September 10, 2012

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The following patent record is from the CAplusSM database.


Patent Number: US 8232395
Title: Method for producing 2-(2-amino-pyrimidin-4-yl)-1H-indole-5-carboxylic acid derivatives
Inventor(s): Graeser, Joachim; Billen, Guenter; Linkies, Adolf; Metzenthin, Tobias
Patent Assignee(s): Sanofi-Aventis Deutschland G.m.b.H., Germany
Source: PCT Int. Appl., 54pp. CODEN: PIXXD2
Language: German

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.

Please note:  Abstracts for patent records in CAplus are routinely enhanced to better describe the claimed invention. In this example, CAS enhanced the abstract using additional information found in the patent.


View the full-text U.S. patent from USPTO.

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