Title:
METHOD FOR APPLYING PALLADIUM CHLORIDE TO SYNTHESISE PHARMACEUTICAL INTERMEDIATE PHENANTHRENE COMPOUND
Document Type and Number:
WIPO Patent Application WO/2016/141830
Kind Code:
A1
Abstract:
The present invention relates to a method for applying palladium chloride to synthesise a phenanthrene compound as shown in formula (I), the method comprising: reacting the compound of formula (II) with the compound of formula (III) in an inert atmosphere, in the presence of a palladium chloride-containing catalyst, organic ligands and a base, and in a solvent, thereby obtaining the compound of formula (I), wherein R1 and R2 are each independently H, a C1-C6 alkyl group, a C1-C6 alkoxy group or a halogen, R3 is a C6-C10 aryl group or a C5-C8 heteroaryl group, the C6-C10 aryl group or the C5-C8 heteroaryl group being optionally substituted by 1-3 substituents, the substituents being C1-C6 alkyl groups or halogens. The method obtains a good effect via the selection of an appropriate catalyst, organic ligands, base and solvent, and has wide prospects for industrial application.
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Inventors:
ZHAI XUEYAN (CN)
Application Number:
PCT/CN2016/075415
Publication Date:
September 15, 2016
Filing Date:
March 03, 2016
Export Citation:
Assignee:
ZHU XIAOTAO (CN)
International Classes:
C07B37/10; C07C2/42; C07C17/275; C07C15/30; C07C25/22; C07D213/127; C07D213/16
Foreign References:
| CN104692986A | 2015-06-10 | |||
| CN102827077A | 2012-12-19 |
Other References:
YAO, Q.W. ET AL.: "Ligand-Free Heck Reaction: Pd(Oac)2 As An Active Catalyst Revisited", JOURNAL OF ORGANIC CHEMISTRY, vol. 68, no. 19, 16 August 2003 (2003-08-16), pages 7529, 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
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
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