Electric Literature of 92525-10-5, As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 92525-10-5 name is 3-Iodo-1-methyl-1H-pyrazole, This compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below.
A suspension of 3 ,3-dimethyl-6- (4,4,5 ,5-tetramethyl- 1,3 ,2-dioxaborolan-2-yl)indolin-2-one (200 mg) and 5-bromo-2-methylpyrimidine (181 mg) in 1,4-dioxane (2 ml) and aqueous sodiumcarbonate (2 M) was flushed with argon, then [1,1?-bis(diphenylphosphino)ferrocene] dichloropalladium(II) (26 mg) was added and stirring was continued at 115 C for 3 h. The mixture was evaporated and the residue purified by flash chromatography (silica gel, gradient, 0% to 10% MeOH in dichloromethane) to give the title compound (148 mg, 84%) as a brown solid. MS (mlz): 254.2 [(M+H) :_The title compound was prepared in analogy to example ic using 3,3-dimethyl-6-(4,4,5,5- tetramethyl- 1,3 ,2-dioxaborolan-2-yl)indolin-2-one from example lb and 3-iodo- i-methyl-i Hpyrazole to give the title compound (26%) as an off-white solid. MS (mlz): 242.1 [(M+H)?i.
At the same time, in my other blogs, there are other synthetic methods of this type of compound, 3-Iodo-1-methyl-1H-pyrazole, and friends who are interested can also refer to it.
Reference:
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; HILPERT, Hans; KOLCZEWSKI, Sabine; HUMM, Roland; STOLL, Theodor; MUSER, Thorsten; PLANCHER, Jean-Marc; GAUFRETEAU, Delphine; (142 pag.)WO2015/197567; (2015); A1;,
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics