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Title:
METHOD FOR SYNTHESIZING MEDICAL INTERMEDIATE PHENANTHRENE COMPOUNDS IN SODIUM ACETATE ENVIRONMENT
Document Type and Number:
WIPO Patent Application WO/2016/141824
Kind Code:
A1
Abstract:
The present invention relates to a method for synthesizing medical intermediate phenanthrene compounds, as shown by formula (I) below, in a sodium acetate environment. The method comprises the following steps: reacting a compound as shown by formula (II) and a compound as shown by formula (III) in a solvent under an inert atmosphere in the presence of a catalyst, an organic ligand and sodium acetate, and thereby obtaining the compound of formula (I), wherein R1 and R2 are each independently H, C1-C6 alkyl, C1-C6 alkyloxy or halogen; and R3 is C6-C10 aryl or C5-C8 heteroaryl, wherein the C6-C10 aryl or C5-C8 heteroaryl is optionally substituted by 1-3 substituents, the substituents being C1-C6 alkyl or halogen. The method achieves good effects due to the selection of a suitable catalyst, organic ligand, base and solvent, and has wide industrial application prospects.

Inventors:
ZHAI XUEYAN (CN)
Application Number:
PCT/CN2016/075401
Publication Date:
September 15, 2016
Filing Date:
March 03, 2016
Export Citation:
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Assignee:
JIN YINGHUA (CN)
International Classes:
C07B37/10; C07C2/42; C07C17/275; C07C15/30; C07C25/22; C07D213/127; C07D213/16
Foreign References:
CN104692986A2015-06-10
CN102827077A2012-12-19
Other References:
KIM, K.H. ET AL.: "2,3-Dichloro-5,6-dicyano-para-benzoquinone (DDQ)/Methane sulfonic Acid (MsOH)-Mediated Intramolecular Arene-Alkene Oxidative Coupling", ADVANCED SYNTHESIS & CATALYSIS, vol. 356, no. 4, 20 February 2014 (2014-02-20), XP055308696, ISSN: 1615-4169
YAO, Q.W. ET AL.: "Ligand-Free Heck Reaction: Pd (OAc) 2 as an Active Catalyst Revisited", THE JOURNAL OF ORGANIC CHEMISTRY, vol. 68, no. 19, 16 August 2003 (2003-08-16), XP001170659, ISSN: 0022-3263
SHIMIZU, M. ET AL.: "Palladium-catalyzed Double Cross-coupling Reaction of 1,2-Bis(pinacolatoboryl)alkenes and -Arens with 2,2'-Dibromobiaryls:Annulative Approach to Functionalized Polycyclic Aromatic Hydrocarbons", TETRAHEDRON, vol. 67, no. 41, 12 August 2011 (2011-08-12), pages 8014 - 8026, XP028288356, ISSN: 0040-4020, DOI: doi:10.1016/j.tet.2011.08.019
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