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1. WO2016141824 - METHOD FOR SYNTHESIZING MEDICAL INTERMEDIATE PHENANTHRENE COMPOUNDS IN SODIUM ACETATE ENVIRONMENT

Publication Number WO/2016/141824
Publication Date 15.09.2016
International Application No. PCT/CN2016/075401
International Filing Date 03.03.2016
IPC
C07B 37/10 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
37Reactions without formation or introduction of functional groups containing hetero atoms, involving either the formation of a carbon-to-carbon bond between two carbon atoms not directly linked already or the disconnection of two directly linked carbon atoms
10Cyclisation
C07C 17/275 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
17Preparation of halogenated hydrocarbons
26by reactions involving an increase in the number of carbon atoms in the skeleton
272by addition reactions
275of hydrocarbons and halogenated hydrocarbons
C07C 2/42 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
2Preparation of hydrocarbons from hydrocarbons containing a smaller number of carbon atoms
02by addition between unsaturated hydrocarbons
42homo- or co-oligomerisation with ring formation, not being a Diels-Alder conversion
C07C 25/22 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
25Compounds containing at least one halogen atom bound to a six-membered aromatic ring
18Polycyclic aromatic halogenated hydrocarbons
22with condensed rings
C07C 15/30 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
15Cyclic hydrocarbons containing only six-membered aromatic rings as cyclic part
20Polycyclic condensed hydrocarbons
27containing three rings
30Phenanthrenes
C07D 213/127 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06containing only hydrogen and carbon atoms in addition to the ring nitrogen atom
127Preparation from compounds containing pyridine rings
CPC
C07B 37/10
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
37Reactions without formation or introduction of functional groups containing hetero atoms, involving either the formation of a carbon-to-carbon bond between two carbon atoms not directly linked already or the disconnection of two directly linked carbon atoms
10Cyclisation
C07C 15/30
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
15Cyclic hydrocarbons containing only six-membered aromatic rings as cyclic parts
20Polycyclic condensed hydrocarbons
27containing three rings
30Phenanthrenes
C07C 17/275
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
17Preparation of halogenated hydrocarbons
26by reactions involving an increase in the number of carbon atoms in the skeleton
272by addition reactions
275of hydrocarbons and halogenated hydrocarbons
C07C 2/42
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
2Preparation of hydrocarbons from hydrocarbons containing a smaller number of carbon atoms
02by addition between unsaturated hydrocarbons
42homo- or co-oligomerisation with ring formation, not being a Diels-Alder conversion
C07C 25/22
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
25Compounds containing at least one halogen atom bound to a six-membered aromatic ring
18Polycyclic aromatic halogenated hydrocarbons
22with condensed rings
C07D 213/127
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06containing only hydrogen and carbon atoms in addition to the ring nitrogen atom
127Preparation from compounds containing pyridine rings
Applicants
  • 金英花 JIN, Yinghua [CN]/[CN]
Inventors
  • 翟学研 ZHAI, Xueyan
Priority Data
201510100568.506.03.2015CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) METHOD FOR SYNTHESIZING MEDICAL INTERMEDIATE PHENANTHRENE COMPOUNDS IN SODIUM ACETATE ENVIRONMENT
(FR) PROCÉDÉ DE SYNTHÈSE DE COMPOSÉS PHÉNANTHRÈNE, INTERMÉDIAIRES MÉDICAUX, DANS UN ENVIRONNEMENT D'ACÉTATE DE SODIUM
(ZH) 乙酸钠环境下合成医药中间体菲化合物的方法
Abstract
(EN)
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.
(FR)
La présente invention concerne un procédé de synthèse de composés phénanthrène, intermédiaires médicaux, tels que représentés par la formule (I) ci-dessous, dans un environnement d'acétate de sodium. Le procédé comprend les étapes suivantes : la réaction d'un composé tel que représenté par la formule (II) et d'un composé tel que représenté par la formule (III) dans un solvant sous une atmosphère inerte en présence d'un catalyseur, d'un ligand organique et d'acétate de sodium, permettant d'obtenir le composé de formule (I), dans lequel R1 et R2 sont chacun indépendamment H, un groupe alkyle en C1-C6, un groupe alkyloxy en C1-C6 ou un atome d'halogène; et R3 est un groupe aryle en C6-C10 ou un groupe hétéroaryle en C5-C8, le groupe aryle en C6-C10 ou le groupe hétéroaryle en C5-C8 étant éventuellement substitué par 1 à 3 substituants, les substituants étant un groupe alkyle en C1-C6 ou un atome d'halogène. Le procédé permet d'obtenir de bons effets en raison de la sélection d'un catalyseur, d'un ligand organique, d'une base et d'une solvant appropriés, et présente de vastes perspectives d'application industrielle.
(ZH)
本发明涉及一种乙酸钠环境下合成式(I)所示菲化合物的方法,所述方法包括:惰性气氛下,在催化剂、有机配体和乙酸钠存在下,于溶剂中,式(II)化合物与式(III)化合物发生反应,从而得到式(I)化合物;其中,R1、R2各自独立地为H、C1-C6烷基、C1-C6烷氧基或卤素;R3为C6-C10芳基或C5-C8杂芳基,所述C6-C10芳基或C5-C8杂芳基任选被1-3个取代基取代,所述取代基为C1-C6烷基或卤素。所述方法通过合适催化剂、有机配体、碱和溶剂的选择而取得了良好的效果,具备广泛的工业应用前景。
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