These common heterocyclic compound, 24243-71-8, name is Propane-1-sulfonamide, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route. HPLC of Formula: C3H9NO2S
A mixture of 5-(6-chloro-2-phenylpyrimidin-4-yl)-1,3-dimethylpyridin-2(1H)-one (51 mg, 0.2 mmol), propane-1-sulfonamide (37 mg, 0.3mmo1), Pd(dba)3 (18 mg, 0.02 mmol), Xphos (9 mg, 0.2 mmol), CsCO3 (130 mg, 0.4 mmol) in dioxane (3 mL) was stirred and heated at 90 C. for 16 hr. The reaction mixture was diluted with water and extracted with EtOAc (3*). The extracts were combined, washed with brine, dried (Na2SO4) and concentrated. The residue was purified by flash column chromatography (EA:Hex, 0-100%) to provide the 16 mg (23%) of the desired product as an off-white solid. 1H NMR (400 MHz, DMSO-d6) delta ppm 0.99 (t, J=7.45 Hz, 3H) 1.78 (sxt, J=7.38 Hz, 2H) 2.14 (s, 3H) 3.32 (s, 3H) 3.62 (s, 3H) 3.63-3.69 (m, 2H) 7.06 (s, 1H) 7.51-7.59 (m, 3H) 7.99 (s, 1H) 8.41-8.52 (m, 2H) 8.64 (d, J=2.27 Hz, 1H) 11.26 (br. s., 1H).
The synthetic route of Propane-1-sulfonamide has been constantly updated, and we look forward to future research findings.
Reference:
Patent; CELGENE QUANTICEL RESEARCH, INC.; Bennett, Michael John; Betancort, Juan Manuel; Boloor, Amogh; Kanouni, Toufike; Stafford, Jeffrey Alan; Veal, James Marvin; Wallace, Michael Brennan; (250 pag.)US2017/298040; (2017); A1;,
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