Title:
PROCESS FOR PREPARING INTERMEDIATE OF ANTI-TUMOR DRUG NIRAPARIB AND INTERMEDIATE THEREOF
Document Type and Number:
WIPO Patent Application WO/2019/072237
Kind Code:
A1
Abstract:
Disclosed is a process for preparing an intermediate of anti-tumor drug niraparib and an intermediate thereof. The present invention discloses a process for preparing compound (f), which comprises conducting a cyclization reaction of compound (e) in a solvent and in the presence of a base to give compound (f). The process of the present invention does not involve the steps of catalytic reduction or catalytic coupling reaction of precious metals and chiral separation, which has advantages such as low equipment requirements, simple operation, favorable industrial production, avoiding waste liquid containing heavy metals and phosphorus, low cost and high product ee value.
Inventors:
WANG TIANHAO (CN)
Application Number:
PCT/CN2018/110025
Publication Date:
April 18, 2019
Filing Date:
October 12, 2018
Export Citation:
Assignee:
ZAI LAB SHANGHAI CO LTD (CN)
International Classes:
C07D211/76; A61K31/16; A61K31/416; C07B57/00; C07D211/02
Foreign References:
| CN106854176A | 2017-06-16 | |||
| CN106432056A | 2017-02-22 | |||
| CN201710953949A | 2017-10-13 | |||
| CN106432056A | 2017-02-22 | |||
| CN106432057A | 2017-02-22 | |||
| CN106883166A | 2017-06-23 | |||
| CN106749181A | 2017-05-31 | |||
| CN106749180A | 2017-05-31 | |||
| CN106432058A | 2017-02-22 |
Other References:
MERCEDES AMAT ET AL.: "Dynamic Kinetic Resolution of Racemic 7-Aryl-b-oxoesters. Enantioselective Synthesis of 3-Arylpiperidines", J. ORG. CHEM., 26 June 2002 (2002-06-26), pages 5343 - 5351, XP055592156
ORGANIC PROCESS RESEARCH & DEVELOPMENT, vol. 15, 2011, pages 831 - 840
ORGANIC PROCESS RESEARCH & DEVELOPMENT, vol. 18, 2014, pages 215 - 227
PHILIPP SCHAFER ET AL.: "Asymmetric Suzuki-Miyaura coupling of heterocycles via Rhodium-catalysed allylic arylation of racemates", NATURE COMMUNICATIONS, vol. 8, no. 1, pages 2017, XP055708848, DOI: 10.1038/ncomms15762
CHEOL K. CHUNG ET AL.: "Process Development of C-N Cross-Coupling and Enantioselective Biocatalytic Reactions for the Asymmetric Synthesis of Niraparib", ORGANIC PROCESS RESEARCH AND DEVELOPMENT, vol. 18, no. 1, 2014, pages 215 - 227, XP055263728, DOI: 10.1021/op400233z
JOURNAL OF ORGANIC CHEMISTRY, vol. 77, no. 16, 2012, pages 7028 - 7045
See also references of EP 3694836A4
ORGANIC PROCESS RESEARCH & DEVELOPMENT, vol. 15, 2011, pages 831 - 840
ORGANIC PROCESS RESEARCH & DEVELOPMENT, vol. 18, 2014, pages 215 - 227
PHILIPP SCHAFER ET AL.: "Asymmetric Suzuki-Miyaura coupling of heterocycles via Rhodium-catalysed allylic arylation of racemates", NATURE COMMUNICATIONS, vol. 8, no. 1, pages 2017, XP055708848, DOI: 10.1038/ncomms15762
CHEOL K. CHUNG ET AL.: "Process Development of C-N Cross-Coupling and Enantioselective Biocatalytic Reactions for the Asymmetric Synthesis of Niraparib", ORGANIC PROCESS RESEARCH AND DEVELOPMENT, vol. 18, no. 1, 2014, pages 215 - 227, XP055263728, DOI: 10.1021/op400233z
JOURNAL OF ORGANIC CHEMISTRY, vol. 77, no. 16, 2012, pages 7028 - 7045
See also references of EP 3694836A4
Attorney, Agent or Firm:
SHANGHAI BESHINING LAW OFFICE (CN)
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