[EN] HETEROARYL COMPOUNDS AND USES THEREOF<br/>[FR] COMPOSÉS HÉTÉROARYLE ET UTILISATIONS ASSOCIÉES
申请人:CELGENE AVILOMICS RES INC
公开号:WO2014144737A1
公开(公告)日:2014-09-18
The present invention relates to compounds useful as inhibitors of protein kinases, containing a cysteine residue in the ATP binding site. The invention further provides for pharmaceutically acceptable compositions comprising therapeutically effective amounts of one or more of the protein kinase inhibitor compounds and methods of using said compositions in the treatment of cancers and carcinomas.
Enantioselective Annulation Reactions of Bisenolates Prepared Through Dearomatization Reactions of Aromatic and Heteroaromatic Diesters
作者:Jaime Pérez-Vázquez、Alberte X. Veiga、Gustavo Prado、F. Javier Sardina、M. Rita Paleo
DOI:10.1002/ejoc.201101427
日期:2012.2
A one-pot, enantioselective strategy for the dearomatization–annulation of aromaticdiesters to give a range of highly functionalized polycyclic molecules with excellent enantioselectivity is presented. This methodology is based on the reaction of bisenolates, prepared by treating aromaticdiesters with trialkyltin lithium reagents, which involves a stanna-Brook rearrangement, with 1,ω-dihaloalkanes
Formal [5+1] annulation reactions of dielectrophilic peroxides: facile access to functionalized dihydropyrans
作者:Chen Zhong、Qi Yin、Yukun Zhao、Qinfeng Li、Lin Hu
DOI:10.1039/d0cc05565d
日期:——
A general [5+1] annulation reaction, which utilized 4-bromo- or 4-mesyloxy-but-2-enyl peroxides as unique five-atom bielectrophilic synthons to participate in the C–C and the subsequent umpolung C–O bond-forming reactions with C1 nucleophiles, has been developed for the facilesynthesis of 2,2-disubstituted dihydropyrans in high yields under mild basic conditions. The dihydropyrans, which are readily
derivatives 4 through Wolff rearrangement and interaction of the tert-amino moiety with the ketene functionality. Variable amounts of either ammoniumylides 5 or of products resulting from their transformations were also formed during the course of the reaction. If the amino moiety was substituted by a benzyl or an allyl group, indolinones, resulting from [1,3] or [1,2] benzylic or allylic shifts,
A method for preparing polycondensation products of guanidine, aminoguanidine or diaminoguanidine G with one or more benzyl or allyl derivatives BA according to the following reaction scheme is provided:
wherein X, R
1
, Gua, Y and Z are as defined in the specification. In the disclosed method, at least one benzyl or allyl derivative BA is subjected to a polycondensation reaction with excessive guanidine, aminoguanidine or diaminoguanidine G upon elimination of HX.