发明名称 |
3,5-Disubstituted tetrahydrofuran-2-ones. |
摘要 |
3,5-Di:substd. tetrahydrofuran-2-ones (I) and their salts are new: R1 = opt. esterified COOH; hydroxymethyl; or formyl; R2, R4 = aliphatic, cycloaliphatic-aliphatic, araliphatic or heteroaryl-aliphatic gp.; R3 = N3; or NH2 opt. substd. by an aliphatic or araliphatic gp. and/or by an amino protecting gp. Certain starting materials and intermediates are also claimed. Further claimed is the conversion of (I) into aryl-substd. hydroxylated amino-alkanoic acid amides (II) by: (i) condensing (I) where R1 = CHO (obtd. as required from (I) where R1 = opt. esterified COOH by redn. or from (I) where R1 = CHOH by dehydrogenation) with a Grignard reagent (a); (ii) protecting the OH gp. in the resulting tertiary alcohol (b); (iii) reacting the protected alcohol (c) obtd. with an amine (d); and (iv) catalytically hydrogenating the prod. obtd. Ra = aromatic or heteroaromatic gp.; Rb = aliphatic, cycloaliphatic or heteroaromatic-aliphatic substd. amino; R = protecting gp.; R30 = amino mono- or di-substd. by lower alkyl or mono-substd. by lower alkanoyl; Q = H or OH. |
申请公布号 |
EP0678514(A1) |
申请公布日期 |
1995.10.25 |
申请号 |
EP19950810237 |
申请日期 |
1995.04.07 |
申请人 |
NOVARTIS AG |
发明人 |
GOESCHKE, RICHARD, DR.;HEROLD, PETER, DR.;RIGOLLIER, PASCAL, DR.;MAIBAUM, JUERGEN KLAUS, DR. |
分类号 |
C07C229/36;C07C231/02;C07C237/20;C07C255/13;C07C271/16;C07C271/18;C07C271/22;C07D241/08;C07D263/26;C07D295/13;C07D307/33;C07D413/06 |
主分类号 |
C07C229/36 |
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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