140410-47-5Relevant articles and documents
Hydrogen-Bonding Pincer Complexes with Two Protic N-Heterocyclic Carbenes from Direct Metalation of a 1,8-Bis(imidazol-1-yl)carbazole by Platinum, Palladium, and Nickel
Marelius, David C.,Darrow, Evan H.,Moore, Curtis E.,Golen, James A.,Rheingold, Arnold L.,Grotjahn, Douglas B.
, p. 10988 - 10992 (2015)
Pincer protic N-heterocyclic carbene (PNHC) complexes were synthesized by direct metalation, the formation of a metal carbon bond from an unfunctionalized C-H bond in a single synthetic step. Significantly, direct metalation succeeded even for a first-row metal, nickel. The chloride complexes were isolated and then converted to the acetate, triflate, or in the platinum case, a hydride analogue. Crystal structures and 1H, 13C, and 15NNMR data, as well as IR spectra, document the effects of intramolecular hydrogen bonding and the planar but flexible pincer framework. Anti-Markovnikov addition of O-H bonds to alkynes, including catalyzed alkyne hydration, were demonstrated on the Pt triflate analog. Protic N-heterocyclic carbenes in a pinch: Unusual bis-protic N-heterocyclic carbene (PNHC) pincer complexes were synthesized by direct metalation, making two metal-carbon bonds from unfunctionalized C-H bonds in a single synthetic step. Significantly, direct metalation succeeded even for a first-row metal, nickel (see scheme).
Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: Structure-activity relationship of the aryl region
Probst, Gary D.,Bowers, Simeon,Sealy, Jennifer M.,Stupi, Brian,Dressen, Darren,Jagodzinska, Barbara M.,Aquino, Jose,Gailunas, Andrea,Truong, Anh P.,Tso, Luke,Xu, Ying-Zi,Hom, Roy K.,John, Varghese,Tung, Jay S.,Pleiss, Michael A.,Tucker, John A.,Konradi, Andrei W.,Sham, Hing L.,Jagodzinski, Jacek,Toth, Gergely,Brecht, Eric,Yao, Nanhua,Pan, Hu,Lin, May,Artis, Dean R.,Ruslim, Lany,Bova, Michael P.,Sinha, Sukanto,Yednock, Ted A.,Gauby, Shawn,Zmolek, Wes,Quinn, Kevin P.,Sauer, John-Michael
scheme or table, p. 6034 - 6039 (2010/11/04)
The structure-activity relationship of the prime region of hydroxyethylamine BACE inhibitors is described. Variation in the aryl linker region with 5- and 6-membered heterocycles provided compounds such as 33 with improved permeability and reduced P-gp liability compared to benzyl amine analog 1.
METHODS OF TREATMENT OF AMYLOIDOSIS USING ASPARTYL-PROTEASE INHIBITORS
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Page/Page column 198, (2010/02/13)
The invention relates to acetyl 2-hydroxy-1,3-diaminospirocyclohexanes and derivatives thereof that are useful in treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.
SUBSTITUTED UREA AND CARBAMATE, PHENACYL-2-HYDROXY-3-DIAMINOALKANE, AND BENZAMIDE-2-HYDROXY-3-DIAMINOALKANE ASPARTYL-PROTEASE INHIBITORS
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Page/Page column 227-228, (2010/02/14)
The invention relates to acetyl 2-hydroxy-1,3-diaminospirocyclohexanes and derivatives thereof that are useful in treating at least one disease, disorder, and condition associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and condition associated with abnormal deposition of A-beta protein.
SYNTHESIS OF CHROMANONES
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Page 44, (2008/06/13)
Processes for the preparation of biologically active chromanones are disclosed, including processes for the preparation of intermediates useful in the preparation of the biologically active chromanones. The chromanones and the intermediates disclosed herein may be useful for a variety of therapies, including the treatment of various cancers and the treatment of inflammation and inflammation related disorders.
