Method for synthesizing nitrofuran metabolite furazolidone AOZ-D4

The invention discloses a furazolidone AOZ-D4 synthesis method, which comprises: 1) carrying out a reaction on deuterated acetic acid and bromine in the presence of TFAA to obtain deuterated bromoacetic acid; 2) carrying out a reaction on the deuterated bromoacetic acid and oxalyl chloride (or SOCl2...

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Hauptverfasser: WANG MIN, CHANG BAIYANG, GONG LAN, WANG TONGTONG, WANG RAN, YANG MENGRUI, ZHOU JIAN
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention discloses a furazolidone AOZ-D4 synthesis method, which comprises: 1) carrying out a reaction on deuterated acetic acid and bromine in the presence of TFAA to obtain deuterated bromoacetic acid; 2) carrying out a reaction on the deuterated bromoacetic acid and oxalyl chloride (or SOCl2) in DMF, adding benzyl alcohol, and continuously carrying out a reaction to obtain deuterated benzyl bromoacetate; 3) adding the deuterated benzyl bromoacetate into the THF solution of NaBD4, and carrying out a reaction to obtain deuterated bromoethanol; 4) dissolving hydrazine hydrate in dehydrated alcohol, adding NaOH, stirring, adding the deuterated bromoethanol, and carrying out a reaction to obtain deuterated 2-hydroxyethyl hydrazine; and 5) carrying out a reaction on the deuterated 2-hydroxyethyl hydrazine and dimethyl carbonate in the presence of an alkali to synthesize furazolidone AOZ-D4. 本发明公开了一种呋喃唑酮AOZ-D4的合成方法。该方法包括下述步骤:1)在TFAA存在下,使氘代乙酸与溴素进行反应,得到氘代溴乙酸;2)使氘代溴乙酸与草酰氯(或SOCl)在DMF中进行反应,然后再加入苄醇继续进行反应,得到氘代溴乙酸苄酯