发明名称 |
PROCESS FOR THE PREPARATION OF (R)-2-BROMO-3-PHENYL-PROPIONIC ACID |
摘要 |
Process for the preparation of (R)-2-bromo-3-phenylpropionic acid starting from D-phenylalanine, sodium nitrite and HBr in an aqueous solution, the reaction being carried out in the presence of a bromide salt, at a temperature between -10 and 30 DEG C. The total amount of HBr plus bromide salt lies between 3 and 10 equivalents, calculated relative to the amount of D-phenylalanine, preferably between 4 and 8 equivalents, the amount of bromide salt ranging from 0.5 to 7 equivalents, calculated relative to the amount of D-phenylalanine. The bromide salt is preferably formed in situ from HBr and a base, for instance KOH or NaOH. Preferably, the (R)-2-bromo-3-phenylpropionic acid obtained is subsequently converted into (S)-2-acetylthio-3-phenylpropionic acid using thioacetic acid and an organic base, for instance thriethylamine. The (S)-2-acetylthio-3-phenylpropionic acid obtained can be converted into a pharmaceutical, in particular an ACE inhibitor, for instance Omapatrilat. |
申请公布号 |
WO0158837(A2) |
申请公布日期 |
2001.08.16 |
申请号 |
WO2001NL00079 |
申请日期 |
2001.02.02 |
申请人 |
DSM N.V.;LOMMEN, FRANCISCUS, ALPHONS, MARIE;KOLLER, HELMUT;SCHERUBL, HERBERT |
发明人 |
LOMMEN, FRANCISCUS, ALPHONS, MARIE;KOLLER, HELMUT;SCHERUBL, HERBERT |
分类号 |
C07B53/00;C07B61/00;C07C51/363;C07C57/58;C07C319/14;C07C321/16;C07C327/32;C07D513/04 |
主分类号 |
C07B53/00 |
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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