Synthesis method of lercanidipine intermediates

A technology of a dipine intermediate and a synthesis method, which is applied in the field of synthesis of lercanidipine intermediates and can solve the problems of low yield and the like

Active Publication Date: 2013-10-23
CHONGQING SHENGHUAXI PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0020] But this route is long and the yield is relatively low

Method used

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  • Synthesis method of lercanidipine intermediates
  • Synthesis method of lercanidipine intermediates
  • Synthesis method of lercanidipine intermediates

Examples

Experimental program
Comparison scheme
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Embodiment 1

[0035] Embodiment 1: Preparation of compound III by chlorination of compound II

Embodiment 1-1

[0036] Example 1-1 29.6 g (0.2 mol) of compound II was dissolved in 200 mL of chloroform, and the temperature was raised to 50°C. 14.3 mL (0.2 mol) of thionyl chloride was added dropwise and reacted for 5 h. The reaction liquid was concentrated to obtain a yellow oil (compound III), weighing 33.3 g, which was directly used in the next reaction.

Embodiment 1-2

[0037] Example 1-2 29.6 g (0.2 mol) of Compound II was dissolved in 250 mL of dichloromethane and cooled to 0°C. 99.7 mL (1.4 mol) of thionyl chloride was added dropwise and reacted for 20 h. The reaction solution was concentrated to obtain a yellow oil (compound III), weighing 34.3 g, which was directly used in the next reaction.

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PUM

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Abstract

The invention discloses a synthesis method of lercanidipine intermediates. The method comprises the following steps of: taking cinnamic acid as an initial material, obtaining cinnamoyl chloride by chlorination, and then obtaining N-methyl cinnamon amide by amination; further carrying out friedel-crafts alkylation reaction together with benzene to obtain N-methyl-1,1-diphenylacetamide under the effect of a catalyst; and finally obtaining the N-methyl-3,3-diphenyl alanine by carbonyl reduction. The route is cheap and available in material, convenient to react and operate, high in yield, low in cost and suitable for industrial application.

Description

technical field [0001] The invention relates to a synthesis method of a lercanidipine intermediate. Background technique [0002] Lercanidipine is a third-generation dihydropyridine calcium channel blocker developed by Italian company Recordati. Its chemical name is 3,5-pyridinedicarboxylic acid-1,4-di Hydrogen-2,6-dimethyl-4-(3-nitrobenzene) 2-[(3,3-diphenylpropyl)methylamine]-1,1-dimethylmethyl ester hydrochloride, The chemical structure is shown below, [0003] [0004] It was first launched in the Netherlands in 1997 under the product names of Lerdip, zanedip, and Zanidipllo, and then launched in France, Australia, Germany and other countries. In Europe, this product is used for various types of hypertension, and in the UK it is only used for mild and moderate hypertension. The dosage form of this product is tablet, and the recommended dose is 10mg / qd, which is taken orally at least 15 minutes before meals. The product was listed in China by the Italian Recordati ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C211/27C07C209/50
Inventor 王庆何亮
Owner CHONGQING SHENGHUAXI PHARMA CO LTD
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