Electric Literature of 121492-06-6, These common heterocyclic compound, 121492-06-6, name is N-Boc-(2-Aminoethyl)-N-methylamine, 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.
Example 128: N-{5-[3-(4-Bromo-2-fluoro-phenylamino)-pyridin-4-yl]- [1 ,3,4]oxadiazol-2-yl}-N’-methyl-ettiane-1 ,2-diamine; Step 1 : 5-[3-(4-Bromo-2-fluoro-phenylamino)-pyridin-4-yl]-3H-[1 ,3,4]oxadiazol-2-one (example 19, 100mg, 0.277mmol) was dissolved in ethanol (3ml), N-(2-aminoethyl)-N – methylcarbamic acid ^-butylester (96rng, 0.554mmol) was added and the mixture was stirred for20min at 1500C in a microwave oven. The volatiles were removed to give the crude compound, which was used in the next step.Step 2: Dry dichloromethane (5ml) was added to the product derived from step 1 followed by triphenylphosphine (113rng, 0.429mmol), triethylamine (58mul, 0.416mmol) and carbon tetrachloride (107mul, 1.11 mmol). The mixture was heated at 1000C for20min in a microwave oven, the volatiles were removed and the crude material was purified by preparative HPLC to give 87mg (62/yield) of the Boc-protected title compound. The material was treated with 4N HCI in dioxane (4ml) for 1h at ambient temperature and the volatiles were removed to give the pure title compound. LC-MS (method V): rt = 1.94rnin; m/z [M+ H]+ 407/409.
The synthetic route of 121492-06-6 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; APPLIED RESEARCH SYSTEMS ARS HOLDING N.V.; WO2006/45514; (2006); A1;,
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