- Palladium(II)-Catalyzed C(sp 3)-H Activation of N,O-Ketals towards a Method for the β-Functionalization of Ketones
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A method for the formal β-functionalization of aliphatic ketones via a palladium-catalyzed sp 3 C-H activation pathway is reported. An N,O-ketal directs an aliphatic C-H carbonylation to form γ-lactams which upon hydrolysis generate γ-keto carb
- Ho, Danny K.H.,Calleja, Jonas,Gaunt, Matthew J.
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- Enantioselective Addition of Alkynyl Ketones to Nitroolefins Assisted by Br?nsted Base/H-Bonding Catalysis
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Various sets of enolizable alkynyl ketones (including methyl ynones with α-aryl, α-alkenyl, and α-alkoxy groups) were able to react smoothly with nitroolefins with the assistance of bifunctional Br?nsted base/H-bond catalysts to provide adducts with two consecutive tertiary stereocenters in a highly diastereo- and enantioselective fashion. Further transformation of the obtained adducts into optically active acyclic and polycyclic molecules, including some with intricate carbon skeletons, was also demonstrated.
- Campano, Teresa E.,Iriarte, Igor,Olaizola, Olatz,Etxabe, Julen,Mielgo, Antonia,Ganboa, I?aki,Odriozola, José M.,García, Jesús M.,Oiarbide, Mikel,Palomo, Claudio
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supporting information
p. 4390 - 4397
(2019/03/07)
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- Preparation method of 1-benzyl-8-tert-butyl-2-(hydroxymethyl)-diazaspirane decane dicarboxylate
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The invention relates to a preparation method of 1-benzyl-8-tert-butyl-2-hydroxymethyl-1,8-diazaspirane[4.5]decane-1,8-dicarboxylate, mainly aiming at solving the technical problem that a suitable industrial synthesis method does not exist at present. The
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- C5-C6-CARBOCYCLIC FUSED IMINOTHIADIAZINE DIOXIDES AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
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In its many embodiments, the present invention provides certain C5-C6-carbocyclic fused iminothiazine dioxide compounds, including compounds Formula (I): and tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1, ring A, RA, m, -L1-, ring B, RB, n, q, ring C, RC, and p are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.
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Page/Page column 79; 80
(2017/07/29)
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- C5-C6-OXACYLIC FUSED IMINOTHIAZINE DIOXIDE COMPOUNDS BEARING AN ETHER LINKER AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
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In its many embodiments, the present invention provides certain C5-C6-oxacyclic fused iminothiazine dioxide compounds bearing an ether linker, including compounds Formula (I) or a tautomer thereof, and pharmaceutically acceptable salts of said compounds a
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Page/Page column 50
(2017/09/05)
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- C5-C6-OXACYLIC FUSED IMINOTHIADIAZINE DIOXIDE COMPOUNDS BEARING AN ETHER LINKER AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
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In its many embodiments, the present invention provides certain C5-C6-oxacyclic fused iminothiadiazine dioxide compounds bearing an ether linker, including compounds Formula (I): or a tautomer thereof, and pharmaceutically acceptable salts of said compoun
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Page/Page column 49; 50
(2017/09/05)
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- C5, C6 OXACYCLIC-FUSED IMINOTHIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS
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In its many embodiments, the present invention provides certain C2-ring-substituted iminothiazine compounds, including compounds Formula (I): (structurally represented) or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and, w
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Page/Page column 57; 56
(2014/07/08)
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- C5-C6 OXACYCLIC-FUSED THIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
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In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula : (I) and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein each of ring A, ring B, ring C, R2, R3, R4, m, n, p, and -L1- is as defined herein. The novel compounds of the invention may be useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including Alzheimer's disease, are also disclosed.
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Page/Page column 61-62
(2012/10/18)
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- [3,3]-sigmatropic rearrangement/5-exo-dig cyclization reactions of benzyl alkynyl ethers: Synthesis of substituted 2-indanones and indenes
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Substituted benzyl alkynyl ethers, prepared from the corresponding α-alkoxy ketones in a two-step sequence involving enol triflate formation and KOtBu-induced E2 elimination, undergo [3,3]-sigmatropic rearrangement/ intramolecular 5-exo-dig cyclization at 60 °C to form substituted 2-indanones in good overall yields. 1,3-cis-Disubstituted-2-indanones are formed preferentially when the benzylic substituent R1 is bulky. Substituted indenes may be prepared from 2-indanones in high yields by Horner-Wadsworth-Emmons reaction.
- Tudjarian, Armen A.,Minehan, Thomas G.
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p. 3576 - 3581
(2011/06/25)
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- Expedient synthesis of 3-alkoxymethyl- And 3-aminomethyl-pyrazolo[3,4-b] pyridines
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An effective strategy has been developed for the preparation of 3-alkoxymethyl-pyrazolo[3,4-b]pyridines, compounds that are currently not readily accessible by existing synthetic methods. Further manipulation of these compounds allows for access to 3-alkoxymethyl-pyrazolo[3,4-b]pyridines with a variety of substitution patterns as well as 3-aminomethyl-pyrazolo[3,4-b] pyridines.
- Beutner, Gregory L.,Kuethe, Jeffrey T.,Kim, Mary M.,Yasuda, Nobuyoshi
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supporting information; experimental part
p. 789 - 794
(2009/06/20)
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- L-Selectride-mediated highly diastereoselective asymmetric reductive Aldol reaction: Access to an important subunit for bioactive molecules
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(Equation Presented) L-Selectride reduction of a chiral or achiral enone followed by reaction of the resulting enolate with optically active α-alkoxy aldehydes proceeded with excellent diastereoselectivity. The resulting α,α-dimethyl-β-hydroxy ketones are
- Ghosh, Arun K.,Kass, Jorden,Anderson, David D.,Xu, Xiaoming,Marian, Christine
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supporting information; experimental part
p. 4811 - 4814
(2009/05/31)
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- ANTIBACTERIAL QUINOLINE DERIVATIVES
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The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): including any stereochemically isomeric form thereof, a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or composit ions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.
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Page/Page column 48
(2008/12/06)
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- A unified synthetic approach to polyketides having both skeletal and stereochemical diversity
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An efficient systematic approach to the diversity-oriented synthesis of polyketides has been developed to provide both skeletal and stereochemical diversity. Each synthetic intermediate is also a desired polyketide fragment and no protecting group manipul
- Shang, Shiying,Iwadare, Hayato,Macks, Daniel E.,Ambrosini, Lisa M.,Tan, Derek S.
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p. 1895 - 1898
(2008/02/12)
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- Synthesis of (+)-7a-epi-7-deoxycasuarine via cross metathesis
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Olefin cross metathesis of vinyl pyrrolidine derivatives has been explored, culminating in a concise synthesis of (+)-7a-epi-7-deoxycasuarine in nine steps, from commercially available starting materials.
- Koch, David,Maechling, Simon,Blechert, Siegfried
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p. 7112 - 7119
(2008/02/07)
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- Reactions between weinreb amides and 2-magnesiated oxazoles: A simple and efficient preparation of 2-acyl oxazoles
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(Chemical Equation Presented) Treatment of oxazole or 5-aryl oxazoles with i-PrMgCl smoothly generates the corresponding 2-Grignard reagents, which react with Weinreb amides to provide exclusively 2-acyl oxazole products.
- Pippel, Daniel J.,Mapes, Christopher M.,Mani, Neelakandha S.
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p. 5828 - 5831
(2008/02/09)
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- ARYLOXYALKYLAMINE NK-1/SSRI INHIBITORS
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The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts and solvates, their pharmaceutical compositions, and their use in treating disorders associated with an excess or imbalance of tachykinins or serotonin or both.
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Page/Page column 10
(2010/02/15)
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- Non-carbonyl-stabilized metallocarbenoids in synthesis: The development of a tandem rhodium-catalyzed bamford-stevens/thermal aliphatic claisen rearrangement sequence
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A tandem rhodium-catalyzed Bamford-Stevens/Claisen rearrangement is presented. The tandem reaction uses Eschenmoser hydrazones for the in situ generation of non-carbonyl-stabilized diazo alkanes, which are presumably intercepted by Rh(II) catalysts to induce a 1,2-hydride migration. This sequence provides high levels of stereocontrol for the generation of simple acyclic (Z)-enol ethers. These enol ethers undergo either thermal or Lewis acid accelerated Claisen rearrangements to provide products of high diastereopurity. Also presented are cascade reactions, wherein a third chemical step occurs after the initial tandem sequence (i.e., Bamford-Stevens/Claisen/ene and Bamford-Stevens/Claisen/Cope). Copyright
- May, Jeremy A.,Stoltz, Brian M.
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p. 12426 - 12427
(2007/10/03)
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- MICROBIOLOGICAL SYNTHESIS OF VARIOUSLY PROTECTED L-GLYCERALDEHYDES IN HIGH OPTICAL PURITY
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Variously protected L-glyceraldehydes have been enantioselectively synthesized through a sequence involving acylation of formylanion equivalents with glycolic acid derivatives followed by baker's yeast mediated reduction of the resulting ketones.
- Guanti, Giuseppe,Banfi, Luca,Narisano, Enrica
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p. 3547 - 3550
(2007/10/02)
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