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Facile and convenient strategy towards synthesis of 4-substituted 2-aminothiazolo[4,5-d]pyridazinones
β Scribed by Amol A. Thorave; Pinkal N. Prajapati; Jignesh P. Pethani; Krunal C. Kothari; Mukul R. Jain; Pankaj R. Patel; Rajendra K. Kharul
- Publisher
- Elsevier Science
- Year
- 2009
- Tongue
- French
- Weight
- 802 KB
- Volume
- 50
- Category
- Article
- ISSN
- 0040-4039
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β¦ Synopsis
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.
π SIMILAR VOLUMES
A procedure is described for the stepwise introduction of substituents (hydrogen included) into the imidazole ring by FGI of the bromine atoms in l-protected 2,4,5-tribromoimidazoles in the order 2 -f 5 + 4 using halogen-metal exchange techniques. Despite the considerable industrial importance of i