- Asymmetric Hydroacylation Involving Alkene Isomerization for the Construction of C3-Chirogenic Center
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A new transformation pattern for enantioselective intramolecular hydroacylation has been developed involving an alkene isomerization strategy. Proceeding through a five-membered rhodacycle intermediate, 3-enals were converted to C3- or C3,C5-chirogenic cyclopentanones with satisfactory yields, diastereoselectivities, and enantioselectivities. A catalytic cycle has been theoretically calculated and the origin of the stereoselection is rationally explained.
- Liu, Chong,Yuan, Jing,Zhang, Zhenfeng,Gridnev, Ilya D.,Zhang, Wanbin
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supporting information
p. 8997 - 9002
(2021/03/16)
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- Deadly KCN and pricey metal free track for accessing β-ketonitriles employing mild reaction conditions
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A one pot synthesis of β-ketonitriles from readily accessible 3-chloropropenals using economically benign iodine, aqueous ammonia and sodium hydroxide solution, employing mild reaction conditions have been described. This report presents a convenient, inexpensive, highly toxic-matter-free and eco-friendly approach for β-ketonitriles.
- Sharma, Pawan K.,Kumar, Rajiv,Ram, Sita,Chandak, Navneet
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supporting information
p. 1847 - 1856
(2021/04/26)
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- Selective Synthesis of β-Ketonitriles via Catalytic Carbopalladation of Dinitriles
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A practical, convenient, and highly selective method of synthesizing β-ketonitriles from the Pd-catalyzed addition of organoboron reagents to dinitriles has been developed. This method provides excellent functional-group tolerance, a broad scope of substrates, and the convenience of using commercially available substrates. The method is expected to show further utility in future synthetic procedures.
- Zeng, Ge,Liu, Jichao,Shao, Yinlin,Zhang, Fangjun,Chen, Zhongyan,Lv, Ningning,Chen, Jiuxi,Li, Renhao
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p. 861 - 867
(2021/01/09)
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- SeO2-Mediated One-Pot Synthesis of 3-Cyanofurans from 3-Oxo-3-arylpropanenitriles and Substituted Acetaldehydes
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An SeO2-mediated one-pot method was established for the synthesis of 3-cyanofurans from 3-oxo-3-arylpropanenitriles and substituted acetaldehydes. The generality of the reaction was explored, and a plausible mechanism is proposed.
- Zhou, Jie,Zhu, Xinhai,Huang, Manna,Wan, Yiqian
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supporting information
p. 2317 - 2321
(2017/05/01)
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- Substrate-controlled switchable asymmetric annulations to access polyheterocyclic skeletons
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An unexpected domino process from Morita-Baylis-Hillman carbonates of isatins and acrylate and α-cyano-α,β-unsaturated ketones to deliver highly enantioenriched tetrahydrofuro[2′,3′:4,5]pyrano[2,3-b]indoles catalysed by cinchona-derived tertiary amines, involving α-regioselective cyclopropanation, ring-opening, and ring-closure cascade reactions, was disclosed. In contrast, spirooxindoles incorporating a cyclopentene motif were produced through [3+2] annulations by employing Morita-Baylis-Hillman carbonates from isatins and acrylonitrile under similar catalytic conditions. Density functional theory calculations were conducted to elucidate the novel domino process and the switchable annulation reactions.
- Wang, Kai-Kai,Wang, Pan,Ouyang, Qin,Du, Wei,Chen, Ying-Chun
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supporting information
p. 11104 - 11107
(2016/09/19)
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- Pyrazolotriazines as inhibitors of nucleases
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The invention provides compounds represented by the structural formula (1): wherein R1, R2, R3 and R4 are as defined in the claims. The compounds are inhibitors of nucleases, and are useful in particular in a method of treatment and/or prevention of proliferative diseases, neurodegenerative diseases, and other genomic instability associated diseases.
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Paragraph 0104; 0105; 0106; 0107; 0115-0121
(2016/01/12)
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- PYRAZOLOPYRIMIDINYL INHIBITORS OF UBIQUITIN-ACTIVATING ENZYME
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Disclosed are chemical entities that inhibit ubiquitin-activating enzyme (UAE), each of which is a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein Y is and W, Z, XY, RY1, RY2 and RY3 are defined herein; pharmaceutical compositions comprising the chemical entities; and methods of using the chemical entities. These chemical entities are useful for treating disorders, particularly cell proliferation disorders, including cancers.
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Paragraph 0269; 0270
(2013/08/28)
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- Synthesis and biological effects of novel 2-amino-3-naphthoylthiophenes as allosteric enhancers of the A1, adenosine receptor
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The current study describes the synthesis and biological evaluation of a novel series of 2-amino-3-naphthoylthiophenes, with variable modifications at the 4- and 5-position of the thiophene as well as the naphthoyl ring. Allosteric enhancer activity was m
- Baraldi, Pier Giovanni,Romagnoli, Romeo,Pavani, Maria Giovanna,Del Carmen Nu?ez, Maria,Tabrizi, Mojgan Aghazadeh,Shryock, John C.,Leung, Edward,Moorman, Allan R.,Uluoglu, Canan,Iannotta, Valeria,Merighi, Stefania,Borea, Pier Andrea
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p. 794 - 809
(2007/10/03)
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- Indium-mediated coupling of bromoacetonitriles with aromatic acyl cyanides: convenient synthesis of aromatic α-cyano ketones
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Indium-mediated coupling of bromoacetonitrile and 2-bromopropionitrile with a variety of aromatic acyl cyanides afforded the corresponding aromatic α-cyano ketones in moderate to good yields under mild and neutral conditions.
- Yoo, Byung Woo,Hwang, Sun Kyun,Kim, Dong Yoon,Choi, Jin Woo,Ko, Jae Jung,Choi, Kyung Il,Kim, Joong Hyup
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p. 4813 - 4816
(2007/10/03)
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- Pharmacologically active CNS compounds
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The invention relates to compounds of formula (I) and salts thereof wherein R1 and R2 are the same or different and are each selected from hydroxy, or a group NR9R10 wherein R9 and R10 are each hydrogen, alkyl, aryl, arylalkyl or together with the nitrogen atom to which they are attached form a ring, optionally containing a further heteroatom and optionally further substituted by alkyl, aryl or arylalkyl;, R3 is selected from hydrogen, haloalkyl, alkyl and halo, R4 to R8 are the same or different, and are each selected from hydrogen, halo, nitro, amino, sulphonamido or alkylsulphonylamino;, or R4 and R5 or R5 and R6 may together form a carbocyclic ring;, with the proviso that at least one of R4 to R8 is other than hydrogen. The compounds may be used for the treatment or prophylaxis of a neurodegenerative or other neurological disorder of the CNS, the aetiology of which includes excessive release of the neurotransmitter glutamate.
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