- Metallaphotoredox Perfluoroalkylation of Organobromides
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Ruppert-Prakash type reagents (TMSCF3, TMSC2F5, and TMSC3F7) are readily available, air-stable, and easy-to-handle fluoroalkyl sources. Herein, we describe a mild, copper-catalyzed cross-coupling of these fluoroalkyl nucleophiles with aryl and alkyl bromides to produce a diverse array of trifluoromethyl, pentafluoroethyl, and heptafluoropropyl adducts. This light-mediated transformation proceeds via a silyl-radical-mediated halogen atom abstraction pathway, which enables perfluoroalkylation of a broad range of organobromides of variable steric and electronic demand. The utility of the method is demonstrated through the late-stage functionalization of several drug analogues.
- Zhao, Xiangbo,MacMillan, David W. C.
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supporting information
p. 19480 - 19486
(2020/12/18)
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- Discovery of potent and selective dipeptidyl peptidase IV inhibitors derived from β-aminoamides bearing subsituted triazolopiperazines
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A series of β-aminoamides bearing triazolopiperazines have been discovered as potent, selective, and orally active dipeptidyl peptidase IV (DPP-4) inhibitors by extensive structure-activity relationship (SAR) studies around the triazolopiperazine moiety.
- Kim, Dooseop,Kowalchick, Jennifer E.,Brockunier, Linda L.,Parmee, Emma R.,Eiermann, George J.,Fisher, Michael H.,He, Huaibing,Leiting, Barbara,Lyons, Kathryn,Scapin, Giovanna,Patel, Sangita B.,Petrov, Aleksandr,Pryor, Kelly Ann D.,Roy, Ranabir Sinha,Wu, Joseph K.,Zhang, Xiaoping,Wyvratt, Matthew J.,Zhang, Bei B.,Zhu, Lan,Thornberry, Nancy A.,Weber, Ann E.
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p. 589 - 602
(2008/09/17)
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- FUSED TRIAZOLE DERIVATIVES AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
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The present invention is directed to novel fused triazole derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme ("DPP-IV inhibitors") and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
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Page/Page column 47
(2008/06/13)
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