101349-95-5Relevant articles and documents
Diverse ortho-C(sp2)-H functionalization of benzaldehydes using transient directing groups
Liu, Xi-Hai,Park, Hojoon,Hu, Jun-Hao,Hu, Yan,Zhang, Qun-Liang,Wang, Bao-Long,Sun, Bing,Yeung, Kap-Sun,Zhang, Fang-Lin,Yu, Jin-Quan
, p. 888 - 896 (2017)
Pd-catalyzed C-H functionalizations promoted by transient directing groups remain largely limited to C-H arylation only. Herein, we report a diverse set of ortho-C(sp2)-H functionalizations of benzaldehyde substrates using the transient directing group strategy. Without installing any auxiliary directing group, Pd(II)-catalyzed C-H arylation, chlorination, bromination, and Ir(III)-catalyzed amidation, could be achieved on benzaldehyde substrates. The transient directing groups formed in situ via imine linkage can override other coordinating functional groups capable of directing C-H activation or catalyst poisoning, significantly expanding the scope for metal-catalyzed C-H functionalization of benzaldehydes. The utility of this approach is demonstrated through multiple applications, including late-stage diversification of a drug analogue.
ANTIPROLIFERATION COMPOUNDS AND USES THEREOF
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, (2019/11/11)
The present invention provides compounds of Formula I′, or pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods of use thereof for treating cellular proliferative disorders (e.g., cancer).
Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP2 Receptor Antagonist for Treatment of Asthma
Sandham, David A.,Barker, Lucy,Brown, Lyndon,Brown, Zarin,Budd, David,Charlton, Steven J.,Chatterjee, Devnandan,Cox, Brian,Dubois, Gerald,Duggan, Nicholas,Hall, Edward,Hatto, Julia,Maas, Janet,Manini, Jodie,Profit, Rachael,Riddy, Darren,Ritchie, Catherine,Sohal, Bindi,Shaw, Duncan,Stringer, Rowan,Sykes, David A.,Thomas, Matthew,Turner, Katharine L.,Watson, Simon J.,West, Ryan,Willard, Elisabeth,Williams, Gareth,Willis, Jennifer
supporting information, p. 582 - 586 (2017/05/17)
Further optimization of an initial DP2 receptor antagonist clinical candidate NVP-QAV680 led to the discovery of a follow-up molecule 2-(2-methyl-1-(4-(methylsulfonyl)-2-(trifluoromethyl)benzyl)-1H-pyrrolo[2,3-b]pyridin-3-yl)acetic acid (compou