A kind of synthetic method of 2-thiophene methylamine

Abstract

The invention belongs to the field of organic synthesis and in particular relates to a synthesis method of 2-thienylmethylamine. The synthesis method comprises the following steps: adding 2-thiophenecarboxaldehyde, a solvent, hydroxylamine inorganic acid salt and water into a reactor; stirring and dissolving to sufficiently mix the raw materials; adding acid into the reactor; meanwhile, adding zinc powder in batches; controlling temperature and time to enable the raw materials in a mixed solution in the reactor to sufficiently react; after reacting, dripping ammonia water and a sodium hydroxide water solution respectively; sufficiently stirring and displacing the 2-thiophenecarboxaldehyde; filtering, extracting, decompressing and rectifying to obtain a finished-product of the 2-thiophenecarboxaldehyde. The synthesis method has the advantages that the raw materials are cheap and easy to obtain, the dosage of the zinc powder is less, and the process is simple; the rectified target product 2-thiophenecarboxaldehyde has relatively good quality, and the mol yield (of the 2-thiophenecarboxaldehyde) reaches 61 percent or more.

Description

technical field [0001] The invention belongs to the field of organic synthesis, and in particular relates to a synthesis method of 2-thienylamine. Background technique [0002] 2-Thienylmethylamine, also known as: thiophene-2-methylamine, English name: 2-Thienylmethylamine, CAS NO: [27757-85-3], is an important organic intermediate, which has been used in many fields in recent years. In the field of medicine, it is a key intermediate in the synthesis of the diuretic azosemide and the anti-helminth drug cinnamonium chlorbenzenesulfonate. Some people also apply it to the research of anti-tumor drugs, which can enhance the anti-tumor activity of the drugs. In addition, it is also used in the research of nanomaterials and agrochemical herbicides. There are various synthetic routes of 2-thienylmethylamine: Cui Baojun and others prepared it by Mannich reaction with thiophene, ammonium chloride and formaldehyde aqueous solution (see "Chemistry and Adhesion", Volume 32, Issue 6, 20...

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Problems solved by technology

Li, Yuehui et al. used 2-thiophene carboxamide as raw material, organic boronic acid as catalyst, and phenylsilane as reducing agent, yield: 63% (see Angewandte Chemie, International Edition (2013), 52, (44 ), 11577-11580. ), the advantage of the above-mentioned method is that the yield is high; but the disadvantage is also obvious that the raw materials are not easy to obtain and the reducing agent and catalyst used are more expensive

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