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Synthesis method of timolol maleate intermediates

A technology of timolol maleate and a synthesis method is applied in the synthesis field of synthesizing timolol maleate intermediates, can solve problems such as difficult separation of products, is beneficial to large-scale industrial production, and achieves stable quality of high-quality products , the effect of easy operation

Active Publication Date: 2012-05-30
TIANJIN CENT PHARM CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

And the product is not easy to separate

Method used

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  • Synthesis method of timolol maleate intermediates
  • Synthesis method of timolol maleate intermediates
  • Synthesis method of timolol maleate intermediates

Examples

Experimental program
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Effect test

preparation Embodiment 1

[0029] Put 30g diol amine (0.2mol), 94ml benzaldehyde (3.28 times, 0.91mol), 70ml cyclic compound (dioxane 0.65mol, 1.82 times), put into reaction bottle, reaction temperature 113-115 ℃, reflux After 13 hours, it was evaporated to 130°C under reduced pressure to obtain 47.9 g of oxazole, with a yield of 99.89%.

preparation Embodiment 2

[0031]30g diol amine (0.2mol), 94ml benzaldehyde (3.28 times, 0.91mol), 62ml cyclic compound (toluene, 0.57mol, 1.6 times), put into reaction bottle, reaction temperature 120 ℃, reflux 10 hours, reduce Pressure steamed to 130°C, 48g of oxazole was obtained with a yield of 100.3%.

preparation Embodiment 3

[0033] Put 30g of diolamine (0.2mol), 94ml of benzaldehyde (3.28 times, 0.91mol), 57ml of cyclic compound (1,4-cyclohexadiene, 1.5 times, 0.52mol) into the reaction flask, and the reaction temperature was 125 -130°C, reflux for 8 hours, and evaporate to 130°C under reduced pressure to obtain 48.3 g of oxazole, with a yield of 100.3%.

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Abstract

The invention discloses a synthesis method of timolol maleate intermediates, which takes a cyclic compound as a dissolvent. The synthesis method is characterized in that the cyclic compound is taken as the dissolvent, and amine diol and benzaldehyde generates oxazole product by cyclization; and the timolol maleate intermediate is obtained after distillation, wherein the molar ratio of the cyclic compound as the dissolvent to the amine diol is 1:2-6.5. The invention adopts the cyclic compound as the dissolvent to replace a highly toxic benzene dissolvent so as to obtain high-quality and high-yield timolol maleate intermediates. The synthesis method of the invention has simple operation in industrial production, repeatedly recycled dissolvent, and environment protection, and is more favorable for large-scale industrial production.

Description

Technical field: [0001] The invention belongs to the technical field of organic chemical synthesis and relates to a preparation method of a pharmaceutical intermediate, more specifically a method for synthesizing a timolol maleate intermediate by using a cyclic compound as a solvent. Background technique: [0002] Secondary glaucoma is a combination of some eye diseases and some systemic diseases in the eye, which can be caused by advanced cataract or lens dislocation. With age, the lens expands and increases in size (overmature cataract), pushing the iris forward, blocking the angle of the chamber, and forming crystalline glaucoma. The drug treatment of secondary glaucoma can be divided into topical drug and systemic drug according to different ways of administration. The topical timolol maleate is a non-selective β-adrenergic receptor blocker, which has no obvious endogenous sympathomimetic activity and local anesthetic effect, and has no direct inhibitory effect on the m...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D263/04
Inventor 陈士功徐振艳王学元赵海林李云秋
Owner TIANJIN CENT PHARM CO LTD
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