发明名称 PROCESS FOR THE PREPARATION OF 4-(FLUOROPHENYL)PIPERIDINE ESTERS
摘要 <p>Firstly a process for the preparation of the (-) trans ester of structure (4), [a valuable intermediate in the preparation of paroxetine] comprising resolution of the corresponding racemic cis ester by the formation of a salt with a chiral acid to give the (+) cis ester, followed by epimerisation of the (+) cis ester with a strong base. Secondly a process for the preparation of a crystalline salt of a racemic trans compound of structure (4) comprising contacting a solution of racemic trans compound of structure (4) with a suitable acidic component, isolating the crystalline product and optionally recrystallising the product. Thirdly a process for the preparation of the (-) trans ester of structure (4) which comprises forming a solution of the product of the process of the second aspect of this invention and a chiral acid, and seeding the solution with a crystalline salt formed from the (-) trans product of the process of the first aspect of this invention and the same chiral acid.</p>
申请公布号 WO2001029002(A1) 申请公布日期 2001.04.26
申请号 GB2000004058 申请日期 2000.10.20
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