1,2-Dichloro-3-isocyanatobenzene → HCID 67270552, compound

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Reaction Steps

Using the same general approach as for Example 524, ethyl 2-(3-(5-amino-3-(thiophen-2-yl)-1H-pyrazol-1-yl)phenyl)acetate (0.202 g, 0.403 mmol, 1.00 eq) was transformed to ethyl 2-(3-(5-amino-3-(thiophen-2-yl)-1H-pyrazol-1-yl)phenyl)propanoate. This, in turn, was combined with 2,3-dichlorophenyl isocyanate, according to general method A, to afford 2-(3-(5-(3-(2,3-dichlorophenyl)ureido)-3-(thiophen-2-yl)-1H-pyrazol-1-yl)phenyl)propanoic acid. Using general method J, this product was combined with 0.5M NH3 in dioxane (4.03 ml, 2.01 mmol, 5.00 eq) to afford 0.145 g (72%) of 1-(1-(3-(1-amino-1-oxopropan-2-yl)phenyl)-3-(thiophen-2-yl)-1H-pyrazol-5-yl)-3-(2,3-dichlorophenyl)urea.

Provenance & Evidence