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Resultant Ruisidilasu from generic delavird and resveratrol, and synthetic method

A technology of delavirdine and resveratrol, applied in the field of chemical pharmacy, can solve problems such as low bioavailability

Inactive Publication Date: 2007-02-21
汪忠辉
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0018] Aiming at the disadvantages of low bioavailability of first-generation antiviral drugs (reverse transcriptase and protease inhibitors), a breakthrough has been made in the research of second-generation antiviral drugs aimed at improving drug bioavailability and increasing blood drug concentration

Method used

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  • Resultant Ruisidilasu from generic delavird and resveratrol, and synthetic method
  • Resultant Ruisidilasu from generic delavird and resveratrol, and synthetic method
  • Resultant Ruisidilasu from generic delavird and resveratrol, and synthetic method

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032]Take resveratrol 5g (0.022mol), NaOH 2.64g (0.066mol), water 80mL, succinic anhydride 2.2g (0.022mol). Stir the reaction at room temperature for 30 minutes, and acidify the reaction solution with 100 mL of dilute hydrochloric acid (1 mol / L). Extracted with ethyl acetate, anhydrous Na 2 SO 4 dry. The crude product was subjected to silica gel column chromatography (developing solvent: ethyl acetate:petroleum ether:acetic acid=1:1:0.01, v:v) to obtain Compound A. Take compound A 1.47g (4.5mmol), DCC 1.42g (6.9mmol), THF 25mL, delavirdine intermediate 1.3g (3.4mmol). The reaction was stirred at room temperature for 5 h, and DCU was removed by filtration. The crude product was subjected to silica gel column chromatography (developing solvent: chloroform:methanol=20:1, v:v) to obtain 1.1g (46%) of the compound risdelasine such as figure 1 shown.

Embodiment 2

[0034] Take delavirdine 1g (2.65mmol), THF 10mL, succinic anhydride 0.265g (2.65mmol). Stir the reaction at room temperature for 30 min, add 200 mL of diethyl ether to precipitate, filter, and dry to obtain 1.15 mg (91%) of Compound B. Take compound B 1.265g (2.65mmol), DCC 0.57g (2.78mmol), THF 10mL, DMAP 0.1g (0.82mmol), resveratrol 0.63g (2.78mmol). The reaction was stirred at room temperature for 5 h, and DCU was removed by filtration. The crude product was subjected to silica gel column chromatography (developing solvent: chloroform:methanol=20:1, v:v) to obtain the compound risdelatin. Such as figure 2 shown.

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Abstract

This invention discloses a method for synthesizing resdelasu from delaviradine intermediate and resveratrol. The method comprises: amidating succinic anhydrate and delaviradine intermediate, and esterifying with resveratrol to obtain resdelasu; or esterifying succinic anhydrate with resveratrol, and amidating with delaviradine intermediate to obtain resdelasu. Resdelasu has the same magnitude order of in vitro bioactivity with anti-HIV drug delaviradine, thus can be used as a new anti-HIV drug.

Description

technical field [0001] The invention belongs to the technical field of chemical pharmacy. Background technique [0002] product name Approval of brand name Types of company name Zidovudine (AZT) Didanosine (ddI) Zalcitabine (ddC) Stavudine (d4T) Lamivudine (3TC) Saquinavir (SQV) Nevirapine (NVP) Ritonavir (ABT-538) Indinavir (IDV) AZT+3TC Delavirdine (DLV) Nelfinavir (NFV) 1987 1991 1992 1994 1995 1995 1996 1996 1996 1997 1997 1997 Retrovir Videx Hivid Zerit Epivir Invirase Viramune Norvir Crixivan Combivir Rescriptor Viracept NRTI NRTI N...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/14C07D209/18
Inventor 王恩思王曦燕方龙贺丽鹏
Owner 汪忠辉
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