Synthesis of 2-hydrophobic-5-methoxy-diazole [4,5-b]-dipyridine

Abstract

Synthesis of 2-tertiary-5-methyl imidazole(4,5-b)pyridine is carried out by preparing 2-amino-3-nitro-6-clopyridine by 2,6-dichlo-3-nitropyridine, preparing 2-amino-3-nitro-6-methyl pyridine by 2-amino-3-nitro-6-clopyridine, and preparing 2-amino-3-nitro-6-methyl pyridine-2,3-diamino-6-methyl pyridine-MIPT. Its advantages include less reactive volume, shorter reactive time, higher reactive efficiency, lower cost and no environmental pollution.

Description

Technical field: [0001] The invention belongs to a preparation method of a pharmaceutical intermediate, in particular to a synthesis process of an intermediate 2-mercapto-5-methoxyimidazo[4,5-b]pyridine in the production of Tateprazole. Background technique: [0002] 2-Mercapto-5-methoxyimidazo[4,5-b]pyridine (abbreviated as MIPT) is the drug Tenatoprazole (TU-199) Tenatoprazole[CAS: 113712-98-4]) ​​5-Methoxy-2 -{[(4-Methoxy-3,5-Dimethyl-2-pyridinyl)methyl]sulphinyl}-1H-imidazo[4,5-b]pyridine.5-methoxy-2-(4-methoxy- 3,5-lutidine-2-methylsulfinyl)-imidazo(4,5-b)pyridine, the molecular formula is: C16H18N4O3S. ) important intermediates. Tenatoprazole was originally a proton pump inhibitor jointly developed by Tokyo Tanabe, Japan Mitsubishi Pharmaceutical Company, and Japan Hokuriku Pharmaceutical Company, and was authorized to France Negma Company to develop the drug. It submitted a new drug application in Japan in April 1999 and April 2002 Approved for listing. Compared w...

AI Technical Summary

Problems solved by technology

However, there are very few manufacturers of the intermediate MIPT in the production process, almost none in China, and most of them are at the laboratory level in foreign countries, and its process characteristics cannot meet industrial production.

There have been related synthesis reports in Japanese patents, but a large amount of metallic sodium is used in the process, which is not suitable for industrial production