104863-68-5Relevant academic research and scientific papers
Palladium(II)-Catalyzed C(sp 3)-H Activation of N,O-Ketals towards a Method for the β-Functionalization of Ketones
Ho, Danny K.H.,Calleja, Jonas,Gaunt, Matthew J.
, p. 454 - 458 (2019)
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
Enantioselective Addition of Alkynyl Ketones to Nitroolefins Assisted by Br?nsted Base/H-Bonding Catalysis
Campano, Teresa E.,Iriarte, Igor,Olaizola, Olatz,Etxabe, Julen,Mielgo, Antonia,Ganboa, I?aki,Odriozola, José M.,García, Jesús M.,Oiarbide, Mikel,Palomo, Claudio
supporting information, p. 4390 - 4397 (2019/03/07)
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.
Preparation method of 1-benzyl-8-tert-butyl-2-(hydroxymethyl)-diazaspirane decane dicarboxylate
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, (2017/12/27)
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
C5-C6-CARBOCYCLIC FUSED IMINOTHIADIAZINE DIOXIDES AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
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Page/Page column 79; 80, (2017/07/29)
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.
C5-C6-OXACYLIC FUSED IMINOTHIAZINE DIOXIDE COMPOUNDS BEARING AN ETHER LINKER AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
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Page/Page column 50, (2017/09/05)
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
C5-C6-OXACYLIC FUSED IMINOTHIADIAZINE DIOXIDE COMPOUNDS BEARING AN ETHER LINKER AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
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Page/Page column 49; 50, (2017/09/05)
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
C5, C6 OXACYCLIC-FUSED IMINOTHIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS
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Page/Page column 57; 56, (2014/07/08)
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
C5-C6 OXACYCLIC-FUSED THIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
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Page/Page column 61-62, (2012/10/18)
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.
[3,3]-sigmatropic rearrangement/5-exo-dig cyclization reactions of benzyl alkynyl ethers: Synthesis of substituted 2-indanones and indenes
Tudjarian, Armen A.,Minehan, Thomas G.
, p. 3576 - 3581 (2011/06/25)
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.
Expedient synthesis of 3-alkoxymethyl- And 3-aminomethyl-pyrazolo[3,4-b] pyridines
Beutner, Gregory L.,Kuethe, Jeffrey T.,Kim, Mary M.,Yasuda, Nobuyoshi
supporting information; experimental part, p. 789 - 794 (2009/06/20)
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.
