Synthetic Route of 121492-06-6, As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 121492-06-6 name is N-Boc-(2-Aminoethyl)-N-methylamine, This compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below.
To a solution of N-methyl-N-Boc-ethylenediamine (2.05 ml, 11.48 mmol) and NaCNBH3(685 mg, 10.9 mmol) in MeOH (20 mL) was added 2,4,6-trimethoxybenzaldehyde (2.14 g,10.9 mmol) as a solution in MeOH/DCM 1:1 v/v (40 ml) over 2 h. The mixture was stirred at room temperature for 1 h, acidified with 0.4 M HC1 (60 mL) and stirred further 30 mm. The reaction mixture was extracted 4 times with 150 mL ethyl acetate. The combined organic phase was washed with sat. NaHCO3 solution (200 mL) and brine (90 mL), dried overNa2SO4 and the solvents were evaporated under reduced pressure. The resulting N-methyl-NBoc-N?-Tmob-ethylenediamine 2a was dried in vacuo and used in the next reaction step without further purification.Yield: 4.02 g, 99%, colorless oil.
At the same time, in my other blogs, there are other synthetic methods of this type of compound, N-Boc-(2-Aminoethyl)-N-methylamine, and friends who are interested can also refer to it.
Reference:
Patent; ASCENDIS PHARMA A/S; BISEK, Nicola; WEISBROD, Samuel; BIGOTT, Kornelia; (116 pag.)WO2018/11266; (2018); A1;,
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