公开(公告)号：WO2003097606A1

公开(公告)日：2003-11-27

申请号：PCT/IB2000/001057

申请日：2000-07-28

Applicant: HERBEX, PRODUTOS QUÍMICOS, SA ,  SARAGGA, José, Manuel ,  CORREIA, Pedro, Brito ,  ROMÃO, Carlos, Crispim ,  CORREIA, Luís, Brito ,  PEREIRA, Maria, Florbela ,  FERNANDES, Ana, Cristina ,  BORGES, José, Enrique ,  TAVARES, Regina ,  COSTA, Maria do Céu ,  TEIXEIRA, Fátima

Inventor： CORREIA, Pedro, Brito ,  ROMÃO, Carlos, Crispim ,  CORREIA, Luís, Brito ,  PEREIRA, Maria, Florbela ,  FERNANDES, Ana, Cristina ,  BORGES, José, Enrique ,  TAVARES, Regina ,  COSTA, Maria do Céu ,  TEIXEIRA, Fátima

IPC: C07D213/89

CPC classification number: C07D213/89 ,  C07D213/61 ,  C07D213/65 ,  C07D401/12

Abstract: The present invention describes a new process for the preparation of omeprazole, lansoprazole and pantoprazole of formula (XXI), (XXXIII), and which involves the formation of pyridines N-oxide using a rhenium compound as a catralyst, followed by nitration of the 4-position with nitric acid fuming in presence of a claycop. The chlorination of the 2-methyl group of pyridine was achieved by using the POCI 3 /Et 3 N, which allowed the preparation of the derivates 2-chloromethylpyridines in only one step. These derivates reacted with the mercaptobenzimidazolic derivatives in presence of ultra-sonic radiation, giving the thioethers. The oxidation of these thioethers was done with several oxidizing agents and the required anti-ulcer compounds were obtained after the substitution of nitro group by the corresponding OR groups.

Abstract translation: 本发明描述了制备式（XXI），（XXXIII）的奥美拉唑，兰索拉唑和泮托拉唑的新方法，其涉及使用铼化合物作为催化剂形成吡啶N-氧化物，然后硝化4 - 在硝酸存在下，用硝酸发烟。 通过使用POCI> 3 <3> N来实现吡啶的2-甲基的氯化，其允许仅在一个步骤中制备衍生物2-氯甲基吡啶。 这些衍生物在超声辐射存在下与巯基苯并咪唑衍生物反应，得到硫醚。 这些硫醚的氧化用几种氧化剂进行，并且在用相应的OR基团取代硝基之后获得所需的抗溃疡化合物。