Method for preparing enamine derivates

A technology for derivatives and enamines, applied in the field of preparation of enamine derivatives, can solve the problems of large consumption of triethyl orthoformate and acetic anhydride, unsuitable for large-scale production, trivial preparation of DMFA, etc., and achieves low cost and high reaction efficiency. Mild conditions and high yields
CN101230013BActive Publication Date: 2012-01-25ZHEJIANG GUOBANG PHARMA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
ZHEJIANG GUOBANG PHARMA
Publication Date
2012-01-25

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Abstract

The invention discloses a method for preparing enamine derivatives, which comprises the steps that: 1) the iminium salts with a molecular structural formula as III and the metal salt comprising active methylene with a molecular structural formula as II are selected as raw materials, and the molar ratio of iminium salts to metal salts comprising active methylene ranges from 1 : 1 to 3 : 1 ; 2) under a temperature of -50 DEG C to 100 DEG C, the iminium salts are gradually added into the organic solvent containing the metal salts comprising active methylene, to carry out a react for 0 to 40 hours with heat preservation under minus 50DEG C to 100DEG C; the solution of enamine derivatives with a molecular structural formula as I is obtained. The method for preparing enamine derivatives has simple process with high yield and mild reactive condition.
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Description

technical field

[0001] The invention relates to a preparation method of an enamine derivative (molecular structural formula I), which can be used to synthesize fluoroquinolone drug intermediates (molecular structural formula IV) and other compounds. Background technique

[0002] Fluoroquinolones are widely used as antibiotics, and the synthetic methods of their key intermediates (IV) have multiple reports. Taking the synthesis of the main ring compound of ciprofloxacin-cyclopropanecarboxylic acid (molecular structural formula is A) as an example, the synthetic method of the key intermediate (IV) is introduced.

[0003]

[0004] Molecular structure IV: R 1 is a substituent with electron-withdrawing effect; R 4 Any one of C1~C6 alkyl; X 1 、X 2 、X 3 and x 4 Both are halogen, hydrogen, amino or nitro; X 5 for halogen.

[0005] The synthetic routes suitable for industrialized production are mainly divided into two categories according to different starting materials: o...

Claims

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