEN YU; YANG YONG; LI ZHIYU: "Identification of novel PARP-1 inhibitors: Drug design, synthesis and biological evaluation", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, ELSEVIER, AMSTERDAM NL, vol. 25, no. 20, 22 August 2015 (2015-08-22), Amsterdam NL , pages 4557 - 4561, XP029285853, ISSN: 0960-894X, DOI: 10.1016/j.bmcl.2015.08.060
PARK JINJAE, CHEON CHEOL-HONG: "Total Synthesis of Rucaparib", THE JOURNAL OF ORGANIC CHEMISTRY, AMERICAN CHEMICAL SOCIETY, vol. 87, no. 7, 1 April 2022 (2022-04-01), pages 4813 - 4817, XP093031455, ISSN: 0022-3263, DOI: 10.1021/acs.joc.2c00083
PARK JINJAE, CHEON CHEOL-HONG: "Total Synthesis of Rucaparib", THE JOURNAL OF ORGANIC CHEMISTRY, AMERICAN CHEMICAL SOCIETY, vol. 87, no. 7, 1 April 2022 (2022-04-01), pages 4813 - 4817, XP093031455, ISSN: 0022-3263, DOI: 10.1021/acs.joc.2c00083
Attorney, Agent or Firm:
PADO IP LAW PLLC (KR)
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