3182-79-4Relevant academic research and scientific papers
Synthesis of 8-deoxypumiliotoxin 193H and 9-deoxyhomopumiliotoxin 207O
Okada, Takuya,Yamamoto, Taiga,Kato, Daiki,Kawasaki, Masashi,Saporito, Ralph A.,Toyooka, Naoki
, p. 3797 - 3800 (2018)
The asymmetric synthesis of 8-deoxypumiliotoxin 193H and 9-deoxyhomopumiliotoxin 207O has been achieved, starting from both enantiomers of (+)- and (?)-10. Enantiomerically pure alcohols (+)- and (?)-10 were obtained by lipase-mediated kinetic resolution of racemic 10, which was prepared in 3 steps from new lactam-type building block (?)-8 in a highly stereoselective manner.
Easy approach to 3-benzylimino-2-pyrrolidinones from 3-chloro-4-chloromethyl-2-pyrrolidinones
Ghelfi, Franco,Ghirardini, Gianluca,Libertini, Emanuela,Forti, Luca,Pagnoni, Ugo M.
, p. 8595 - 8597 (1999)
3-Benzylimino-2-pyrrolidinones can be prepared in good yield by heating 3-chloro-4-chloromethyl-2-pyrrolidinones, benzylamine and NaI in THF at 80°C. An endo-dehydrohalogenation followed by a SN2' substitution on the intermediate allyl chloride
Discovery and Early Clinical Development of LY3202626, a Low-Dose, CNS-Penetrant BACE Inhibitor
McKinzie, David L.,Winneroski, Leonard L.,Green, Steven J.,Hembre, Erik J.,Erickson, Jon A.,Willis, Brian A.,Monk, Scott A.,Aluise, Christopher D.,Baker, Thomas K.,Lopez, Jose E.,Hendle, J?rg,Beck, James P.,Brier, Richard A.,Boggs, Leonard N.,Borders, Anthony R.,Cocke, Patrick J.,Garcia-Losada, Pablo,Lowe, Stephen L.,Mathes, Brian M.,May, Patrick C.,Porter, Warren J.,Stout, Stephanie L.,Timm, David E.,Watson, Brian M.,Yang, Zhixiang,Mergott, Dustin J.
, p. 8076 - 8100 (2021/06/28)
The beta-site APP cleaving enzyme 1, known as BACE1, has been a widely pursued Alzheimer's disease drug target owing to its critical role in the production of amyloid-beta. We have previously reported the clinical development of LY2811376 and LY2886721. L
Evaluating the Viability of Successive Ring-Expansions Based on Amino Acid and Hydroxyacid Side-Chain Insertion
Lawer, Aggie,Epton, Ryan G.,Stephens, Thomas C.,Palate, Kleopas Y.,Lodi, Mahendar,Marotte, Emilie,Lamb, Katie J.,Sangha, Jade K.,Lynam, Jason M.,Unsworth, William P.
supporting information, p. 12674 - 12683 (2020/09/17)
The outcome of ring-expansion reactions based on amino/hydroxyacid side-chain insertion is strongly dependent on ring size. This manuscript, which builds upon our previous work on Successive Ring Expansion (SuRE) methods, details efforts to better define the scope and limitations of these reactions on lactam and β-ketoester ring systems with respect to ring size and additional functionality. The synthetic results provide clear guidelines as to which substrate classes are more likely to be successful and are supported by computational results, using a density functional theory (DFT) approach. Calculating the relative Gibbs free energies of the three isomeric species that are formed reversibly during ring expansion enables the viability of new synthetic reactions to be correctly predicted in most cases. The new synthetic and computational results are expected to support the design of new lactam- and β-ketoester-based ring-expansion reactions.
MACROCYCLIC COMPOUNDS AND THEIR USE IN THE TREATMENT OF DISEASE
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Page/Page column 65, (2020/07/14)
The invention relates to heterocyclic compounds of the formula (I), in which all of the variables are as defined in the specification; capable of modulating the activity of CFTR. The invention further provides a method for manufacturing compounds of the invention, and its therapeutic uses. The invention further provides methods to their preparation, to their medical use, in particular to their use in the treatment and management of diseases or disorders including Cystic fibrosis and related disorders.
Reactions of Hexadehydro-Diels-Alder (HDDA)-Derived Benzynes with Thioamides: Synthesis of Dihydrobenzothiazino-Heterocyclics
Palani, Vignesh,Chen, Junhua,Hoye, Thomas R.
supporting information, p. 6312 - 6315 (2016/12/23)
Reaction of thioamides (e.g., II) with benzynes generated by the hexadehydro-Diels-Alder (HDDA) cycloisomerization (e.g., I) produces dihydrobenzothiazines (e.g., III). It is postulated that the reaction proceeds via benzothietene (cf. IV) and o-thiolatoa
BACE INHIBITORS
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Page/Page column 20-21, (2014/05/24)
The present invention provides compounds of Formula I useful as BACE inhibitors in the treatment of e.g. Alzheimer's disease : wherein A is selected from the group consisting of; of; R1 is H or F; R2 is H, -OCH3, C1-C3 alkyl,; R3 is H, -CH3, or -OCH3; and R4 is H or F; or a pharmaceutically acceptable salt thereof.
A versatile polypeptoid platform based on N-allyl glycine
Robinson, Joshua W.,Schlaad, Helmut
supporting information; experimental part, p. 7835 - 7837 (2012/08/29)
N-Allyl glycine N-carboxyanhydride (NCA) was synthesized and polymerized by ring opening polymerization under homo- or heterophase conditions to afford well-defined polypeptoids (MW = 1.5-10.5 kg mol-1, PDI = 1.1-1.4). Poly(N-allyl glycine) demonstrated stimuli-responsive behaviour in water and was readily modified via thiol-ene photochemistry under experimentally benign conditions. This journal is
Efficient and stereodivergent synthesis of deoxyimino sugars
Hong, Bor-Cherng,Chen, Zhong-Yi,Nagarajan, Arumugam,Kottani, Rudresha,Chavan, Vishal,Chen, Wei-Hung,Jiang, Yea-Fen,Zhang, Shuo-Cang,Liao, Ju-Hsiou,Sarshar, Sepehr
, p. 2457 - 2468 (2007/10/03)
Both cis- and trans-2-substituted-1,2,3,6-tetrahydro-pyridin-3-ols have been prepared via an aldol condensation-ring-closing metathesis sequence. A stereodivergent synthesis of optionally functionalized deoxyimino sugars was achieved via asymmetric dihydroxylation or epoxidation/nucleophilic substitution of these tetrahydropyridines.
Novel lincomycin derivatives possessing antimicrobial activity
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, (2008/06/13)
Novel lincomycin derivatives are disclosed. These lincomycin derivatives exhibit antibacterial activity. The compounds of the subject invention may exhibit potent activities against bacteria, including gram positive organisms, and may be useful antimicrobial agents. Methods of synthesis and of use of the compounds are also disclosed.
