Ticagrelor Related Compound 70 HCl synthesis

Yield:1549834-66-3 100%

Reaction Conditions:

with hydrogenchloride in methanol at 50; for 18 h;

Steps:

3 Preparation of 5-amino-2-(propylthio)pyrimidine-4,6-diol Hydrochloride (Compound IIIA-HCl)

6 M HCl (5 mL) was added to a suspension of N-(4,6-dihydroxy-2-(propylthio)pyrimidin-5-yl)acetamide of example 2 (5 g, 20.55 mmol) in MeOH (20 mL).
The resulting suspension was stirred at 50° C. for 18 h and was evaporated to dryness.
Toluene was added to the residue and the mixture was concentrated to dryness (3*20 mL) providing 5-amino-2-(propylthio)pyrimidine-4,6-diol (III-HCl) (5 g, quantitative yield, 93.5% HPLC-MS) as a yellowish solid
¹H-NMR (DMSO-d6, 400 MHz, ppm): 3.10 (t, J=6.8 Hz, 3H, CH₂), 1.65 (sex, J=6.8, 7.6 Hz, 2H, CH₂), 0.95 (t, J=7.6 Hz, 3H, CH₃).

References:

US2015/152114,2015,A1 Location in patent:Paragraph 0140 - 0142