A kind of tropane type alkaloid and its synthetic method

A synthesis method and compound technology, applied in the fields of drug combination, organic chemistry, cardiovascular system diseases, etc.
CN109422740BActive Publication Date: 2020-04-21SOUTH CENTRAL UNIVERSITY FOR NATIONALITIES
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SOUTH CENTRAL UNIVERSITY FOR NATIONALITIES
Publication Date
2020-04-21

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Abstract

The invention relates to the technical field of chemical synthesis, and a tropane alkaloid and a synthesis method thereof are particularly disclosed. The structure formula (I) of the target product scopolamine alkaloid is described in the description, the compound of formula (I) is a compound containing a five-membered aza-bridged ring skeleton in which that nitrogen atom is protected by 2-pyridinecarboxylic acid; R1 is hydrogen or methoxycarbonyl; R2 is hydrogen or substituted phenyl, and the tropane alkaloid is racemic. Compounds of formula (I) have a significant relaxing effect on KCl-precontracted rat thoracic aorta, suggesting that compounds of formula (I) have a modulatory effect on vascular endothelial cells or smooth muscle cells, and may inhibit the occurrence and development of hypertension.
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Description

technical field

[0001] The invention belongs to the field of chemical synthesis, and specifically relates to a class of tropane-type alkaloids represented by formula (I) containing a five-membered aza bridge ring skeleton and a synthesis method thereof. Background technique

[0002] Tropane-type alkaloids, whose structure contains Tropane (Tropane), that is, a five-membered aza bridge ring. This type of compound has significant biological activity, such as Atropine (Atropine), Scopolamine (Scopolamine), Anisodamine (Anisodamine) etc., are M choline receptor antagonists. It has the effects of inhibiting glandular secretion, dilating pupils, accelerating heart rate, relaxing bronchi and gastrointestinal smooth muscle. It is clinically used to treat peptic ulcer, visceral colic caused by smooth muscle spasm, epilepsy, seasickness, etc.

[0003]

[0004] Tropine-type alkaloids are esters formed from tropine and different organic acids, and tropine can be obtained by reducin...

Claims

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