发明名称 |
PROCESS FOR THE PRODUCTION OF [2-(4-FLUORO-BENZYL)-PHENYL]-ACETIC ACID |
摘要 |
The present invention relates to a novel process for the production of [2-(4-fluoro-benzyl)-phenyl]-acetic acid, a compound obtainable from phthalic anhydride. The process comprises the subsequent steps a) through e): a) reacting phthalic anhydride with fluorobenzene or a derivative thereof in appropriate reaction conditions; b) over reducing the product obtained in step a) at the ketone moiety; c) reducing the product obtained in step b) with sodium dihydro-bis (2- 15 methoxyethoxy) aluminate (Red-Al) to the corresponding alcohol ; d) chlorinat ing the alcohol obtained in step c) ; e) inserting CO into the product obtained in step d) through an appropriate Pd-containing catalytic system. In an alternative embodiment, the step e) is replaced by the steps f1) and f2) : f1) reacting the product obtained in step d) with sodium cyanide ; f2) hydro lysing the product obtained in step f1). The present invention provides a process for the production of [2-(4-fluoro-benzyl)- phenyl]-acetic acid which is suitable for industrial scale reactors (e.g. which is cleaner and more efficient). Also, [2-(4-fluoro-benzyl)-phenyl]-acetic acid is obtained as a crystalline material with a purity > 95%. |
申请公布号 |
CA2577305(C) |
申请公布日期 |
2013.12.17 |
申请号 |
CA20052577305 |
申请日期 |
2005.08.26 |
申请人 |
JANSSEN PHARMACEUTICA N.V. |
发明人 |
GUILLAUME, MICHEL JOSEPH MAURICE ANDRE;LANG, YOLANDE LYDIA;ROESSLER, ARMIN;ULMER, LARS;LEURS, STEFAN MARCEL HERMAN;DE SMAELE, DIRK |
分类号 |
C07C51/08;C07C51/10;C07C57/58 |
主分类号 |
C07C51/08 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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