186249-74-1Relevant academic research and scientific papers
Asymmetric Vinylogous Aza-Darzens Approach to Vinyl Aziridines
Chogii, Isaac,Das, Pradipta,Delost, Michael D.,Crawford, Mark N.,Njardarson, Jon T.
, p. 4942 - 4945 (2018)
A new asymmetric approach to assemble cis-vinyl aziridines is reported. A reaction of strategically substituted dienolates, decorated with a γ-leaving group, with chiral sulfinimines afforded chiral vinyl aziridine products in good to excellent yields. This is the first systematic study toward the realization of a useful asymmetric vinylogous aza-Darzens reaction. The reaction is initiated by a syn-selective addition, affording cis-vinyl aziridine products after displacement of bromide. The low syn-diastereoselectivity is attributed to competing retro-Mannich pathways.
O2-Assisted Four-Component Reaction of Vinyl Magnesium Bromide with Chiral N-tert-Butanesulfinyl Imines To Form syn-1,3-Amino Alcohols
Gao, Lu,Luo, Jingfan,Song, Zhenlei,Wang, Runping,Zhang, Hongyun,Zheng, Chunmei
supporting information, p. 24644 - 24649 (2021/10/12)
An O2-assisted, four-component reaction has been developed to synthesize a wide range of syn-1,3-amino alcohols in one step. The reaction proceeds by oxygenation of vinyl magnesium bromide (component-I) with O2 (component-II) to give
COVALENT RAS INHIBITORS AND USES THEREOF
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Page/Page column 149, (2021/06/04)
The disclosure features compounds, or pharmaceutically acceptable salts thereof, alone and in combination with other therapeutic agents, pharmaceutical compositions, and protein conjugates thereof, capable of modulating biological processes including Ras, and their uses in the treatment of cancers.
RAS INHIBITORS
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Paragraph 1433-1434, (2021/05/07)
The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.
2-(1,1 '-BIPHENYL)-1 H-BENZO[D]IMIDAZOLE DERIVATIVES AND RELATED COMPOUNDS AS APELIN AND APJ AGONISTS FOR TREATING CARDIOVASCULAR DISEASES
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Paragraph 0001, (2019/03/05)
The present invention provides compounds of Formula (I): wherein all variables are as defined in the specification. The compounds are apelin and APJ agonists for treating cardiovascular diseases. Preferred compounds are 2-(l,l'-biphe -lH-benzo[d]imidazole
Synthesis of enantiomerically pure aryl, hetero aryl and alkyl sulfinimides catalyzed by recyclable tungstophosphoric acid
Srinath,Ramu,Elavarasan,Paradesi,Kumar, R. Mohan,Ilango,Baskar
, p. 294 - 300 (2017/11/15)
A simple and efficient procedure was developed for the preparation of a variety of aryl, hetero aryl and alkyl N-sulfinylimines (2b-2u) with excellent yields (85–94%) using tungstophosphoric acid as catalyst. Also, this new synthetic protocol features hig
BICYCLIC-PYRIMIDINEDIONE COMPOUNDS
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Paragraph 0259; 0260, (2016/07/27)
The present invention provides novel bicyclic pyrimidinedione compounds that are useful for the treatment of hypertrophic cardiomyopathy (HCM) and conditions associated with left ventricular hypertrophy or diastolic dysfunction. The synthesis and characterization of the compounds is described, as well as methods for treating HCM and other forms of heart disease.
Additive effects in the palladium-catalyzed carboiodination of chiral N-allyl carboxamides
Petrone, David A.,Yoon, Hyung,Weinstabl, Harald,Lautens, Mark
supporting information, p. 7908 - 7912 (2014/08/05)
The use of Pd catalysis as a means to synthesize organic halides has recently received increased attention. Among the reported methods is the Pd-catalyzed carboiodination, which uses extremely bulky ligands to facilitate carbon-halogen reductive eliminati
Asymmetric vinylogous Mannich reactions: A versatile approach to functionalized heterocycles
Ruan, Shu-Tang,Luo, Jie-Min,Du, Yu,Huang, Pei-Qiang
supporting information; experimental part, p. 4938 - 4941 (2011/11/06)
Asymmetric vinylogous Mannich reaction (VMR) of 2-(tert- butyldimethylsilyloxy)furan (TBSOF, 1) with (RS)- or (S S)-t-BS-imines (3) furnished 5-aminoalkylbutenolides 7a-k in 75-87% yields with anti/syn ratios ranging from 75:25 to 97:3. Butenolides 7a-f,k were readily converted into substituted lactones 8 and 5 and 6-substituted 5-hydroxypiperidin-2-ones 11a-g, which are, in turn, key intermediates for the synthesis of many bioactive compounds.
Activation of the Si-B Linkage: Copper-Catalyzed addition of nucleophilic silicon to imines
Vyas, Devendra J.,Froehlich, Roland,Oestreich, Martin
supporting information; experimental part, p. 2094 - 2097 (2011/06/22)
Activation of the Si-B bond through copper-catalyzed transmetalation quickly developed into a practical method to generate Cu-Si reagents These silicon nucleophiles cleanly add to aldehyde-derived imine electrophiles to form R-silylated amines in protic media, and no carbon-tonitrogen Brook-type rearrangement of the intermediate anion is observed. Aside from electron-withdrawing groups at the imine nitrogen atom, for example, SO2Tol and P(O)Ph2, previously delicate nitrogen substituents such as phenyl or benzhydryl are tolerated. The same protocol also allows the unprecedented addition to representative ketone-derived imines.
