150884-51-8Relevant articles and documents
Synthesis of highly substituted 2-spiropiperidines
Griggs, Samuel D.,Thompson, Nathan,Tape, Daniel T.,Fabre, Marie,Clarke, Paul A.
, p. 6663 - 6674 (2018/09/29)
2-Spiropiperidines are a highly desirable, yet under represented structure in drug discovery. 2-Spiropiperidines were synthesised in either a two-pot or one-pot reaction. In the two-pot reaction, the addition of a Weiler dianion to N-Boc imines, followed by deprotection and in situ condensation with a cyclic ketone generated functionalised 2-spiropiperidines in good to excellent yields. In the one-pot reaction, the addition of Chan's diene to N-Boc imines under Maitland-Japp conditions, followed by the addition of sodium bicarbonate and a cyclic ketone formed functionalised 2-spiropiperidines in moderate to good yields.
PYRAZOLE AMIDE DERIVATIVE
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Page/Page column 201, (2015/09/28)
The present invention relates to a novel compound having a function of inhibiting RORγ activity. The present invention also relates to pharmaceutical composition comprising the compound, a use of the compound in treating or preventing autoimmune diseases, inflammatory diseases, metabolic diseases, or cancer diseases.
Rhodium(III)-catalyzed arylation of Boc-imines via C-H bond functionalization
Tsai, Andy S.,Tauchert, Michael E.,Bergman, Robert G.,Ellman, Jonathan A.
supporting information; experimental part, p. 1248 - 1250 (2011/04/16)
The first rhodium-catalyzed arylation of imines proceeding via C-H bond functionalization is reported. Use of a non-coordinating halide abstractor is important to obtain reactivity. Aryl-branched N-Boc-amines are formed, and a wide range of functionality is compatible with the reaction.