Process for preparation of substituted nicotinamides

A technology of dimethylamino and methoxymethyl, applied in the field of preparation of substituted nicotinamide, which can solve the problems of cumbersome steps and low yield
CN114773352AActive Publication Date: 2022-07-22SHANGHAI SIMR BIOTECHNOLOGY CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SHANGHAI SIMR BIOTECHNOLOGY CO LTD
Publication Date
2022-07-22

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Abstract

The invention relates to a method for preparing substituted nicotinamide of a formula (1), which comprises the following steps: step 1): 1, 4-dichlorophthalazine of a formula (I), a compound of a formula (II) and a compound of a formula (IV) are used as starting raw materials to react, and a compound of a formula (V) is obtained by a one-pot method; the preparation method comprises the following steps of 1, carrying out a saponification reaction on a compound shown in a formula (V) to obtain a compound shown in a formula (VI), and 2, carrying out a saponification reaction on the compound shown in the formula (V) to obtain a compound shown in a formula (VI), and 3, carrying out a reaction on the compound shown in the formula (VI) and isopropylamine in the presence of a condensing agent to obtain N-isopropyl-6-(((3-(5-(methoxymethyl) isoxazole-3-yl)-[1, 2, 4] triazole [3, 4-a] phthalazin-6-yl) oxygen) methyl) nicotinamide shown in a formula (1).
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Description

technical field

[0001] The present invention relates to N-isopropyl-6-(((3-(5-(methoxymethyl)isoxazol-3-yl)-[1,2,4]triazo[3,4-a] ] phthalazin-6-yl) oxy) methyl) nicotinamide synthesis process. Background technique

[0002] N-isopropyl-6-(((3-(5-(methoxymethyl)isoxazol-3-yl)-[1,2,4]triazolo[3,4-a]phthalazine -6-yl)oxy)methyl)nicotinamide is an antagonist of the α5-GABAA receptor and is described in Chinese patent application CN2019101857359.

[0003] Antagonists of α5-GABAA receptors were recently identified as useful in the treatment of pain, particularly neuropathic pain (WO), and N-isopropyl-6-(((3-(5-(methoxymethyl) Isoxazol-3-yl)-[1,2,4]triazolo[3,4-a]phthalazin-6-yl)oxy)methyl)nicotinamide was identified as a candidate drug whose structure is shown in formula (1 ) as shown:

[0004]

[0005] For the preparation of N-isopropyl-6-(((3-(5-(methoxymethyl)isoxazol-3-yl)-[1,2,4]triazole[3 in the prior art ,4-a]phthalazin-6-yl)oxy)methyl)nicotinamide method has low yie...

Claims

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