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Facile and convenient strategy towards synthesis of 4-substituted 2-aminothiazolo[4,5-d]pyridazinones
Authors:Amol A. Thorave   Pinkal N. Prajapati   Jignesh P. Pethani   Krunal C. Kothari   Mukul R. Jain   Pankaj R. Patel  Rajendra K. Kharul  
Affiliation:aZydus Research Centre, Sarkhej-Bavala Highway No. 8A, Moraiya, Ahmedabad, Gujarat 382 210, India
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.
Keywords:Thiazolo[4,5-d]pyridazin-7(6H)-ones   Thiazole   N-Bromosuccinimide   Cyclization   Hydrazine hydrate
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