Process for the manufacture of nicorandil

A technology of nicorandil and nitric acid, applied in the field of preparing nicorandil, can solve problems such as safety hazards, unfavorable economic and industrial safety, large processing volume and the like
CN103370301AActive Publication Date: 2013-10-23PROCOS
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
PROCOS
Publication Date
2013-10-23

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Abstract

Disclosed is a process for the synthesis of Nicorandil (1), 2-(nicotinamide)ethyl nitrate, starting from N-(2-hydroxyethyl)nicotinamide (15), using nitration with nitric acid in the presence of acetic anhydride Said synthesis method is particularly advantageous because it solves the safety problems involved in the use of nitric acid as nitrating agent, and allows a product with excellent yields and quality to be isolated.
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Description

Summary of the invention

[0001] The present invention relates to the method for the synthesis of nicorandil (1) 2-(nicotinamide) ethyl nitrate starting from N-(2-hydroxyethyl) nicotinamide (15) and using nitric acid nitration in the presence of acetic anhydride . Background of the invention

[0002] Nicorandil is a vasodilator used in the treatment of angina. Many synthetic methods are known.

[0003] DE2714713 discloses the preparation of nicorandil (1) starting from nicotinoyl chloride hydrochloride (2) and 2-aminoethyl nitrate nitrate (3).

[0004]

[0005] A slightly modified version of the protocol proposed in DE2714713 was used in various references. US4200640 discloses the preparation of nicorandil starting from nicotinoyl chloride hydrochloride (2) and 2-aminoethyl nitrate in the presence of pyridine.

[0006]

[0007] In "Journal of Pharmaceutical Sciences (1999), 61(5), 304-305", the reaction is initiated by nicotinyl chloride (5), which is treated with 2...

Claims

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