1‑n‑substituted benzyl‑6‑n'‑substituent‑2,3,6,9‑tetrahydro‑1h‑[1,4]oxazino[3,2‑g]quinolin‑9‑one ‑8‑Formic acid compound and its preparation method and application

A technology of compounds and substituents, applied in the field of HIV-1 integrase inhibitors, can solve the problems of toxic side effects and limit the application of HAART, and achieve the effect of simple steps and mild reaction conditions
CN104693216BInactive Publication Date: 2017-02-22BEIJING UNIV OF TECH
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
BEIJING UNIV OF TECH
Publication Date
2017-02-22
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention belongs to the technical field of medicine compounds, and discloses a 1-N-substituted benzyl-6-N'-substituent-2,3,6,9-tetralin-1H-[1,4] benzoxazine [3,2-g] quinolone-9-ketone-8-formic acid compound and a preparation method and application thereof. According to the formula (I) of the 1-N-substituted benzyl-6-N'-substituent-2,3,6,9-tetralin-1H-[1,4] benzoxazine [3,2-g] quinolone-9-ketone-8-formic acid compound, R1 represents a benzyl or a substituted benzyl, and R2 represents hydrogen or an alkyl or a hydroxyalkyl or a substituted benzyl or a carboxyalkyl. The method comprises the steps that firstly, 2-amino-5-nitrophenol is used as a raw material, acetylation protection, affinity substitute ring closure and deprotection are performed, affinity substitute is introduced into substituted benzyl, nitro reduction is performed through stannous chloride, condensation is performed, Gould-Jacobs reaction ring closure is performed, affinity substitute is introduced into different substituent groups, and finally hydrolysis is performed to obtain the compound of the formula (I). The compound has the inhibiting effect on the HIV-1 integrase.
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Description

technical field

[0001] The present invention relates to 1-N-substituted benzyl-6-N'-substituent-2,3,6,9-tetrahydro-1H-[1,4]oxazino[3,2-g]quinoline- The 9-keto-8-formic acid compound, its preparation method and its application as an HIV-1 integrase inhibitor belong to the technical field of pharmaceutical compounds. Background technique

[0002] HIV-1 (human immunodeficiency virus-type I), which belongs to the retroviruses, is the virus that causes AIDS. The HIV-1 virus cell invasion of host cells can be roughly divided into the following four stages: In the first stage, the gp120 protein on the outer membrane of HIV-1 specifically recognizes the CD4 molecule on the T cell membrane and binds to it with high affinity, thereby making Target cells are in intimate contact with viral particles. Then gp41 mediates the fusion between the HIV-1 outer lipid membrane and the target cell, and releases the viral core particle into the cytoplasm of the target cell. In the second stage,...

Claims

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