发明名称 |
METHOD FOR PRODUCING L-PROLYL-L-M-SARCOLYSYL-L-P-FLUOROPHENYLALANINE AND DERIVATIVES THEREOF |
摘要 |
<p>The invention relates to the production of L-prolyl-L-m-sarcolysyl-L-p-fluorophenylalanine and to the lower alkyl ester and/or acid addition salts thereof. To this end L-p-fluorophenylalanine presenting a protected carboxyl group is reacted with L-m-sarcolysine presenting a protected amino group, preferably during cooling in an anhydrous medium and in the presence of dicyclohexylcarbodiimide. This yields L-m-sarcolysyl-L-p-fluorophenylalanine presenting a protected amino group and a protected carboxyl group. The amino protective group is then split off, resulting in the formation of L-m-sarcolysyl-L-p-fluorophenylalanine presenting a protected carboxyl group. The resulting product is reacted with proline presenting a protected amino group in the presence of dicyclohexylcarbodiimide, so that L-prolyl-L-m-sarcolysyl-L-p-fluorophenylalanine with a protected amino group is obtained. Finally the amino protective group is split off and possibly the lower alkyl ester group split off and/or the resulting compound transformed into an acid addition salt.</p> |
申请公布号 |
EP1129107(A1) |
申请公布日期 |
2001.09.05 |
申请号 |
EP19980952496 |
申请日期 |
1998.11.19 |
申请人 |
PTC PHARMA AG |
发明人 |
MEHLEM, FRANCESCO;DI VITTORIO, PIETRO |
分类号 |
C07K1/10;C07K5/08;C07K5/097;(IPC1-7):C07K5/08 |
主分类号 |
C07K1/10 |
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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