发明名称 |
PROCEDE DE SYNTHESE ASYMETRIQUE DES DERIVES S-ACYLES DE L'ACIDE 2-MERCAPTOMETHYL 3-PHENYL PROPANOIQUE, APPLICATION A LA SYNTHESE DE DERIVES N-(MERCAPTOACYL) AMINO-ACIDES |
摘要 |
A method for the asymmetrical synthesis of S-acylated derivatives of 2-mercaptomethyl 3-phenyl propanoic acid of formula (I) is disclosed. The method comprises the steps of (a) preparing diol (VI) by reducing a malonic ester (V) in the presence of a hydride; (b) preparing respective monoacetates (VII R) or (VII S); (c) oxidising the monoacetates to give acids (IX S) or (IX R); (d) saponifying compounds (IX S) or (IX R) to form hydroxyacids (X S) or (X R); and (e) thioacylating hydroxyacids (X S) or (X R) with a mercaptoacid R1SH (XI) using a Mitsunobu reaction to give the desired acids (I R) or (I S), respectively. The method is useful for synthesising N-(mercaptoacyl) amino acids of formula (II).
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申请公布号 |
FR2744446(A1) |
申请公布日期 |
1997.08.08 |
申请号 |
FR19960001360 |
申请日期 |
1996.02.05 |
申请人 |
SOCIETE CIVILE BIOPROJET |
发明人 |
DANVY DENIS;MONTEIL THIERRY;DUHAMEL PIERRE;DUHAMEL LUCETTE CHAIDRON;LECOMTE JEANNE MARIE ROUSSEAU;SCHWARTZ JEAN CHARLES |
分类号 |
C12P7/62;C07B53/00;C07C29/149;C07C59/48;C07C327/32;(IPC1-7):C07C327/52 |
主分类号 |
C12P7/62 |
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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