发明名称 |
PROCESSES FOR PRODUCING BETA-HALOGENO-ALPHA-AMINO-CARBOXYLIC ACIDS AND PHENYLCYSTEINE DERIVATIVES AND INTERMEDIATES THEREOF |
摘要 |
<p>Preparation of optically active N-protected S-phenylcysteine (III) using new process for preparing beta -halogeno-alpha -aminocarboxylic acid (I) starting materials. Preparation of beta -halogeno-alpha -aminocarboxylic acid (I) comprises treating a beta -hydroxyaminocarboxylic acid (IV) or its salt with a halogenating agent and an acid to halogenate the hydroxy group. In (IV) the basicity of the amino group at the alpha -position is not shielded by the presence of the substituent on the amino group. Independent claims are also included for: (1) a process for the preparation of an optically active N-protected S-phenylcysteine of formula (III) or its salt comprising: (A) subjecting optically active serine or its salt to the above process to give a beta -halogenated alanine compound of formula (I'); (B) protecting the amino group of (I') to give a protected compound of formula (II); and (C) reacting (II) with thiophenol under basic conditions (2) intermediates (I') and (II). [Image] R1amino protecting group and R0 = H; or R1+R0amino protecting group.</p> |
申请公布号 |
EP1046634(A1) |
申请公布日期 |
2000.10.25 |
申请号 |
EP19980961624 |
申请日期 |
1998.12.28 |
申请人 |
KANEKA CORPORATION |
发明人 |
YAMASHITA, KOKI;INOUE, KENJI;KINOSHITA, KOICHI;UEDA, YASUYOSHI;MURAO, HIROSHI |
分类号 |
C07C227/16;C07C229/20;C07C319/14;C07C323/58;C07C323/59;(IPC1-7):C07C229/20;C07C227/40;C07B53/00 |
主分类号 |
C07C227/16 |
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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