- Regioselective methylenation and in situ methanolation of ketones prone to C-C double-bond isomerisation
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An efficient methylenation reaction in isomer-labile ketones is described. The methylenation reaction is based on an improved method for the formation of bis(iodozincio)methane [CH2(ZnI)2]. A subsequent in situ hydroboration-oxidation sequence provides the corresponding methanol derivatives in high yields without double-bond isomerisation. Georg Thieme Verlag Stuttgart.
- Bjornstad, Vidar,Undheim, Kjell
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Read Online
- Chemoselective hydrosilylation of carboxylic acids using a phosphine-free ruthenium complex and phenylsilane
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A highly chemoselective hydrosilylation of carboxylic acids was achieved using a bench-stable, phosphine-free Ru-complex tethered with hemi-labile thiophene ligands as the catalyst, employing phenylsilane as the reducing agent. The methodology was further elaborated towards the one-pot synthesis of indole and benzoxazine via tandem reduction/cyclization of acid and nitro group.
- Abhilash, Vishwanathan,Gadakh, Amol V.,Ganesh, Sambasivam,Hegde, Shivaprasad N.,Jacob, Anand,Karthik, C. S.,Lamees, Thundianandi,Mathivanan, Namachivayam,Sathiyanarayanan, Arumugam Murugan
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supporting information
(2022/03/01)
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- NON-LYSOSOMAL GLUCOSYLCERAMIDASE INHIBITORS AND USES THEREOF
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The invention provides compounds for inhibiting glucosylceramidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds.
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Paragraph 00199
(2020/12/01)
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- Acid-Promoted Hydroformylative Synthesis of Alcohol with Carbon Dioxide by Heterobimetallic Ruthenium-Cobalt Catalytic System
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The acid-aided heterobimetallic ruthenium-cobalt catalytic system for the reductive hydroformylation with carbon dioxide was established. Various alkenes, including waste from biomass and petroleum industry, could be upgraded to valuable alcohols with this protocol. Acid-promoted reverse water-gas shift (RWGS), thereby accelerating the hydroformylative synthesis of alcohol. The theoretical computations revealed that acid promoted RWGS by facilitating the dehydroxylation of ruthenium hydroxy carbonyl intermediate.
- Zhang, Xuehua,Tian, Xinxin,Shen, Chaoren,Xia, Chungu,He, Lin
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p. 1986 - 1992
(2019/03/17)
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- GLUCOSYLCERAMIDE SYNTHASE INHIBITORS FOR THE TREATMENT OF DISEASES
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Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions associated with the enzyme glucosylceramide synthase (GCS).
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Paragraph 000258
(2015/04/15)
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- ALPHA-KETOHETEROCYCLES AND METHODS OF MAKING AND USING
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Compounds are disclosed that are effective in inhibition of fatty acid amide hydrolase, an enzyme responsible for catabolism of endogenous cannabinoids such as anandamide. The compounds are useful as analgesic compounds and as sleep-inducing compounds, that can be orally administered, and that can have a relatively long duration of effect. Methods of preparation of the compounds are also provided. The compounds are conformationally constrained analogs of heterocyclylketones such as oxazolylketones.
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Page/Page column 135
(2012/08/27)
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- Reversible competitive α-ketoheterocycle inhibitors of fatty acid amide hydrolase containing additional conformational constraints in the acyl side chain: Orally active, long-acting analgesics
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A series of α-ketooxazoles containing conformational constraints in the C2 acyl side chain of 2 (OL-135) were examined as inhibitors of fatty acid amide hydrolase (FAAH). Only one of the two possible enantiomers displayed potent FAAH inhibition (S vs R en
- Ezzili, Cyrine,Mileni, Mauro,McGlinchey, Nicholas,Long, Jonathan Z.,Kinsey, Steven G.,Hochstatter, Dustin G.,Stevens, Raymond C.,Lichtman, Aron H.,Cravatt, Benjamin F.,Bilsky, Edward J.,Boger, Dale L.
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supporting information; experimental part
p. 2805 - 2822
(2011/06/24)
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- Identification of a novel class of succinyl-nitrile-based Cathepsin S inhibitors
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The synthesis and in vitro activities of a series of succinyl-nitrile-based inhibitors of Cathepsin S are described. Several members of this class show nanomolar inhibition of the target enzyme as well as cellular potency. The inhibitors displaying the greatest potency contain N-alkyl substituted piperidine and pyrrolidine rings spiro-fused to the α-carbon of the P1 residue.
- Bekkali, Younes,Thomson, David S.,Betageri, Raj,Emmanuel, Michel J.,Hao, Ming-Hong,Hickey, Eugene,Liu, Weimin,Patel, Usha,Ward, Yancey D.,Young, Erick R.R.,Nelson, Richard,Kukulka, Alison,Brown, Maryanne L.,Crane, Kathy,White, Della,Freeman, Dorothy M.,Labadia, Mark E.,Wildeson, Jessi,Spero, Denice M.
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p. 2465 - 2469
(2008/03/11)
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- 2-CYANOPYRROLOPYRIMIDINES AND PHARMACEUTICAL USES THEREOF
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The invention relates to pyrrolo pyrimidines of formula (I), wherein Y represents -(CH2)t-O- or -(CH2)r-S-, p is 1 or 2, r is 1, 2 or 3, t is 1, 2 or 3, or Y is -(CH2)j- or -CH=CH-, j is 1 or 2; p is 1 or 2, or Y is -(CH2)f-, f is 1 or 2, p is 1, and the further radicals and symbols have the meaning as defined herein; their preparation, their use as pharmaceuticals, pharmaceutical compositions containing them, the use of such a compound for the manufacture of a pharmaceutical preparation for the treatment of neuropathic pain and to a method for the treatment of such a disease in animals, especially in humans.
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Page/Page column 36
(2010/02/08)
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- Photochemical synthesis of highly functionalized cyclopropyl ketones
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A series of di- and trisubstituted cyclopropyl ketones 11 were prepared by irradiation of ketones 3 and 5, which bear a leaving group adjacent to the carbonyl C-atom. The required ketones 3 could be easily synthesized either by functionalization of ketones 1 with a hypervalent iodine reagent, 2, or by O-sulfonylation of α-hydroxy ketones 7. The nitrates 5 were obtained by treatment of the corresponding α-bromo ketones with AgNO3. The irradiation of 3 and 5 must be performed in the presence of an acid scavenger (1-methyl-1H-imidazole) to obtain the cyclopropanes 11 in good yields. The synthetic efficiency of the method was, among other things, demonstrated by the preparation of a highly strained bicyclo[2.1.0]pentane 11i in good yield. The mechanism of the photochemical cyclization was investigated by means of photokinetic measurements, as well as by quantum-chemical calculations. It was shown that the presence of the leaving group substantially influences all steps of the photochemical reaction cascade. The X-ray crystal structures of 11j and exo-11k were also determined.
- Wessig, Pablo,Muehling, Olaf
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p. 865 - 893
(2007/10/03)
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- Thromboxane A2 synthetase inhibitors. 2. Syntheses and activities of tetrahydronaphthalene and indan derivatives.
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A series of 1-imidazolylalkyl-substituted or 5-thiazolylalkyl-substituted tetrahydronaphthalenecarboxylic acid and indancarboxylic acid derivatives were prepared and tested for the inhibitory activities of thromboxane A2 (TXA2) production in vitro and ex
- Kanao,Watanabe,Kimura,Saegusa,Yamamoto,Kanno,Kanaya,Kubo,Ashida,Ishikawa
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p. 1326 - 1334
(2007/10/02)
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- Certain [(1-imidazolyl)-lower-alkylene]-tetrahydronaphthalenecarboxylic acids or corresponding idan-carboxylic acids which are thromboxane A2
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Benzocycloalkane derivatives of the formula (I) STR1 wherein: Z represents a methylene group or an ethylene group, either one of R1 and R2 represents --(CH2)m --COOR3 and the other represents STR2 whe
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