Statistics shows that 1092286-30-0 is playing an increasingly important role. we look forward to future research findings about 5-Chloro-2-methyl-3-pyridinecarboxylic acid.
Electric Literature of 1092286-30-0, With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.1092286-30-0, name is 5-Chloro-2-methyl-3-pyridinecarboxylic acid, molecular formula is C7H6ClNO2, molecular weight is 171.58, as common compound, the synthetic route is as follows.
Example 3.1 and 3.2Trans-5-Chloro-N-[4-(5,6-dihydro-4H-cyclopentapyrazol-1 -ylmethyl)- cyclohexyl]-2-methyl-nicotinamide and Trans-5-Chloro-N-[4-(5,6-dihydro-4H- cyclopentapyrazol-2-ylmethyl)-cyclohexyl] -2-methyl-nicotlnamideTrans-4-(5,6-dihydro-4H-cyclopentapyrazof-1-ylrriethyl)-cydohexylamine(intermediate H) (118 mg, 0.461 mmol) was suspended in DMF (2 ml) and treated with 5-chloro-2-methyl-nicotinic acid (96 mg, 0.461 mmol) and HATU (210 mg, 0.554 mmol) . DIPEA (0.321 ml, 1.845 mmol) was added and the reaction mixture was stirred at RT for 1 hour. The mixture was partitioned between DC and water and the organic phase was separated and washed with water, brine, dried (MgS04) and the solvent was removed in vacuo. The crude product was purified by chromatography on basic Alumina, eluting with a iso-hexane/EtOAc to afford a -1: 1 mixture of regiosisomers.LCMS Rt = 2.15 min; [M+H 373. Method LowpH_v002. The mixture was separated using by SFC using conditions described in the ‘General Conditions’ section.Ex. 3.1 : Trans-5-Chloro-N-[4-(5,6-dihydro-4H-cyclopentapyrazol-1-ylmethyl)- cyclohexyl]-2-methyl-nicotinamide:1 H N R (500MHz, DMSO) delta 8.52 (1 H, d), 8.40 (1 H, d), 7.78 (1 H, d), 7.06 (1H, s), 3.80 (2H,d) 3.66 (1H, m), 2.66 (2H, m), 2.51 (2H, m), 2.47 (3H, s), 1.91 (2H, m), 1.73 (1H, m), 1.59 (2H, m), 1.21 (2H, m), 1.08 (2H, m).Ex. 3.2: Trans-5-Chloro-N-[4-(5,6-dihydro-4H-cyclopentapyrazol-2-ylmethyl)- cyclohexyl] -2-methyl-nicotinamide:1 H NMR {500MHz, DMSO) delta 8.52 (1 H, d), 8.40 (1 H, d), 7.78 (1 H, d), 7.27 (1 H, s), 3.83 (2H,d) 3.65 (1H, m), 2.53 (2H, m), 2.48 (3H, s), 2.30 (2H, m), 1.89 (2H, m), 1.71 (1H, m), 1.58 (2H, m), 1.20 (2H, m), 1.05 (2H, m).
Statistics shows that 1092286-30-0 is playing an increasingly important role. we look forward to future research findings about 5-Chloro-2-methyl-3-pyridinecarboxylic acid.
Reference:
Patent; NOVARTIS AG; BEATTIE, David; BRUCE, Ian; COLSON, Anny-Odile; CULSHAW, Andrew James; SHARP, Thomas; WO2011/95450; (2011); A1;,
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