- Synthesis of Dipyridyl Sulfides from Pyridyl-Pyridinium Halides
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Reactions of pyridyl-pyridinium halides with thiolpyridines and thiourea were investigated.New dipyridyl sulfides were obtained by this method. - Keywords: Di-(4-pyridyl)-sulfides; Pyridyl-pyridinium chlorides; Thiolpyridines; Thiourea
- Boduszek, Bogdan,Wieczorek, Jan S.
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- HALOALLYLAMINE SULFONE DERIVATIVE INHIBITORS OF LYSYL OXIDASES AND USES THEREOF
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The present invention relates to novel compounds which are capable of inhibiting certain amine oxidase enzymes. These compounds are useful for treatment of a variety of indications, e.g., fibrosis, cancer and/or angiogenesis in human subjects as well as i
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Paragraph 0319; 0320
(2020/02/23)
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- Grignard-Reagent-Promoted Desulfonylation/Intramolecular Coupling for the Synthesis of 2-(1-Fluorovinyl)pyridines
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A novel process involving Grignard-reagent-promoted desulfonylation/intramolecular coupling of readily available α-fluoro-α,β-unsaturated-(2-pyridyl)sulfones was realized that provided a series of polysubstituted 2-(1-fluorovinyl)pyridines in good yields. The intrinsic coordination between pyridine and Mg(II) along with the "negative fluorine effect"of the substrates should play the key role for the smooth transformation in the absence of transition-metal catalysts.
- Jiang, Gaoxi,Kang, Lei,Qian, Jinlong,Yang, Huameng,Zhang, Jinlong
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supporting information
p. 9118 - 9122
(2020/12/02)
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- Synthesis and characterization of 2-pyridylsulfur pentafluorides
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Current approaches to prepare SF5-substituted heterocycles during the synthesis of targeted heterocyclic compounds require the use of SF5-functionalized aryl or alkyne reagents or SF5Cl as a source of the SF5 functional group. Herein we report that excess oxidative fluorination of 2,2' -dipyridyl disulfide with a KF/Cl2 /MeCN system leads to the formation of thirteen new 2-pyridylsulfur chlorotetrafluorides (2-SF4Cl-pyridines). These molecules are found to undergo further chlorine-fluorine exchange reactions by treatment with silver(I) fluoride enabling ready access to a series of ten new substituted 2-pyridylsulfur pentafluorides (2-SF5-pyridines). This is the first preparatively simple and readily scalable example of the transformation of an existing heterocyclic sulfur functionality to prepare SF5-substituted heterocycles.
- Kanishchev, Oleksandr S.,Dolbier, William R.
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supporting information
p. 280 - 284
(2015/04/21)
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- PYRIDIN-2-YL-AMINO-1,2,4-THIADIAZOLE DERIVATIVES AS GLUCOKINASE ACTIVATORS FOR THE TREATMENT OF DIABETES MELLITUS
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Provided are compounds of Formula (I): wherein R2, R3, R13, L and D2 are as defined in the specification, which are useful in the treatment and/or prevention of diseases or disorders mediated by deficient levels of glucokinase activity or which can be treated by activating glucokinase including, but not limited to, diabetes mellitus, impaired glucose tolerance, IFG (impaired fasting glucose) and IFG (impaired fasting glycemia), as well as other diseases and disorders such as those discussed herein
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Page/Page column 97
(2009/05/29)
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- SULFONYLAMINO-ACETIC ACID DERIVATIVES
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The invention relates to novel sulfonylamino-acetic acid derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of such compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as orexin receptor antagonists.
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- Aniline derivatives
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The invention concerns aniline derivatives of formula I STR1 wherein m is 1, 2 or 3, n is 0, 1, 2 or 3, Q is phenyl or naphthyl or a 5- or 6-membered heteroaryl moiety containing 1, 2 or 3 heteroatoms selected from oxygen, nitrogen and sulfur, and X, R1 and R2 are defined in the claims; or pharmaceutical compositions containing them, and the methods of using the compounds as tyrosine kinase inhibitors and for the treatment of proliferative diseases such as cancer.
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- Azetidinone compounds useful in the preparation of carbapenem antibiotics and process for preparing carbapenem and penem compounds
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Compounds of formula (I): STR1 wherein: R1 is hydrogen or a hydroxy-protecting group; R2 is alkyl, alkoxy, halogen, optionally substituted phenyl or optionally substituted phenoxy; R3 is optionally substituted pyridyl, optionally substituted quinolyl or phenyl group which has a substituent of formula --CYNR5 R6, where Y is oxygen or sulfur, and R5 and R6 are each alkyl, aryl or aralkyl, or R5 and R6 and the nitrogen to which they are attached together form a heterocyclic group; is R4 hydrogen or an amino-protecting group; and Z is sulfur or oxygen; are valuable intermediates in the preparation of carbapenem compounds and retain a desirable configuration during conversion to such carbapenem compounds. Penem and carbapenem compounds having a group of formula --SA' are prepared from a corresponding compound having a substituted thio, sulfinyl or sulfonyl group at this position by reaction with a compound A'SH (where A' is an organic group) in the presence of a salt of a metal of Group II or III of the Periodic Table.
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- VERSATILE SYNTHESIS OF AN INTERMEDIATE FOR THE 1β-METHYLCARBAPENEM SYNTHESIS
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A 1β-methylcarboxylate (1) which is a requisite intermediate for the synthesis of the 1β-methylcarbapenem was obtained in an efficient manner by the coupling reaction of a Z(O)-pyridylthiosilyl enol ether and a 4-acetoxyazetidinone derivative in the presence of ZnCl2 in CH2Cl2.The reactive silyl enol ether was prepared by the reverse addition method in high yield.
- Hirai, Koichi,Iwano, Yuji,Mikoshiba, Isamu,Koyama, Hiroo,Nishi, Takahide
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p. 277 - 280
(2007/10/02)
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- Deoxydative Thiation of 3-Substituted Pyridine N-Oxides with 4-Methoxytoluene-α-thiol: A Divergent Route to Pyridinethiols
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Synthesis of 3-substituted 2-pyridinethiols was achieved by thiation of pyridine N-oxides with 4-methoxytoluene-α-thiol in the presence of diethylcarbamoyl chloride followed by cleavage of the resulting sulfides.The case of substitution was shown to be affected by nucleophilicity of the N-oxide oxygen.Addition of zinc bromide to the reaction, a need for triethylamine, decreased most of the yield for thiation products but the formation of 3-methoxy-2-methoxybenzylthiopyridine was only improved.A plausible mechanism of the substitution, particularly β-thiation to the N-oxide function, is discussed compared with the regiochemistry observed in the reaction with diethoxyphosphoryl chloride instead of diethylcarbamoyl chloride.The debenzylation to pyridinethiol was also found to be dependent on the electron-density in the pyridine ring.
- Sato, Nobuhiro,Nagano, Eiichi
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p. 691 - 698
(2007/10/02)
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- The Synthesis and Some Reactions of Novel Pyridine-2(1H)-thiones
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The use of methyl 3-mercaptopropionate for the conversion of halogenated pyridins to pyridine thiones and thiols is described, and limitations of the reaction discussed.S-Alkylation and oxidation reactions of the products from these reactions are reported.
- Dunn, A. D.,Norrie, R.,L'Hostis, J.,Marjot, S.
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p. 119 - 125
(2007/10/02)
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