公开(公告)号：EP2658839B1

公开(公告)日：2014-10-22

申请号：EP11817220.4

申请日：2011-12-28

Applicant: Procos S.p.A.

Inventor： BAROZZA, Alessandro ,  COLOMBO, Matteo ,  ROLETTO, Jacopo ,  PAISSONI, Paolo

IPC: C07C201/02

CPC classification number: C07C201/02 ,  C07C203/04

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：EP2687521A1

公开(公告)日：2014-01-22

申请号：EP12177209.9

申请日：2012-07-20

Applicant: Procos S.p.A.

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

IPC: C07D317/24

CPC classification number: C07D317/24

Abstract: A process for the preparation of Landiolol 1, ((S)-2,2-dimethyl-1,3-dioxolan-4-yl)methyl 3-(4-((S)-2-hydroxy-3-(2-(morpholine-4-carboxamido) ethylamino)propoxy)phenyl)propanoate) starting from (S)-(2,2-dimethyl-1,3-dioxolan-4-yl)methyl 3-(4-hydroxyphenyl)propanoate, an alkylating agent with epoxide structure, in particular epichlorohydrin, and 2-(morpholine-4-carboxamido)ethanamine in the form of the free base or of a salt thereof.

Said process is carried out without isolating most intermediates, does not require chromatographic purifications and is particularly advantageous in terms of yields and productivity. Furthermore, the resulting Landiolol is particularly pure and can be conveniently transformed into Landiolol hydrochloride with high enantiomeric purity.

Abstract translation: 一种制备兰地洛尔1（（S）-2,2-二甲基-1,3-二氧戊环-4-基）甲基3-（4 - （（S）-2-羟基-3-（2- （吗啉-4-甲酰氨基）乙基氨基）丙氧基）苯基）丙酸乙酯），由（S） - （2,2-二甲基-1,3-二氧戊环-4-基）甲基3-（4-羟基苯基） 具有环氧结构的试剂，特别是表氯醇，和游离碱形式的2-（吗啉-4-甲酰氨基）乙胺或其盐。 所述方法在不分离大多数中间体的情况下进行，不需要色谱纯化，并且在产率和生产率方面是特别有利的。 此外，所得的兰地洛尔是特别纯的，并且可以方便地以高对映体纯度转化为盐酸兰地洛尔。

公开(公告)号：EP2658839A1

公开(公告)日：2013-11-06

申请号：EP11817220.4

申请日：2011-12-28

Applicant: Procos S.p.A.

Inventor： BAROZZA, Alessandro ,  COLOMBO, Matteo ,  ROLETTO, Jacopo ,  PAISSONI, Paolo

IPC: C07C201/02

CPC classification number: C07C201/02 ,  C07C203/04

Abstract: Disclosed is a process for the synthesis of Nicorandil (1), 2-(nicotinamide)ethyl nitrate, starting from N-(2-hydroxyethyl)nicotinamide (15), using nitration with nitric acid in the presence of acetic anhydride Said synthesis method is particularly advantageous because it solves the safety problems involved in the use of nitric acid as nitrating agent, and allows a product with excellent yields and quality to be isolated.

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