公开(公告)号：EP2394994A1

公开(公告)日：2011-12-14

申请号：EP11168652.3

申请日：2011-06-03

Applicant: Procos S.p.A.

Inventor： Garavaglia, Fabio ,  Barozza, Alessandro ,  Roletto, Jacopo ,  Paissoni, Paolo

IPC: C07D213/74 ,  A61K31/44

CPC classification number: C07D213/74

Abstract: A process for the preparation of Dalfampridine (1), 4-aminopyridine, starting from 4-pyridinecarbonitrile using a one-pot procedure.

Said process is carried out with no need for isolating intermediates and is particularly advantageous as far as environment, yields, productivity and purity of the resulting product are concerned, both in the reaction mixture and in the isolated crystal.

Abstract translation: 使用一锅法由4-吡啶甲腈制备Dalfampridine（1），4-氨基吡啶的方法。 所述方法不需要分离中间体，并且在反应混合物和分离的晶体中都涉及所得产物的环境，产率，生产率和纯度方面是特别有利的。

公开(公告)号：EP2703383A1

公开(公告)日：2014-03-05

申请号：EP13179063.6

申请日：2013-08-02

Applicant: Procos S.p.A.

Inventor： Barozza, Alessandro ,  Veronese, Martino ,  Roletto, Jacopo ,  Paissoni, Paolo

IPC: C07C233/18 ,  C07C231/02 ,  C07C231/10 ,  C07C41/26 ,  C07C303/28 ,  C07C213/08

CPC classification number: C07C41/26 ,  C07C213/08 ,  C07C231/02 ,  C07C231/10 ,  C07C233/18 ,  C07C303/28 ,  C07C217/60 ,  C07C309/66 ,  C07C43/23

Abstract: Disclosed is a process for the synthesis of Agomelatine (1), N-(2-(7-methoxynaphthalen-1-yl)ethyl)acetamide from ethyl 2-(7-methoxynaphthalen-1-yl)acetate (4).

Said synthesis method is particularly advantageous compared with known procedures because it uses low-cost reagents under mild reaction conditions and allows the isolation of a product with excellent yields and quality.

Abstract translation: 公开了一种由2-（7-甲氧基萘-1-基）乙酸乙酯（4）合成青霉烯（1），N-（2-（7-甲氧基萘-1-基）乙基）乙酰胺的方法。 所述合成方法与已知方法相比是特别有利的，因为它在温和的反应条件下使用低成本的试剂，并允许以优异的产率和质量分离产物。

公开(公告)号：EP2394994B1

公开(公告)日：2013-02-13

申请号：EP11168652.3

申请日：2011-06-03

Applicant: Procos S.p.A.

Inventor： Garavaglia, Fabio ,  Barozza, Alessandro ,  Roletto, Jacopo ,  Paissoni, Paolo

IPC: C07D213/74 ,  A61K31/44

CPC classification number: C07D213/74