44 results about "Addition elimination" patented technology

The present invention relates to a new synthetic method of nafamostat mesylate intermediate - 6-amidino-2-naphthol mesylate. The new method uses 6-hydroxyl-2-naphthaldehyde as a raw material, and uses dimethyl sulfoxide as a reaction solvent to react with hydroxylamine hydrochloride for addition and elimination to obtain 6-cyano-2-naphthol, 6-cyano-2-naphthol A pinner reaction occurs in HCl / methanol solution to obtain 6-hydroxyl-2-naphthiminomethyl ester hydrochloride, and then feed ammonia to carry out ammonolysis reaction to obtain 6-amidino-2-naphthol, 6-amidino ‑2‑naphthol is successively reacted with sodium bicarbonate and methanesulfonic acid to be converted into 6‑amidino‑2‑naphthol mesylate. In the new synthetic method, the preparation of the first step 6-cyano-2-naphthol adopts a brand-new method, which avoids the use of highly toxic copper cyanide in the traditional method, and is simple to operate and mild in condition; the second step adopts an improved The pinner method uses the reaction of acetyl chloride and methanol to generate HCl instead of directly passing HCl gas into the reaction system. The improved method is more operable and easier to realize industrialization.

An isolongifolenone oxime ether derivative is prepared by the following steps of: taking isolongifolenone as the raw material, synthesizing isolongifolenone oxime through addition-elimination reaction, and performing alkylation reaction of the isolongifolenone oxime. Simultaneously, the isolongifolenone oxime ether derivative disclosed by the invention can inhibit bacteria, such as staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, bacillus proteus vulgaris and pseudomonas aeruginosa, and fungus, such as Aspergillus niger, exserohilum turcicum, corn sheath blight, alternaria musae Bovr.et Bat. and colletotrichum musae; and the isolongifolenone oxime ether derivative has the excellent insecticidal action for insect pests, such as aphid and rice planthopper.

A method of preparing (S)-2-amino-5-methoxytetralin hydrochloride[(S)-2-amino-5-methoxyl-1,2,3,4-tetrahydronaphthalene hydrochloride], comprising the steps of: (1) producing a compound (I) by addition-elimination reaction of 5-methoxy-2-tetralone and R-(+)-a-phenylethylamine; (2) producing a compound (II) by reduction reaction of the compound (I) with a reducing agent; and (3) producing a compound (II) hydrochloride by reacting the compound (II) with a salt-forming agent, then carrying out reduction reaction with a palladium-carbon catalyst to produce (S)-2-amino-5-methoxytetralin hydrochloride. The method can significantly increase the yield of (S)-2-amino-5-methoxytetralin hydrochloride with short synthetic path, low preparation cost and less pollution, which is environmentally friendly and is suitable for medical industrialized production. The structural formulae of the compound (I) and the compound (II) are:respectively.