Discovery of 1103234-56-5

The synthetic route of 1103234-56-5 has been constantly updated, and we look forward to future research findings.

1103234-56-5, name is 2,6-Difluoro-3-(propylsulfonamido)benzoic acid, belongs to amides-buliding-blocks compound, is considered to be a conventional heterocyclic compound, which is widely used in drug synthesis. The chemical synthesis route is as follows. Recommanded Product: 1103234-56-5

Step A: Diphenylphosphonic azide (9.082 mL, 0.04214 mol) was added to stirred solution of 2,6-difluoro-3-(propylsulfonamido)benzoic acid (10.234 g, 0.036647 mol) and triethylamine (11.75 mL, 0.08429 mol) in tetrahydrofuran (100 mL, 1 mol) and the reaction mixture was stirred at room temperature for 3 hours and then heated to reflux for an additional hour. lH-pyrazole (2.5 g, 0.037 mol) was added to the reaction mixture, followed by heating to reflux for 1 additional hour. After cooling to room temperature and removal of the solvent under reduced pressure, an orange-colored oil was obtained. This crude material was purified by silica gel chromatography; eluent: 0-50% ethyl acetate: heptane. The obtained material was recrystalized from 150 mL of a solution of ethyl acetate / heptane (1:3, v/v) to give N-(2,6- difluoro-3-(propylsulfonamido)phenyl)-lH-pyrazole-l-carboxamide with 90% purity (4.4 g, 87%). 1H NMR (500 MHz, DMSO-d6) delta 10.33 (s, IH), 9.70 (s, IH), 8.41 (d, J=2.6, IH), 7.92 (d, J=Ll, IH), 7.42 (td, J=8.9, 5.8, IH), 7.22 (t, J=9.2, IH), 6.62 (dd, J=2.7, 1.6, IH), 3.13 – 3.03 (m, 2H), 1.80 – 1.70 (m, 2H), 1.04 – 0.93 (m, 3H). LC/MS: m/z 345.2 [M+l].

The synthetic route of 1103234-56-5 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; GENENTECH, INC.; ALIAGAS, Ignacio; GRADL, Stefan; GUNZNER, Janet; MATHIEU, Simon; PULK, Rebecca; RUDOLPH, Joachim; WEN, Zhaoyang; WO2011/25965; (2011); A1;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics