PROCÉDÉ DE PRÉPARATION DE DÉRIVÉS D'AMINO-BENZOFURANE
    2.
    发明公开
    PROCÉDÉ DE PRÉPARATION DE DÉRIVÉS D'AMINO-BENZOFURANE 审中-公开
    用于生产氨基苯并呋喃衍生物

    公开(公告)号:EP2552900A1

    公开(公告)日:2013-02-06

    申请号:EP11718443.2

    申请日:2011-03-31

    申请人: SANOFI

    摘要: The invention relates to a process for preparing 5-aminobenzofuran derivatives of general formula: Formula (I), in which R
    1 is hydrogen or an alkyl group and R
    2 is an alkyl or dialkylaminoalkyl group. According to the invention, the compounds of formula (I) are prepared by treating a 5‑N‑alkylamidobenzofuran derivative of general formula: in which R
    1 and R
    2 have the same meaning as above and R
    3 is an alkyl group, with a strong acid, so as to form an acid addition salt of the compound of formula (I), which salt is itself treated, if necessary, with a basic agent so as to form this compound of formula (I) in free base form.

    PROCEDE DE PREPARATION DE DERIVES D'AMINO-BENZOYL-BENZOFURANE
    3.
    发明公开
    PROCEDE DE PREPARATION DE DERIVES D'AMINO-BENZOYL-BENZOFURANE 审中-公开
    制备DE衍生物氨基苯甲酰 - 苯并呋喃

    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

    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。