Synthetic method of novel ferulic acid derivative

A synthesis method and a technology of derivatives, which are applied in the field of medicine, can solve problems such as inability to solve stability problems, affect the therapeutic effect of products, and attenuate anti-oxidation ability, and achieve strong blood vessel expansion function, strong anti-oxidation ability, and strong anticoagulant effect Effect

Active Publication Date: 2012-12-26
李志强
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  • Abstract
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Problems solved by technology

This not only seriously affects the therapeutic effect of the product, but also produces new impurities, which may cause new adverse reactions
[0007] At present, ferulic acid derivatives, including sodium ferulate, piperazine ferulate, and ethyl ferulate, cannot solve their stability problems. In actual production, transportation, storage, especially in high temperature environments, their antioxidant capacity Decay faster

Method used

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  • Synthetic method of novel ferulic acid derivative
  • Synthetic method of novel ferulic acid derivative
  • Synthetic method of novel ferulic acid derivative

Examples

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Embodiment Construction

[0028] Implementation example one:

[0029] Synthetic method of ethyl acetyl ferulate

[0030] Put 10~20g of ethyl ferulate and 30~100ml of tetrahydrofuran in a reaction vessel, stir, add 8~20g of anhydrous sodium carbonate after completely dissolving, and weigh 5~15g of acetic anhydride in the funnel, add slowly in a normal temperature water bath Acetic anhydride, stirred, heated to 30~55°C and reacted for 0.5~2 hours, added 30~100ml of purified water, stirred, collected the organic layer, filtered the solid with suction and dried to obtain ethyl acetyl ferulate. Its synthetic reaction formula is as follows:

[0031] C 12 h 15 o 4 (Ethyl ferulate) + C 4 h 6 o 3 (Acetic anhydride) → C 2 h 4 o 2 (Acetic acid) +C 14 h 17 o 5 (Ethyl Acetyl Ferulate)

[0032] CH 3 COOH (acetic acid) + Na 2 CO 3 (sodium carbonate) → NaHCO 3 (sodium bicarbonate) + CH 3 COONa (sodium acetate).

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Abstract

The invention discloses a novel ferulic acid derivative, its application and a synthetic method thereof. The novel ferulic acid derivative is a compound as shown in the formula (I), wherein R1 and R2 are respectively C1-10 alkyl. According to the compound as shown in the formula (I), ferulic acid molecule is used as the base. By modification or reconstruction of the side-chain structure of the ferulic acid molecule, stability of ferulic acid is raised, and its pharmacological effects are substantially enhanced.

Description

technical field [0001] The invention belongs to the technical field of medicines and relates to a synthesis method of ferulic acid derivatives. Background technique [0002] The chemical name of Ferulic Acid is 4-hydroxy 3-methoxycinnamic acid (see Figure 1), which is one of the derivatives of cinnamic acid (also known as cinnamic acid, 3-phenyl 2-acrylic acid). Ferulic acid is a non-peptide endothelin receptor antagonist that relaxes vascular smooth muscle, resists platelet aggregation, inhibits platelet 5-hydroxytryptamine release, and inhibits platelet thromboxane A 2 (TXA 2 ), enhance the activity of prostaglandins, analgesia, and relieve vasospasm. It is the basic raw material for the production of medicines for the treatment of cardiovascular and cerebrovascular diseases, kidney diseases and leukopenia. Such as Xinxuekang, Limai Capsules, Taitai Oral Liquid, etc., it can also play a role in bodybuilding and skin protection in the human body. [0003] [0004] Mo...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C69/734C07C67/08A61K31/222A61P9/10A61P3/10A61P13/12
Inventor 唐楷熊传捷
Owner 李志强
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