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.2002-24-6, name is 2-Aminoethanol hydrochloride, molecular formula is C2H8ClNO, molecular weight is 97.544, as common compound, the synthetic route is as follows.name: 2-Aminoethanol hydrochloride
A dichloromethane (5 ml) solution of the [6-[(4-chlorophenylsulfonyl)(2,5-difluorophenyl)methyl]pyridin-3-yl]carboxylic acid (100 mg, 0.236 mmol) obtained in Example 50 were added triethylamine (80 mul, 0.566 mmol), 4-dimethylaminopyridine (15 mg, 0.118 mmol), 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (54 mg, 0.283 mmol) and ethanolamine hydrochloride (28 mg, 0.283 mmol). The resulting mixture was stirred at room temperature for 17.5 hours. The reaction mixture was diluted with dichloromethane. The diluted mixture was washed sequentially with water, a saturated aqueous solution of sodium bicarbonate and brine. The organic layer thus obtained was dried over magnesium sulfate and concentrated under reduced pressure. The residue thus obtained was subjected to flash silica gel column chromatography. The fraction obtained from the dichloromethane_methanol=30:1 eluate was concentrated under reduced pressure to give the title compound (69 mg, 0.148 mmol, 63%) as a white powder. 1H-NMR (400MHz, CDCl3) delta: 2.38 (1H,t, J=4.9Hz), 3.65 (2H,td, J=5.4, 4.9Hz), 3.85 (2H,q, J=4.6Hz), 5.99 (1H,s), 6.77 (1H,brs), 6.90-6.96 (1H,m), 7.00-7.06 (1H,m), 7.42 (2H,d, J=8.6Hz), 7.56 (2H,d, J=8.6Hz), 7.70 (1H,d, J=8.1Hz), 7.97-8.01 (1H,m), 8.15 (1H,dd, J=8.1, 2.2Hz), 8.99 (1H,d, J=2.2Hz)H,m), mp: 179 to 181C. Elemental Analysis for C21H17ClF2N2O4S: Calculated: C,54.02; H, 3.67; Cl, 7.59; F,8.14; N,6.00; S,6.87. Found: C, 53.83; H,3.63; Cl, 7.72; F, 8.14; N,6.06; S, 7.02.
At the same time, in my other blogs, there are other synthetic methods of this type of compound,2002-24-6, 2-Aminoethanol hydrochloride, and friends who are interested can also refer to it.
Reference:
Patent; DAIICHI PHARMACEUTICAL CO., LTD.; EP1640366; (2006); A1;,
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