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CAPLUS COPYRIGHT 2012 ACS
||Method for producing 2-(2-amino-pyrimidin-4-yl)-1H-indole-5-carboxylic acid derivatives
||Graeser, Joachim; Billen, Guenter; Linkies, Adolf; Metzenthin, Tobias
||Sanofi-Aventis Deutschland G.m.b.H., Germany
||PCT Int. Appl., 54pp. CODEN: PIXXD2
The invention relates to a method for producing the compds. of formula I, to novel intermediates obtained during the production of the compds. of formula I and to their use as intermediates for producing IkB kinase inhibitors. Compds. of formula I wherein R1 is H, C1-12 alkyl, C6-14 aryl, C3-8 cycloalkyl, and 4- to 15-membered heterocycle; R2 and R3 are independently H, C1-12 alkyl, (un)substituted C6-14 aryl, C3-8 cycloalkyl and 4- to 15-membered heterocycle; P is H and N-protecting group; and their method for preparing them are claimed. Example compound II was prepared by alkynylation of Me 4-amino-3-iodobenzoate with trimethylsilylacetylene; the resulting 4-amino-3-(trimethylsilylethynyl)benzoic acid Me ester underwent desilylation to give 4-amino-3-ethynylbenzoic acid Me ester, which underwent cross-coupling with 2-(methylamino)-4-chloropyrimidine to give 4-amino-3-[(2-methylaminopyrimidin-4-yl)ethynyl]benzoic acid Me ester, which underwent cyclization to give compound II.
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