发明名称 |
Fremgangsmåde til fremstilling af halogenerede alpha-aminoketoner og alpha-aminoalkoholer |
摘要 |
<p>Prodn. of halogenated alpha -amino ketones or alcohols of formula (I) comprises: (a) reacting an amino acid ester of formula (II) with a lower alkyl-lithium cpd. and a silyl chloride of formula ClSiR4R5R6 (IV) to form a silyl protected deriv. of formula (III); (b) reacting (III) with a dihalomethane and a lower alkyl-lithium to give a ketone of formula (I; Q = CO); and opt. (c) reducing the ketone to an alcohol of formula (I; Q = CHOH): X = halogen; Q = CO or CHOH; R1 = amino protecting gp.; R2 = H or an amino acid side chain; R3 = lower alkyl; R4-R6 = lower alkyl or phenyl.</p> |
申请公布号 |
DK0703209(T3) |
申请公布日期 |
2001.04.23 |
申请号 |
DK19950114167T |
申请日期 |
1995.09.09 |
申请人 |
F. HOFFMANN-LA ROCHE AG |
发明人 |
HILPERT, HANS |
分类号 |
C07B61/00;C07C269/06;C07C271/16;C07C271/18;C07C319/20;C07C323/43;(IPC1-7):C07C21/00;C07F7/10;C07C213/00;C07B51/00;C07C221/00 |
主分类号 |
C07B61/00 |
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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