公开(公告)号：EP2580224A1

公开(公告)日：2013-04-17

申请号：EP11729738.2

申请日：2011-06-10

申请人： SANOFI

发明人： FEREY, Vincent ,  MATEOS-CARO, Julia ,  MONDIERE, Régis ,  VAYRON, Philippe ,  VIGNE, Sylvie

IPC分类号： C07F17/02

CPC分类号： C07F17/02

摘要： The invention relates to a method of synthesis of ferroquine of formula (F) or of its metabolite of formula (Fm): comprising a reaction of reductive amination, said reaction comprising: (i) a stage of condensation of the aldhehyde-amino ferrocene of formula (1 ), which R represents a hydrogen atom or a methyl group, with the 7-chloroquinolin- amine of formula (2) as shown below, followed by (ii) a stage of reduction of the product of condensation obtained in the preceding stage (iii) then a stage of hydrolysis of the reaction mixture in the presence of an aqueous solution of ammonia or of citric acid.

公开(公告)号：EP2580224B1

公开(公告)日：2014-05-28

申请号：EP11729738.2

申请日：2011-06-10

申请人： SANOFI

发明人： FEREY, Vincent ,  MATEOS-CARO, Julia ,  MONDIERE, Régis ,  VAYRON, Philippe ,  VIGNE, Sylvie

IPC分类号： C07F17/02

CPC分类号： C07F17/02

公开(公告)号：EP2595976A1

公开(公告)日：2013-05-29

申请号：EP11754698.6

申请日：2011-07-18

申请人： SANOFI

发明人： BON, Xavier ,  BIENCOURT, Christine ,  LEROY, Corinne ,  MATEOS-CARO, Julia ,  VAYRON, Philippe

IPC分类号： C07D307/80

CPC分类号： A61K31/343 ,  C07D307/80

摘要： The invention relates to a process for preparing 5-aminobenzoylbenzofuran derivatives of formula (I), in which R
1 represents hydrogen or an alkyl group and R
2 represents hydrogen, an alkyl, alkoxy or dialkylaminoalkoxy group, by reduction of a 5-nitrobenzofuran derivative of formula (II) using a hydrogen transfer agent, in the presence of palladium-on-charcoal as catalyst and in an ether or an ether mixture as solvent.

摘要翻译： 本发明涉及制备式（I）的5-氨基苯甲酰基苯并呋喃衍生物的方法，其中R 1表示氢或烷基，R 2表示氢，烷基，烷氧基或二烷基氨基烷氧基，通过还原5-硝基苯并呋喃衍生物 使用氢转移剂，在作为催化剂的钯 - 炭的存在下和作为溶剂的醚或醚混合物中进行。