- A Convenient Multigram Scale Synthesis of Tetrahydrothiophene-3-one-1,1-dioxide
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A short and efficient multigram scale synthesis of tetrahydrothiophene-3-one-1,1-dioxide is described.
- Altenbach, Robert J.,Kalvoda, Ladislav,Carroll, William A.
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- Merging Halogen-Atom Transfer (XAT) and Cobalt Catalysis to Override E2-Selectivity in the Elimination of Alkyl Halides: A Mild Route towardcontra-Thermodynamic Olefins
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We report here a mechanistically distinct tactic to carry E2-type eliminations on alkyl halides. This strategy exploits the interplay of α-aminoalkyl radical-mediated halogen-atom transfer (XAT) with desaturative cobalt catalysis. The methodology is high-yielding, tolerates many functionalities, and was used to access industrially relevant materials. In contrast to thermal E2 eliminations where unsymmetrical substrates give regioisomeric mixtures, this approach enables, by fine-tuning of the electronic and steric properties of the cobalt catalyst, to obtain high olefin positional selectivity. This unprecedented mechanistic feature has allowed access tocontra-thermodynamic olefins, elusive by E2 eliminations.
- Zhao, Huaibo,McMillan, Alastair J.,Constantin, Timothée,Mykura, Rory C.,Juliá, Fabio,Leonori, Daniele
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supporting information
p. 14806 - 14813
(2021/09/18)
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- IMIDAZO [4, 5 -C] PYRIDINE DERIVATIVES USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES
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Wherein R1, L1, R3, R4, Cy, L2 and R5 are as defined herein. Novel imidazolopyridines according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic or inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons.
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Paragraph 00570
(2013/08/28)
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- Synthesis of cyclopentapyridine and thienopyridine derivatives as potential calcium channel modulators
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In this study, novel condensed 1,4-dihydropyridines bearing cyclopentanone (1-21) or tetrahydrothiophene-1,1-dioxide ring (22-42) with various ester substituents were synthesized via a modified Hantzsch reaction and their calcium channel modulator activities were investigated on isolated rat ileum and rat thoracic aorta. The introduction of a cyclopentanone ring fused to the 1,4-dihydropyridine nucleus and methyl, ethyl and allyl moieties to the ester group led to more active calcium modulators. Georg Thieme Verlag KG Stuttgart · New York.
- Guenduez,Safak,Kaygsz,Kosar,Simsek,Erol,Linden
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experimental part
p. 167 - 175
(2012/09/08)
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- Synthesis and myorelaxant activity of fused 1,4-dihydropyridines on isolated rabbit gastric fundus
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Strategy, Management and Health Policy Preclinical Research In the present study, 25 novel condensed 1,4-dihydropyridine (DHP) derivatives bearing cyclopentane, cyclohexane, or tetrahydrothiopene ring with a bulky and lipophilic moiety (3-pyridylmethyl) in the ester group were synthesized via a modified Hantzsch reaction, and their calcium channel modulator activities were assayed on isolated rabbit gastric fundus smooth muscle strips. To evaluate the myorelaxant effects of the compounds, the maximum relaxant response (Emax) and pD 2 values were calculated. The results indicated that all compounds produced concentration-dependent relaxation and the introduction of five- or six-membered rings to the DHP nucleus and 3-pyridiylmethyl moiety to the ester group led to potent calcium antagonists.
- Safak, Cihat,Guenduez, Miyase Goezde,Oezlhan, Sevil Oezger,Simasek, Rahime,Is, Fatma,Yildirim, Seniz,Fincan, Goekce Sevim Oeztuerk,Saraoglu, Yusuf,Linden, Anthony
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p. 332 - 342
(2012/10/29)
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- Pyrano, piperidino, and thiopyrano compounds and methods of use
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The present invention provides novel compounds of formula I which may be useful in hyperpolarizing cell membranes, opening potassium channels, relaxing smooth muscle cells, and inhibiting bladder contractions.
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- Pyrano, piperidino, and thiopyrano compounds and methods of use
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The present invention provides novel compounds of formula I which may be useful in hyperpolarizing cell membranes, opening potassium channels, relaxing smooth muscle cells, and inhibiting bladder contractions.
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- Synthesis of Novel Cyclic Sulfone Dihydropyridines Facilitated by a Selective Ethyl Diazoacetate Ring Expansion
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A series of novel cyclic sulfone dihydropyridines with five to nine membered rings have been synthesized.Anomalous intermediates isolated from the Hantzch condensation were found to vary depending on the sulfone ring size and aromatic substitution.Tin tetrachloride has been shown to be a superior Lewis acid catalyst for ethyl diazoacetate ring expansion of the requisite β-keto cyclic sulfone precursors.
- Dodd, John H.,Schwender, Charles F.,Gray-Nunez, Yolanda
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p. 1453 - 1456
(2007/10/02)
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- 3-OXOTETRAHYDROTHIOPHEN-1,1-DIOXIDE A VERSATILE SYNTHETIC INTERMEDIATE
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An improved preparation and valuable new reactions of 3-oxotetrahydrothiophen-1,1-dioxide are described.
- Belletire, J. L.,Spletzer, E. G.
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p. 269 - 272
(2007/10/02)
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- NEW METHODS FOR THE SYNTHESIS OF (ALKYLTHIO)DIHYDROTHIOPHENE-1,1-DIOXIDES
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The reaction of alkanethiols with 3,4-dihalotetrahydrothiophene-1,1-dioxides is a convenient method for the synthesis of 3-alkylthio-2,3-dihydrothiophene-1,1-dioxides, 3-alkylthio-2,5-dihydrothiophene-1,1-dioxides, and 3-alkylthio-4,5-dihydrothiophene-1,1
- Tolstikov, G. A.,Novitskaya, N. N.,Shul'ts, E. E.
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p. 1134 - 1141
(2007/10/02)
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- STEREOSPECIFIC SYNTHESIS OF ETHERS OF HYDROXYTETRAHYDROTHIOPHENE-1,1-DIOXIDES USING INTERPHASE CATALYSIS
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Methods have been developed for the stereospecific synthesis of O-benzyl- and O-methyl-derivatives of hydroxytetrahydrothiophene-1,1-dioxides in the presence of phase transfer catalysts.
- Tolstikov, G. A.,Novitskaya, N. N.,Shul'ts, E. E.
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p. 1129 - 1134
(2007/10/02)
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