公开(公告)号：US08884033B2

公开(公告)日：2014-11-11

申请号：US13742816

申请日：2013-01-16

Applicant: Sanofi

Inventor： Xavier Bon ,  Christine Biencourt ,  Corinne Leroy ,  Julia Mateos-Caro ,  Philippe Vayron

IPC: C07D307/00 ,  A61K31/343 ,  C07D307/80

CPC classification number: A61K31/343 ,  C07D307/80

Abstract: The disclosure relates to a process for preparing 5-aminobenzoylbenzofuran derivatives of formula I: in which R1 and R2 are as defined in the disclosure; 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.

Abstract translation: 本公开涉及制备式I的5-氨基苯甲酰基苯并呋喃衍生物的方法：其中R 1和R 2如本公开中所定义; 通过还原式II的5-硝基苯并呋喃衍生物：使用氢转移剂，在钯/炭作为催化剂存在下，在醚或醚混合物中作为溶剂。

公开(公告)号：US08497375B2

公开(公告)日：2013-07-30

申请号：US13709710

申请日：2012-12-10

Applicant: Sanofi

Inventor： Vincent Ferey ,  Julia Mateos-Caro ,  Régis Mondiere ,  Philippe Vayron ,  Sylvie Vigne

IPC: C07F15/00

CPC classification number: C07F17/02

Abstract: 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 an aldehyde-amino ferrocene of formula (III), in which R represents a hydrogen atom or a methyl group, with 7-chloroquinolin-4-amine as shown below, followed by (ii) a stage of reduction of the product of condensation obtained in the preceding stage and (iii) then a stage of hydrolysis of the reaction mixture in the presence of an aqueous solution of ammonia or of citric acid.

Abstract translation: 本发明涉及一种合成式（F）的铁基或其式（Fm）的代谢物的方法：包括还原胺化的反应，所述反应包括：（i）醛 - 氨基二茂铁的缩合阶段 其中R表示氢原子或甲基的式（III）表示如下所示的7-氯喹啉-4-胺，其后是（ii）在前一阶段获得的缩合产物的还原阶段和（ iii）然后在氨水或柠檬酸水溶液存在下水解反应混合物的阶段。