Lappaconitine aza-cinnamic acid derivatives with anti-tumor activities and a method of preparing the same

US10100036B2 · US · B2

Patent metadata
FieldValue
Publication numberUS-10100036-B2
Application numberUS-201715713934-A
CountryUS
Kind codeB2
Filing dateSep 25, 2017
Priority dateSep 30, 2016
Publication dateOct 16, 2018
Grant dateOct 16, 2018

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  1. Title

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  2. Abstract

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  5. First independent claim

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Abstract

Official abstract text for this publication.

A lappaconitine aza-cinnamic acid derivative having the following formula (I): X is C or N, and R 1 , R 2 , and R 3 are independently H or lower alkyl. A method of preparing the lappaconitine aza-cinnamic acid derivative of formula (I) is also disclosed.

First claim

Opening claim text (preview).

What is claimed is: 1. A lappaconitine aza-cinnamic acid derivative selected from the group consisting of 2. A method of preparing lappaconitine Aza-cinnamic acid derivatives with antitumor activities comprising: reacting a compound of formula (II): with HCl to obtain a compound of formula (III): and reacting the compound of formula (III) with a compound of formula (IV): to obtain a lappaconitine aza-cinnamic acid derivative having the following formula (I): wherein X is C or N, and R 1 , R 2 , and R 3 are independently H or lower alkyl. 3. The method of claim 2 , wherein the compound of formula (II) reacts with 2% HCl in ethanol in a molar ratio of 1:5. 4. The method of claim 2 , wherein the compound of formula (III) reacts with the compound of formula (IV) in DMF in a molar ratio of 1:1.1-12 with DCC as a catalyst. 5. The method of claim 4 , wherein the compound of formula (III) reacts with the compound of formula (IV) at 50° C.-90° C. 6. The method of claim 4 , wherein the compound of formula (III) reacts with the compound of formula (IV) at 60° C.-80° C.

Assignees

Inventors

Classifications

  • C07D401/12Primary

    linked by a chain containing hetero atoms as chain links · CPC title

  • Antineoplastic agents · CPC title

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What does patent US10100036B2 cover?
A lappaconitine aza-cinnamic acid derivative having the following formula (I): X is C or N, and R 1 , R 2 , and R 3 are independently H or lower alkyl. A method of preparing the lappaconitine aza-cinnamic acid derivative of formula (I) is also disclosed.
Who is the assignee on this patent?
Liang Chengyuan, Jia Minyi, Ju Xingke, and 4 more
What technology area does this patent fall under?
Primary CPC classification C07D401/12. Mapped technology areas include Chemistry & Metallurgy.
When was this patent published?
Publication date Tue Oct 16 2018 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
What related patents are in patentsdb?
We list 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).