Yield:66298-49-5 92%

Reaction Conditions:

with hydrogen iodide;sodium iodide in water;acetone at 20; for 18 h;

Steps:

A

Key Intermediate 6 flnt-6): |^"5-(^r3-Ethoxy-benzenesulfonyl)-thia2θl-2-vn-(6-iodo-2-methyl- pyrimidin-4-yl)-amine[0115] Part A: Hydrogen iodide (3.5 M in water, 30.0 mL) was added to a solution of 4,6- dichloro-2-methylpyrimidine (5.00 g, 0.03 mol) and sodium iodide (23.0 g, 0.15 mol) in acetone (150 mL) at RT for 2 h. The reaction mixture was stirred at RT for 16 h, poured onto ice:water [(ca. 1:1) approx. 250 mL] and allowed to warm to RT. The solids were collected by suction filtration, washed with water, and air-dried to give 4,6-diodo-2-methylpyrimidine (9.80 g, 92%) as an off-white solid. LCMS (m/z): 347 (M+H)⁺

References:

WO2007/75852,2007,A2 Location in patent:Page/Page column 33