发明名称 |
L-alanyl-L-proline derivs. prepn. - by reacting deriv. of proline and ethyoxy-carbonyl phenyl-proyl-L alanine |
摘要 |
<p>Prodn. of L-alanyl-L-proline derivs. of formula (I), where R is ethyl or hydrogen, or their pharmaceutically acceptable salts, involves reacting derivs. of proline and N(1(S)-ethoxycarbonyl- 3-phenylpropyl)- L-alanine in solvent at (-5) to (20) deg.C. The proline deriv. comprises N-O-bis-trimethylsilyl- L-proline of formula (II). The deriv. of N(1(S)-ethoxycarbonyl- 3-phenyl-propyl)- L-alamine has formula (III), where Het is imidazolyl-1 or benzothiazolyl-2-thio. The condensn. reaction is carried out in non-polar organic solvent, esp. in dioxane, tetrahydrofuran or methylene chloride. When required, the obtd. cpd. of formula (I) in which R is ethyl is hydrolysed to obtain a cpd. of formula (I) in which R is hydrogen. Yield is 76%; m.pt. is 146-152 deg.C. When the maleate is required, a cpd. of formula (I) in which R is ethyl is treated with maleic acid. Yield is 83% and m.pt. is 143-147 deg.C.</p> |
申请公布号 |
ES2015723(A6) |
申请公布日期 |
1990.09.01 |
申请号 |
ES19890002425 |
申请日期 |
1989.07.10 |
申请人 |
KRKA, TOVARNA ZDRAVIL, N.SOL.O |
发明人 |
MERSLAVIC MARJO;ZUPET PAVEL;FLEGO VESNA;STANOVNIK BRANKO;CIRNSKI JANJA |
分类号 |
A61K31/40;A61K31/401;A61K38/05;A61K38/55;A61P9/00;A61P9/12;C07D207/00;C07D207/16;C07K;C07K1/02;C07K1/113;C07K1/12;C07K5/06;C07K5/062;C07K7/14;C07K14/81;(IPC1-7):C07K5/06 |
主分类号 |
A61K31/40 |
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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