52323-98-5Relevant academic research and scientific papers
(S)-(-)-2-tert-butyl-3-methylene-oxirane: Synthesis and hydroboration of a chiral allene oxide
Konoike,Hayashi,Araki
, p. 1559 - 1566 (1994)
The chiral allene oxide, (S)-(-)-2-tert-butyl-3-methylene-oxiran 12 ((S)-(-)-1-tert-butylallene oxide) was prepared in a moderate yield and in high enantiomeric excess by a three-step conversion starting from 4,4-dimethyl-2-pentyn-1-ol 6. The procedure wa
RECEPTOR INHIBITOR, PHARMACEUTICAL COMPOSITION COMPRISING SAME, AND USE THEREOF
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Paragraph 0161-0162, (2021/01/28)
The present invention discloses a receptor inhibitor of formula (I), a pharmaceutical composition comprising the same and the use thereof.
Transition-metal-free and facile synthesis of 3-alkynylpyrrole-2,4-dicarboxylates from methylene isocyanides and propiolaldehyde
Huo, Xiaoli,Chen, Xiaojuan,Yu, Liya,Zhang, Chong,Zeng, Linghui,Zhu, Huajian,Shao, Jiaan,Fu, Liping,Zhang, Jiankang
supporting information, p. 16430 - 16433 (2021/10/01)
A transition-metal-free, facile and efficient method for the synthesis of 3-alkynylpyrrole-2,4-dicarboxylates from methylene isocyanides and propiolaldehyde with moderate to good yields has been developed. The direct transformation process and good tolerance of various substituents make it an alternative approach to previous protocols, and potential applications of these investigated compounds are expected with or without post-modifications.
Synthesis of Axially Chiral Styrenes through Pd-Catalyzed Asymmetric C?H Olefination Enabled by an Amino Amide Transient Directing Group
Jin, Liang,Li, Ya,Liu, Lei,Liu, Yan-Hua,Shi, Bing-Feng,Song, Hong,Yao, Qi-Jun
supporting information, p. 6576 - 6580 (2020/03/10)
The atroposelective synthesis of axially chiral styrenes remains a formidable challenge due to their relatively lower rotational barriers compared to the biaryl atropoisomers. Herein, we describe the construction of axially chiral styrenes through Pd
Butenolide synthesis from functionalized cyclopropenones
Nguyen, Sean S.,Ferreira, Andrew J.,Long, Zane G.,Heiss, Tyler K.,Dorn, Robert S.,Row, R. David,Prescher, Jennifer A.
supporting information, p. 8695 - 8699 (2019/10/28)
A general method to synthesize substituted butenolides from hydroxymethylcyclopropenones is reported. Functionalized cyclopropenones undergo ring-opening reactions with catalytic amounts of phosphine, forming reactive ketene ylides. These intermediates can be trapped by pendant hydroxy groups to afford target butenolide scaffolds. The reaction proceeds efficiently in diverse solvents and with low catalyst loadings. Importantly, the cyclization is tolerant of a broad range of functional groups, yielding a variety of α- and γ-substituted butenolides.
Gold(i)-catalyzed pathway-switchable tandem cycloisomerizations to indolizino[8,7-: B] indole and indolo[2,3-a] quinolizine derivatives
Liu, Chengjun,Sun, Zenghui,Xie, Fukai,Liang, Guoduan,Yang, Lu,Li, Yaqiao,Cheng, Maosheng,Lin, Bin,Liu, Yongxiang
supporting information, p. 14418 - 14421 (2019/12/05)
Experimental and theoretical explorations were performed on the pathways of the cascade cycloisomerizations of tryptamine-N-ethynylpropiolamide substrates. The methodology provided a common strategy to access either indolizino[8,7-b]indoles or indolo[2,3-
Sodium Phenoxide Mediated Hydroxymethylation of Alkynylsilanes with N-[(Trimethylsiloxy)methyl]phthalimide
Asano, Narumi,Sasaki, Keita,Chataigner, Isabelle,Shigeno, Masanori,Kondo, Yoshinori
supporting information, p. 6926 - 6930 (2017/12/26)
The hydroxymethylation of alkynylsilanes with formaldehyde generated in situ from N-[(trimethylsiloxy)methyl]phthalimide proceeds in the presence of a stoichiometric amount of NaOPh. The reaction occurs at room temperature by using an operationally simple one-step procedure. A variety of alkynylsilanes possessing electron-donating, electron-withdrawing, and halogen groups (including heteroaryl-substituted alkynylsilanes) provide hydroxymethylated products.
HETEROARYL COMPOUNDS USEFUL AS INHIBITORS OF SUMO ACTIVATING ENZYME
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Paragraph 00227, (2015/01/16)
Disclosed are compounds of formula (I): or a pharmaceutically acceptable salt thereof; wherein Y, Ra, Ra', Rc, Rf, X2, Rd, Rd', Re, Re', m, and G have the values described herein and stereochemical configurations depicted at asterisked positions indicate absolute stereochemistry, useful as inhibitors of Sumo Activating Enzyme (SAE). Further provided are pharmaceutical compositions comprising a compound of the disclosure and methods of using the compositions in the treatment of proliferative, inflammatory, cardiovascular and neurodegenerative diseases or disorders.
BRIDGED BICYCLIC AMINO THIAZINE DIOXIDE COMPOUNDS AS INHIBITORS OF BETA-SECRETASE AND METHODS OF USE THEREOF
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Paragraph 0885; 0886, (2015/02/19)
The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, R1, R2, R3, R7 and n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, compounds of Formula III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III, and sub-Formulas thereof.
Substrate scope and stereocontrol in the Rh(II)-catalysed oxyamination of allylic carbamates
Unsworth, William P.,Lamont, Scott G.,Robertson, Jeremy
, p. 7388 - 7394 (2017/09/12)
Application of a modified Du Bois protocol for rhodium-stabilised nitrenoid generation to a variety of allylic carbamates results in 4-acetoxymethyl-1,3-oxazolidin-2-one derivatives with moderate to high levels of stereocontrol.
