Facile and convenient strategy towards synthesis of 4-substituted 2-aminothiazolo[4,5-d]pyridazinones |
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Authors: | Amol A. Thorave Pinkal N. Prajapati Jignesh P. Pethani Krunal C. Kothari Mukul R. Jain Pankaj R. Patel Rajendra K. Kharul |
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Affiliation: | aZydus Research Centre, Sarkhej-Bavala Highway No. 8A, Moraiya, Ahmedabad, Gujarat 382 210, India |
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Abstract: | Convenient synthesis of 4-substituted 2-aminothiazolo[4,5-d]pyridazinones has been achieved in 12 steps with overall yield of 19% by employing Grignard reaction as the key step. The route utilizes well established thiazole ring formation followed by Grignard reaction to introduce substitution at 4-position effectively. In addition to the use of inexpensive chemicals, the present route first time gave access to the 4-substituted 2-aminothiazolo [4,5-d]pyridazinones with free amino group at C-2 position. |
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Keywords: | Thiazolo[4,5-d]pyridazin-7(6H)-ones Thiazole N-Bromosuccinimide Cyclization Hydrazine hydrate |
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