- Preparation method of posaconazole intermediate
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The invention discloses a preparation method of a posaconazole intermediate shown as a formula I. According to the method, p-brominated nitrobenzene and anhydrous piperazine are used as raw materials, and a target product is prepared through a condensation reaction, a reduction reaction, a monoacylation reaction, a cyclization reaction and a diazotization hydrolysis reaction. Compared with a synthesis method taking 1-(4-aminophenyl)-4-(4-hydroxyphenyl)piperazine as a starting material in the prior art, the preparation method provided by the invention has the advantages that the raw materials are easy to obtain, the reaction efficiency is high, the reaction conditions are mild, the yield of a target product is high, the operation is simple and convenient, the efficiency is high, and the cost is low.
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- 1,4-Diarylpiperazines and analogs as anti-tubercular agents: Synthesis and biological evaluation
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Despite progress in modern chemotherapy to combat tuberculosis, the causative pathogen Mycobacterium tuberculosis (M.tb.) is far from eradicated. Bacillary resistance to anti-mycobacterial agents, bacillary persistence and human immunodeficiency virus (HIV) co-infection hamper current drug treatment to completely cure the infection, generating a constant demand for novel drug candidates to tackle these problems. A small library of novel heterocyclic compounds was screened in a rapid luminometric in vitro assay against the laboratory M.tb. strain H37Rv. A group of amidines was found to have the highest potency and was further evaluated for acute toxicity against C3A hepatocytes. Next, the most promising compounds were evaluated for activity against a multi-drug resistant clinical isolate. The group of amidines was also tested for their ability to kill intracellular M.tb. residing in mouse J774A.1 macrophages. Finally, we report on a correlation between the structural differences of the compounds and their anti-mycobacterial activity.
- Forge,Cappoen,Laurent,Stanicki,Mayence,Huang,Verschaeve,Huygen,Vanden Eynde
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scheme or table
p. 95 - 101
(2012/04/10)
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