16019-31-1Relevant academic research and scientific papers
An improved synthesis of 4-chloro-7H-pyrrolo[2,3-d]pyrimidine
Zhang, Yu-Liu,Xu, Cheng-Tao,Liu, Ting,Zhu, Yong,Luo, Yu
, p. 638 - 642 (2018/08/17)
[Figure not available: see fulltext.] An improved seven-step synthesis of 4-chloro-7H-pyrrolo[2,3-d]pyrimidine from dimethyl malonate with 31% overall yield is described. The procedure is operationally simple and practical for the synthesis of the 4-chloro-7H-pyrrolo[2,3-d]pyrimidine building block.
ATROPISOMERISM FOR ENHANCED KINASE INHIBITOR SELECTIVITY
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Page/Page column 33, (2019/01/10)
The invention provides a series of conformationally stable and selective kinase inhibitors, and methods of using the kinase inhibitors. The effect of atropisomerism on kinase selectivity was assessed, finding improved selectivity compared to rapidly inter
Exploiting Atropisomerism to Increase the Target Selectivity of Kinase Inhibitors
Smith, Davis E.,Marquez, Isaac,Lokensgard, Melissa E.,Rheingold, Arnold L.,Hecht, David A.,Gustafson, Jeffrey L.
supporting information, p. 11754 - 11759 (2015/10/05)
Many biologically active molecules exist as rapidly interconverting atropisomeric mixtures. Whereas one atropisomer inhibits the desired target, the other can lead to off-target effects. Herein, we study atropisomerism as a possibility to improve the sele
TMPZnOPiv?LiCl: A new base for the preparation of air-stable solid zinc pivalates of sensitive aromatics and heteroaromatics
Stathakis, Christos I.,Manolikakes, Sophia M.,Knochel, Paul
supporting information, p. 1302 - 1305 (2013/05/09)
A wide range of aryl and heteroaryl zinc pivalates bearing sensitive functionalities were prepared by selective metalation using TMPZnOPiv?LiCl, a new hindered zinc amide base. The new zinc reagents are easy-to-handle solids, which maintain their activity almost entirely (>95%) after 4 h of air exposure and smoothly undergo Negishi cross-couplings and reactions with various electrophiles such as Cu(I)-catalyzed acylations and allylations.
A ring-closing metathesis approach to heterocycle-fused azepines
Moss, Thomas A.
supporting information, p. 993 - 997 (2013/03/28)
Heterocycle-fused azepines, an important class of molecular scaffold, are readily synthesised through the ruthenium-catalysed ring-closing metathesis reaction. Although benzo-fused azepines are well documented, heterocycle-fused examples are poorly developed. Herein, a range of five- and six-membered heterocycle-fused azepines are investigated, allowing access to a series of pharmaceutically interesting products.
CYCLOLIC HYDRAZINE DERIVATIVES AS HIV ATTACHMENT INHIBITORS
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Page/Page column 61-62, (2013/09/26)
Compounds of Formula I are provided, including pharmaceutically acceptable salts thereof: wherein A is selected from the group consisting of: wherein Z is selected from the group consisting of: which are useful as HIV attachment inhibitors.
Discovery of 6,7-dihydro-5H-pyrrolo[2,3-a]pyrimidines as orally available g protein-coupled receptor 119 agonists
Katamreddy, Subba R.,Carpenter, Andrew J.,Ammala, Carina E.,Boros, Eric E.,Brashear, Ron L.,Briscoe, Celia P.,Bullard, Sarah R.,Caldwell, Richard D.,Conlee, Christopher R.,Croom, Dallas K.,Hart, Shane M.,Heyer, Dennis O.,Johnson, Paul R.,Kashatus, Jennifer A.,Minick, Doug J.,Peckham, Gregory E.,Ross, Sean A.,Roller, Shane G.,Samano, Vicente A.,Sauls, Howard R.,Tadepalli, Sarva M.,Thompson, James B.,Xu, Yun,Way, James M.
, p. 10972 - 10994 (2013/02/25)
GPR119 is a 7-transmembrane receptor that is expressed in the enteroendocrine cells in the intestine and in the islets of Langerhans in the pancreas. Indolines and 6,7-dihydro-5H-pyrrolo[2,3-a]pyrimidines were discovered as G protein-coupled receptor 119
PRODUCTION AND USE OF ZINC AMIDES
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Page/Page column 10-11, (2011/12/12)
The application relates to a reagent of the general formula [in-line-formulae]R1R2N—ZnY LiY??(I)[/in-line-formulae] wherein R1, R2 are, independently, selected from H, substituted or unsubstituted aryl or heteroaryl containing one or more heteroatoms, linear, branched or cyclic, substituted or unsubstituted alkyl, alkenyl, alkynyl, or silyl derivatives thereof; and R1 and R2 together can be part of a cyclic or polymeric structure; and wherein at least one of R1 and R2 is other than H; Y is selected from the group consisting of F; Cl; Br; I; CN; SCN; NCO; Halon, wherein n=3 or 4 and Hal is selected from Cl, Br and I; NO3; BF4; PF6; H; a carboxylate of the general formula RXCO2; an alcoholate of the general formula ORX; a thiolate of the general formula SRX; RXP(O)O2; or SCORX; or SCSRX; OnSRx; wherein n=2 or 3; or NOn, wherein n=2 or 3; and a derivative thereof; wherein Rx is a substituted or unsubstituted aryl or heteroaryl containing one or more heteroatoms, linear, branched or cyclic, substituted or unsubstituted alkyl, alkenyl, alkynyl, or derivatives thereof, or H; or as adduct with a solvent; as well as to the preparation and use thereof. 34
FUSED BICYCLIC PYRIMIDINE DERIVATIVES AND METHODS OF USE THEREOF
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Page/Page column 34, (2011/06/19)
The present invention relates to Fused Bicyclic Pyrimidine Derivatives, compositions comprising a Fused Bicyclic Pyrimidine Derivative, and methods of using the Fused Bicyclic Pyrimidine Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G-protein coupled receptor (GPCR) in a patient.
BICYCLIC HETEROCYCLE DERIVATIVES AND USE THEREOF AS GPR119 MODULATORS
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Page/Page column 76-77, (2010/04/03)
The present invention relates to Bicyclic Heterocycle Derivatives of Formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metaboli
