129946-64-1Relevant articles and documents
Method for synthesizing tetrahydroindazole compound
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Paragraph 0037; 0038; 0049; 0050; 0061; 0062; 0075, (2019/06/27)
The invention belongs to the technical field of drug synthesis, and particularly relates to a method for synthesizing a tetrahydroindazole compound. The synthesis method comprises the steps of synthesis of 5,5-dimethyl-2-acetyl-1,3-cyclohexanedione, synthesis of 2 fluoro-4-hydrazinylbenzonitrile, synthesis of 2-fluoro-4-(3,6,6-trimethyl-4-oxo-4,5,6,7-tetrahydro-1H-indazol-1-)benzonitrile, synthesis of 2-(4-hydroxycyclohexylamino)-4-(3,6,6-trimethyl-4-oxo-4,5,6,7-tetrahydro-1H-indazol-1-)benzonitrile, and synthesis of 2-(4-hydroxycyclohexylamino)-4-(3,6,6-trimethyl-4-oxo-4,5,6,7-tetrahydro-1H-indazol-1-)benzamide. The yield of the intermediate 2-fluoro-4-(3,6,6-trimethyl-4-oxo-4,5,6,7-tetrahydro-1H-indazol-1-)benzonitrile is up to 93%, the purity is high, and the prepared tetrahydroindazolecompound is high in purity and suitable for mass production.
A highly selective Hsp90 affinity chromatography resin with a cleavable linker
Hughes, Philip F.,Barrott, Jared J.,Carlson, David A.,Loiselle, David R.,Speer, Brittany L.,Bodoor, Khaldon,Rund, Lauretta A.,Haystead, Timothy A.J.
supporting information; experimental part, p. 3298 - 3305 (2012/07/14)
Over 200 proteins have been identified that interact with the protein chaperone Hsp90, a recognized therapeutic target thought to participate in non-oncogene addiction in a variety of human cancers. However, defining Hsp90 clients is challenging because interactions between Hsp90 and its physiologically relevant targets involve low affinity binding and are thought to be transient. Using a chemo-proteomic strategy, we have developed a novel orthogonally cleavable Hsp90 affinity resin that allows purification of the native protein and is quite selective for Hsp90 over its immediate family members, GRP94 and TRAP 1. We show that the resin can be used under low stringency conditions for the rapid, unambiguous capture of native Hsp90 in complex with a native client. We also show that the choice of linker used to tether the ligand to the insoluble support can have a dramatic effect on the selectivity of the affinity media.
N-arly-substituted nitrogen-containing heterocycles, processes and novel intermediates for their preparation, and their use as herbicides and plant growth regulators
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, (2008/06/13)
Substituted triazolinone compounds of the formula: wherein the variables R1, R2, R7, R8, R12 and X are as defined in the specification are useful as herbicides, plant growth regulators, insecticides a