- Access to dihydropyrano[3,2-: B] pyrrol-5-ones skeletons by N-heterocyclic carbene-catalyzed [3+3] annulations
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A novel and efficient NHC-catalyzed [3+3] annulation of enals with pyrrol-4-ones was developed, thus providing the dihydropyrano[3,2-b]pyrrol-5-one core structures with broad scope and good to excellent enantioselectivities. Notably, this strategy could also expand to the synthesis of axially chiral compounds and polysubstituted indoles.
- Duan, Xiao-Yong,Qi, Jing,Sun, Bo-Yu,Wu, Ya-Tong,Yu, Hai-Fei,Zhang, Rui
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supporting information
p. 9854 - 9857
(2020/09/09)
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- QUINAZOLINE AND QUINOLINE COMPOUNDS AND USES THEREOF
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This invention provides compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein T, J, R, R4, Rq, o, RA, W and RB and subsets thereof are as described in the specification. The compounds are inhibitors of NAMPT and are thus useful for treating cancer, inflammatory conditions, and/or T-cell mediated autoimmune disease.
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Paragraph 00399
(2016/08/17)
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- Ru-catalyzed asymmetric hydrogenation of γ-heteroatom substituted β-keto esters
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A series of enantiomerically pure γ-heteroatom substituted β-hydroxy esters were synthesized with high enantioselectivities (up to 99.1% ee) by hydrogenation of γ-heteroatom substituted β-keto esters in the presence of Ru-(S)-SunPhos catalyst. These asymmetric hydrogenations provide key building blocks for a variety of naturally occurring and biologically active compounds.
- Fan, Weizheng,Li, Wanfang,Ma, Xin,Tao, Xiaoming,Li, Xiaoming,Yao, Ying,Xie, Xiaomin,Zhang, Zhaoguo
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experimental part
p. 9444 - 9451
(2012/01/13)
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- Bicyclic Dihydropyrimidines and Uses Thereof
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The present invention provides compounds having formula (I): (I) and pharmaceutically acceptable derivatives thereof; as described generally and in subclasses herein, which compounds are useful as kinesin inhibitors (e.g., Eg5 inhibitors), and thus are useful, for example, for the treatment of proliferative disorders e.g., cancer. The invention additionally provides methods for preparing compounds of the invention, compositions comprising them, and methods for the use thereof in the treatment of various disorders where Eg5 is involved. In certain embodiments, the present invention provides for compounds, compositions, methods and systems for inhibiting cell growth. More specifically, the present invention provides for methods, compounds and compositions which are capable of inhibiting mitosis in metabolically active cells. Compounds, compositions and methods of the present invention inhibit the activity of a protein involved in the assembly and maintenance of the mitotic spindle. One class of proteins which acts on the mitotic spindle is the family of mitotic kinesins, a subset of the kinesin superfamily.
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- A convergent route for the total synthesis of malyngamides O, P, Q, and R
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(Chemical Equation Presented) A convergent, enantioselective and general synthetic route to a class of marine natural products - malyngamides O (1), P (2), Q (3), R (4), 5″-epi-3 and 5″-epi-4 - bearing a novel vinyl chloride structural motif was developed. The key steps involved construction of the vinyl chloride functionality by Wittig reaction, a DCC/HOBt-promoted amidation, an aldol reaction in the construction of the basic backbone of 1, 2, 3, 4, 5″-epi-3, and 5″-epi-4, and methylation of an enol moiety via either base/acid conditions or a Mitsunobu reaction. Moreover, the absolute configuration of the stereogenic center at C-5″ in 3 was further confirmed by synthesis of the natural product and its C-5″ epimer.
- Chen, Jie,Fu, Xiao-Gang,Zhou, Ling,Zhang, Jun-Tao,Qi, Xian-Liang,Cao, Xiao-Ping
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supporting information; experimental part
p. 4149 - 4157
(2009/09/08)
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- Cdc7 kinase inhibitors: Pyrrolopyridinones as potential antitumor agents. 1. Synthesis and structure-activity relationships
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Cdc7 kinase is an essential protein that promotes DNA replication in eukaryotic organisms. Genetic evidence indicates that Cdc7 inhibition can cause selective tumor-cell death in a p53-independent manner, supporting the rationale for developing Cdc7 small-molecule inhibitors for the treatment of cancers. In this paper, the synthesis and structure-activity relationships of 2-heteroaryl-pyrrolopyridinones, the first potent Cdc7 kinase inhibitors, are described. Starting from 2-pyridin-4-yl-1,5,6,7-tetrahydro-pyrrolo[3,2-c] pyridin-4-one, progress toward a simple scaffold, tailored for Cdc7 inhibition, is reported.
- Vanotti, Ermes,Amici, Raffaella,Bargiotti, Alberto,Berthelsen, Jens,Bosotti, Roberta,Ciavolella, Antonella,Cirla, Alessandra,Cristiani, Cinzia,D'Alessio, Roberto,Forte, Barbara,Isacchi, Antonella,Martina, Katia,Menichincheri, Maria,Molinari, Antonio,Montagnoli, Alessia,Orsini, Paolo,Pillan, Antonio,Roletto, Fulvia,Scolaro, Alessandra,Tibolla, Marcellino,Valsasina, Barbara,Varasi, Mario,Volpi, Daniele,Santocanale, Corrado
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p. 487 - 501
(2008/09/18)
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- PYRROLOPYRROLONES ACTIVE AS KINASE INHIBITORS
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Compounds represented by formula (I) wherein A, R1, R2, R3, and R4 are as defined in the specification, compositions thereof, and methods of use thereof.
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Page/Page column 34
(2010/11/28)
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- BENZOXAZEPINE COMPOUND
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A compound represented by the formula [1]: wherein ring A and ring B each represent an optionally substituted benzene ring; ring C represents an optionally further substituted aromatic ring; R1 represents a lower alkyl group optionally substituted with an optionally substituted hydroxyl group; X1a represents a bond or optionally substituted lower alkylene; X1b represents a bond or optionally substituted lower alkylene; X2 represents a bond, -O- or -S-; X3 represents a bond or an optionally substituted divalent hydrocarbon group; Y represents an optionally esterified or amidated carboxyl group, or a salt thereof. The compound of the formula [I] is safer and has more potent lipid lowering activity such as squalene synthase inhibitory activity (cholesterol lowering activity) and triglyceride lowering activity, and thus it is a compound useful as an agent for preventing or treating hyperlipemia.
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Page/Page column 23-24
(2010/11/08)
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- Stereoselective enol tosylation: Preparation of trisubstituted α,β-unsaturated esters
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(Chemical Equation Presented) The stereoselective preparation of (E)- or (Z)-trisubstituted α,β-unsaturated esters in three steps from N-protected glycine is presented. The key step in the synthesis is the highly selective enol tosylation of γ-amino β-keto esters. The enol tosylates are stable, crystalline compounds that undergo smooth and effective Suzuki-Miyaura coupling reaction with a variety of aryl boronic acids.
- Baxter, Jenny M.,Steinhuebel, Dietrich,Palucki, Michael,Davies, Ian W.
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p. 215 - 218
(2007/10/03)
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- Copper(I)-Promoted Condensation of α-Amino Acids with β-Keto Thio Esters: Synthesis of N-Acylated L-Leucine Derivatives Containing (S)-4-Hydroxy-5-methyl- and (S)-4-Hydroxy-2,5-dimethyl-3-oxohexanoic Acid
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Acylation of lithium enolates of ethyl acetate and ethyl thioacetate with derivatives of (S)-2-hydroxy-3-methylbutanoic acid, activated at the carboxyl function as the acid chloride, unsymmetrical carbonic anhydride, or active ester, furnished the corresp
- Kim, Hwa-Ok,Olsen, Richard K.,Choi, Ok-Soon
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p. 4531 - 4536
(2007/10/02)
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