Method for preparing optically pure 3-amino butyl alcohol

An aminobutanol and optical technology, applied in the field of chiral drug preparation, can solve the problems of large loss in the splitting process, inability to scale up production, high price, etc., and achieve the effects of improving optical purity, reducing the difficulty of splitting, and improving yield
CN101417954BActive Publication Date: 2012-05-09雅本(绍兴)药业有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
雅本(绍兴)药业有限公司
Publication Date
2012-05-09

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Abstract

The invention discloses a method for preparing optical pure 3-aminobutanol, which comprises the following steps: acetylacetic ester and chiral phenethylamine react to generate 3-(1'-benzylmethylamine)-2-crotonate enantiomer, namely 3-(1'-benzylmethylamine)-2-crotonate; potassium borohydride triacetate or sodium borohydride triacetate is used to reduce the 3-(1'-benzylmethylamine)-2-crotonate enantiomer into a 3-(1'-benzylmethylamine)-2-butyric ester enantiomer; then chiral pure 3-(1'-benzylmethylamine)-2-butyric ester is obtained through salification and resolution; and the 3-(1'-benzylmethylamine)-2-butyric ester is subject to reducing debenzylation by palladium-carbon to obtain the optical pure 3-aminobutanol. The method has low cost and high product purity, and is suitable for industrialized production.
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Description

technical field

[0001] The present invention relates to the preparation of chiral drugs. In particular, it relates to a preparation method of optically pure 3-aminobutanol as a chiral drug intermediate. Background technique

[0002] Optically active 3-aminobutanol is a key intermediate of many chiral drugs, such as J.O.C., (Journa l of organic chemistry) 42, 1650, 1977 reports that it is an important intermediate of anticancer drugs; Tetrahedron Lett.29, 231 , 1988, reported that it is an important intermediate in the synthesis of penem antibiotics because it can be derivatized to β-lactam. However, due to the direct resolution method used in the preparation process, many difficulties have been brought about, and 3-aminobutanol has high water solubility and is not easy to extract, so it is difficult to synthesize it.

[0003] The synthetic method of this compound mainly contains, one is Russ.J.of Bio.Chem.30,396,2004 report, 3-aminobutanol is obtained by reduction of chira...

Claims

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