- Kinetic resolution of 5H-pyrrolo[1,2-a]imidazol-7-ol, 6,7-dihydro under continuous flow conditions: An intermediate for chiral ionic liquids synthesis
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In this letter we disclosed an efficient method for the kinetic resolution of an imidazole derivate both in batch and continuous flow conditions. This imidazole derivative has been described to have important applications in different fields and it was obtained, in its enantiomerically pure form, with excellent enantiomeric excess, good yields and short time using continuous flow conditions.
- De Miranda, Amanda S.,Gomes, Juliana C.,Rodrigues Jr., Manoel T.,Costa, Ingrid C.R.,Almeida, Wanda P.,Lopes, Raquel De O.,Miranda, Leandro S.M.,Coelho, Fernando,De Souza, Rodrigo O.M.A.
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- SMALL MOLECULE INHIBITORS OF NF-kB INDUCING KINASE
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The present invention relates to compounds that inhibit NIK and pharmaceutical compositions comprising such compounds and methods of using the same. These compounds and pharmaceutical compositions are envisaged to be useful for preventing or treating diseases such as cancer (such as B-cell malignancies including leukemias, lymphomas and myeloma), inflammatory disorders, autoimmune disorders, immunodermatologic disorders such as palmoplantar pustulosis and hidradenitis suppurativa, and metabolic disorders such as obesity and diabetes.
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Page/Page column 135
(2020/12/11)
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- Substituted (E)-2-methylene-3,4-cyclohexenones through direct and convenient synthesis from cyclohexenone-MBH alcohol in the presence of DMAP
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An unexpected and effective DMAP catalyzed one-step construction of 3,4-cyclohexenone skeleton from simple and easily available cyclohexenone-MBH alcohol has been disclosed. A series of substituted (E)-2-methylene-3,4-cyclo-hexenones have been effectively prepared in excellent yields (up to 93 %) under convenient reaction conditions. Succesful scale-up preparation and synthetic transformations have demonstrated the potentials of this new protocol.
- Ren, Hong-Xia,Song, Xiang-Jia,Wu, Lin,Huang, Zhi-Cheng,Zou, Ying,Li, Xia,Chen, Xiao-Wen,Tian, Fang,Wang, Li-Xin
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supporting information
p. 715 - 719
(2019/01/04)
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- BICYCLIC KETONE COMPOUNDS AND METHODS OF USE THEREOF
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The invention provides novel compounds having the general formula (I): (I) wherein R1, the A ring and the B ring are as described herein, pharmaceutical compositions including the compounds, and methods of using the compounds.
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Page/Page column 60; 61
(2019/02/02)
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- A double-ring structure with imidazole kind of chiral small organic molecular compound and its synthetic method
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The invention relates to an iminazole chiral organic micromolecule compound with a bicyclo-structure, as shown in chemical formula (I), and a synthesizing method thereof. The compound can be applied in various asymmetric reactions as a chiral catalyst, such as asymmetric acylation, asymmetric phosphorylation, asymmetric sulfonylation, asymmetric halogenate, asymmetric Micheal addition, asymmetricSteglich rearrangement reaction, asymmetric Morita-Baylis-Hillman reaction and the like. In addition, the compound also has potential bioactivities, such as anti-ulcer, anti-depression, antibiosis andenzyme inhibitory activities and the like.
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Paragraph 0052; 0053; 0054
(2017/02/23)
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- Enantioselective Black rearrangement catalyzed by chiral bicyclic imidazole
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A newly developed chiral imidazole nucleophilic catalyst, Acyloxy-DPI, was readily prepared and successfully applied to the enantioselective Black rearrangement with up to 88% ee for a wide range of substrates possessing different substituted groups. A pl
- Wang, Mingli,Zhang, Zhenfeng,Liu, Shan,Xie, Fang,Zhang, Wanbin
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supporting information
p. 1227 - 1230
(2014/02/14)
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- Efficient catalysis of aqueous Morita-Baylis-Hillman reactions of cyclic enones by a bicyclic imidazolyl alcohol
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In this paper a new phosphorus-free catalyst for the Morita-Baylis-Hillman reaction is disclosed. A bicyclic imidazolyl alcohol having a Lewis basic center associated with a hydrogen-bond donor group was used as catalyst for the reaction. Aliphatic cycloalkanones such as 2-cyclopentenone and 2-cyclohexanone and aliphatic and aromatic aldehydes were used successfully, and the reaction was found to work nicely using water as solvent in the presence of a phase-transfer additive. Copyright
- Gomes, Juliana C.,Rodrigues Jr., Manoel T.,Moyano, Albert,Coelho, Fernando
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p. 6861 - 6866
(2013/02/23)
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- 6,5-HETEROCYCLIC PROPARGYLIC ALCOHOL COMPOUNDS AND USES THEREFOR
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The invention relates to novel compounds of Formula I: wherein A, Y, R1, R2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.
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Page/Page column 93
(2015/05/06)
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- Chiral bicycle imidazole nucleophilic catalysts: Rational design, facile synthesis, and successful application in asymmetric Steglich rearrangement
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A new type of chiral bicycle imidazole nucleophilic catalyst was rationally designed, facilely synthesized, and successfully applied in an asymmetric Steglich rearrangement with good to excellent yield and enantioselectivity at ambient temperature. Moreov
- Zhang, Zhenfeng,Xie, Fang,Jia, Jia,Zhang, Wanbin
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supporting information; experimental part
p. 15939 - 15941
(2011/01/11)
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