- Selective C-C Bond Cleavage of Cycloalkanones by NaNO2/HCl
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A novel selective fragmentation of cycloalkanones by NaNO2/HCl has been established. The C-C bond cleavage reaction proceeds smoothly under mild conditions, selectively affording versatile keto acids or oxime acids. The methodology can streamline the synthesis of valuable chiral molecules and isocoumarins from readily available feedstocks.
- He, Tianyu,Chen, Dengfeng,Qian, Shencheng,Zheng, Yu,Huang, Shenlin
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supporting information
p. 6525 - 6529
(2021/09/02)
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- p-Toluenesulfonic acid catalysed fluorination of α-branched ketones for the construction of fluorinated quaternary carbon centres
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A p-toluenesulfonic acid catalyzed fluorination of α-branched ketones for the construction of fluorinated quaternary carbon centers has been developed, featuring a broad substrate scope, environmentally benign reaction conditions, and operational simplicity.
- Tang, Shi-Zhong,Bian, Hong-Li,Zhan, Zong-Song,Chen, Meng-En,Lv, Jian-Wei,Xie, Shaolei,Zhang, Fu-Min
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p. 12377 - 12380
(2018/11/30)
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- Discovery of N-(2-aryl-cyclohexyl) substituted spiropiperidines as a novel class of GlyT1 inhibitors
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Screening of the Roche compound library led to the identification of cis-N-(2-phenyl-cyclohexyl)-spiropiperidine 1 as structurally novel GlyT1 inhibitor. The SAR, which was developed in this series, resulted in the discovery of highly potent compounds displaying excellent selectivity against the GlyT2 isoform.
- Pinard, Emmanuel,Ceccarelli, Simona M.,Stalder, Henri,Alberati, Daniela
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p. 349 - 353
(2007/10/03)
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- TRIAZA-SPIROPIPERIDINE DERIVATIVES FOR USE AS GLYT-1 INHIBITORS IN THE TREATMENT OF NEUROLOGICAL AND NEUROPSYCHIATRIC DISORDERS
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The invention relates to compounds of the general formula (I), wherein A-A is -CH2-CH2-, -CH2-CH2-CH2-, -CH2-0- or -0-CH2-; x is hydrogen or hydroxy; R1 is aryl or heteroaryl, unsubstituted or substituted by one or more substituents, selected from the group consisting of lower alkyl, lower alkoxy, halogen or trifluoromethyl; R2 is aryl or heteroaryl, unsubstituted or substituted by one or more substituents, selected from the group consisting of lower alkyl, lower alkoxy, halogen or trifluoromethyl, or is lower alkyl, -(CH2)n--cycloalkyl, -(CH2)n-CF3, -(CH2)p-0-lower alkyl, -(CH2)1,2-phenyl, optionally substituted by halogen, lower alkyl, lower alkoxy or trifluoromethyl, or is -(CH2)p-NRR", wherein W and R" form together with the N-atom a heterocyclic ring, selected from the group consisting of piperidine, morpholine, thiomorpholine or 1, I-dioxo thiomorpholine; R3, R4 are independently from each other hydrogen, lower alkyl, phenyl or benzyl; R5 is hydrogen, lower alkyl or benzyl; R6 is hydrogen or lower alkyl; n is 0, 1 or 2; and p is 2 or 3; and to pharmaceutically acceptable acid addition salts thereof for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.
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Page/Page column 32
(2010/02/11)
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- SUBSTITUENT EFFECTS ON THE REGIO- AND STEREOSELECTIVITY OF GAS-PHASE ACID-INDUCED RING OPENING IN 1-ARYLCYCLOHEXENE OXIDES
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Comparative analysisof the ratio of the isomeric monomethyl ethers of 1-arylcyclohexane-1,2-diols formed in the gas-phase and solvolytic acid-induced methanolysis of several 1-arylcyclohexene oxides indicates the intrinsic electronic factors detrminimg the regio- and stereochemical course of the nucleophilic attack, related to the partial degree of carbocationic character at the reaction centre in the substitution transition state.
- Cecchi, P.,Pizzabiocca, A.,Renzi,G.,Chini, M.,Crotti, P.,et al.
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p. 4227 - 4234
(2007/10/02)
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