- Synthesis and neuroprotective properties of isosteric analogs of nicotine
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A method has been developed for the synthesis of isosteric analogs of nicotine involving ethers of S(-)-1-2-pyrrolidinemethanol and S(-)-1-2-pyrrolidineethanol based on the Mitsunobu reaction. The results of testing the synthesized compounds as calcium channel blockers are presented.
- Matveeva,Podrugina,Morozkin,Tkachenko,Zefirov
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- Kinetic profiling of prolinate-catalyzed α-amination of aldehydes
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Deconvolution of the role of off-cycle species from the desired catalytic cycle leads to an optimized protocol for the prolinate-catalyzed amination of aldehydes. The scope of complex reaction networks will be greatly broadened by understanding ancillary rate processes that influence the productive catalytic pathway.
- Hein, Jason E.,Armstrong, Alan,Blackmond, Donna G.
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- METHOD FOR PRODUCING AZO COMPOUNDS
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PROBLEM TO BE SOLVED: To provide a method that can produce azo compounds at good yields by making oxygen or an oxygen-containing gas act on hydrazo compounds when oxidatively dehydrogenating them. SOLUTION: Azo compounds are produced by making oxygen or an oxygen-containing gas act on hydrazo compounds in the presence of nitrite compounds, bromine compounds and a solvent. SELECTED DRAWING: None COPYRIGHT: (C)2018,JPOandINPIT
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Paragraph 0046
(2018/04/14)
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- METHOD FOR PRODUCING AZO COMPOUNDS
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PROBLEM TO BE SOLVED: To provide a method that can produce azo compounds at good yields by making oxygen or an oxygen-containing gas act on hydrazo compounds when oxidatively dehydrogenating them. SOLUTION: Azo compounds are produced by making oxygen or an oxygen-containing gas act on hydrazo compounds in the presence of at least one compound selected from the group consisting of vanadium and cerium compounds, the oxidation reaction to be performed without using a solvent. SELECTED DRAWING: None COPYRIGHT: (C)2018,JPOandINPIT
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Paragraph 0050; 0051
(2018/08/22)
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- METHOD FOR PRODUCING AZO COMPOUNDS
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PROBLEM TO BE SOLVED: To provide a method that can produce azo compounds at good yields by making oxygen or an oxygen-containing gas act on hydrazo groups of hydrazo compounds when oxidatively dehydrogenating them. SOLUTION: Azo compounds are produced by making oxygen or an oxygen-containing gas act on hydrazo compounds in the presence of vanadium or cerium compounds, and a solvent. SELECTED DRAWING: None COPYRIGHT: (C)2018,JPOandINPIT
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Paragraph 0048; 0062
(2018/05/03)
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- Photocatalytic esterification under Mitsunobu reaction conditions mediated by flavin and visible light
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The usefulness of flavin-based aerial photooxidation in esterification under Mitsunobu reaction conditions was demonstrated, providing aerial dialkyl azodicarboxylate recycling/generation from the corresponding dialkyl hydrazine dicarboxylate. Simultaneously, activation of triphenylphosphine (Ph3P) by photoinduced electron transfer from flavin allows azo-reagent-free esterification. An optimized system with 3-methylriboflavin tetraacetate (10%), oxygen (terminal oxidant), visible light (450 nm), Ph3P, and dialkyl hydrazine dicarboxylate (10%) has been shown to provide efficient and stereoselective coupling of various alcohols and acids to esters with retention of configuration.
- M?rz,Chudoba,Kohout,Cibulka
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supporting information
p. 1970 - 1975
(2017/03/11)
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- PROCESSES FOR THE PREPARATION OF HIGHLY PURE PRUCALOPRIDE SUCCINATE AND ITS INTERMEDIATES
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Provided herein are purification processes for the preparation of highly pure prucalopride succinate salt. Provided also herein are improved, commercially viable and industrially advantageous processes for the preparation of Prucalopride and its intermediate compounds, for example, methyl 4-acetylamino-5-chloro-2,3-dihydrobenzo[b]furan-7-carboxylate and alkyl 4-[[(4-amino-5-chloro-2,3-dihydro-7-benzofuranyl)carbonyl]-amino]-1-piperidinecarboxylate.
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Page/Page column 24; 25
(2017/09/05)
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- Method of manufacturing Azodicarboxylic acid diester compd. (by machine translation)
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PROBLEM TO BE SOLVED: To provide a manufacturing method in which an azodicarboxylate diester compound can be efficiently obtained in a high yield and which is industrially advantageous.SOLUTION: There is provided a manufacturing method for azodicarboxylate diester compound including: a process (a) of obtaining a 1,2-hydrazine dicarboxylate diester compound through reaction between hydrazine and a halocarbonate ester; and a process (b) of obtaining an azodicarboxylate diester compound represented by general formula (2) (where A represents a hydrocarbon or a hydrocarbon which may have an ether bond) by oxidizing the 1,2-hydrazine dicarboxylate diester compound obtained in the process (a), the 1,2-hydrazine dicarboxylate diester compound being neither isolated nor refined.
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Paragraph 0026-0028
(2017/04/28)
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- Cu-Catalyzed Aerobic Oxidation of Di-tert-butyl Hydrazodicarboxylate to Di-tert-butyl Azodicarboxylate and Its Application on Dehydrogenation of 1,2,3,4-Tetrahydroquinolines under Mild Conditions
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A new class of co-catalytic system was developed with homogeneous CuI and di-tert-butyl azodicarboxylate for aerobic dehydrogenation of 1,2,3,4-tetrahydroquinolines under mild conditions. The developed co-catalytic system is consisting of di-tert-butyl azodicarboxylate-mediated dehydrogenation of 1,2,3,4-tetrahydroquinoline and aerobic oxidative regeneration of di-tert-butyl azodicarboxylate from di-tert-butyl hydrazodicarboxylate using molecular oxygen as a terminal oxidant. A variety of quinolines were efficiently synthesized by the developed Cu and di-tert-butyl azodicarboxylate co-catalytic system.
- Jung, Dahyeon,Kim, Min Hye,Kim, Jinho
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supporting information
p. 6300 - 6303
(2016/12/23)
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- Macroporous polystyrene-supported (diacetoxyiodo)benzene: An efficient heterogeneous oxidizing reagent
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A heterogeneous, cross-linked macroporous polystyrene-supported (diacetoxyiodo) benzene reagent has been prepared. This reagent is completely insoluble in all solvents and has a rigid pore structure that allows it to function without the need for swelling. Its utility in a variety of oxidation reactions has been demonstrated. Georg Thieme Verlag Stuttgart.
- Shang, Yongjia,But, Tracy Yuen Sze,Togo, Hideo,Toy, Patrick H.
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- Acetylenic α-amino acid-based sulfonamide hydroxamic acid tace inhibitors
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Compounds of the formula: are useful in treating disease conditions mediated by TNF-α, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.
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- 4-substituted piperidine analogs and their use as subtype selective NMDA receptor antagonists
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PCT No. PCT/US96/20872 Sec. 371 Date Sep. 16, 1998 Sec. 102(e) Date Sep. 16, 1998 PCT Filed Dec. 20, 1996 PCT Pub. No. WO97/23216 PCT Pub. Date Jul. 3, 1997Novel 4-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 4-substituted piperidine analogs are selective active antagonists of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions such as stroke, cerebral ischemia, central nervous system trauma, hypoglycemia, psychosis, anxiety, migraine headaches, glaucoma, CMV retinitis, aminoglycoside antibiotics-induced hearing loss, convulsions, chronic pain, opioid tolerance or withdrawal, urinary incontinence or neurodegenerative disorders, such as lathyrism, Alzheimer's Disease, Parkinsonism and Huntington's Disease are described.
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- Liquid crystal materials, mixtures and devices
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Liquid crystal compounds of formula I may be used by themselves or they may be mixed with other liquid crystal compounds to give useful liquid crystal mixtures which may then be used in liquid crystal devices. The materials exhibit smectic mesophases and may therefore be used in ferroelectric, ferrielectric, antiferroelectric, themochromic and electroclinic devices. They may also be used as long pitch materials.
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- HYDROXAMIC ACID AND CARBOXYLIC ACID DERIVATIVES, PROCESS FOR THEIR PREPARATION AND USE THEREOF
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This disclosure relates to a novel class of hydroxamic and carboxylic acid based matrix metalloproteinase inhibitor derivatives. The disclosure further relates to pharmaceutical compositions containing such compounds and to the use of such compounds and compositions in the treatment of matrix metalloproteinase induced diseases.
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- AZABENZIMIDAZOLES IN THE TREATMENT OF ASTHMA, ARTHRITIS AND RELATED DISEASES
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A series of imidazo[4,5-c]pyridines which inhibit platelet activating factor (PAF) and also block leukotriene D4 receptors are useful in treating asthma, arthritis, psoriasis, gastrointestinal distress, myocardial infarction, stroke and shock.
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- Alkylation of azaglycine derivatives
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A process for the preparation of alkylated azaglycine derivatives of the formula I is described in which X is an amino protective group, C1 -C8 -alkanoyl, C6 -C14 -arylcarbonyl or C6 -C14 -aryl-C1 -C4 -alkanoyl, A is amino acid or imino acid radicals optionally protected on the third function, n is 0-10, X being C1 -C8 -alkanoyl, C6 -C14 -arylcarbonyl or C6 -C14 -aryl-C1 -C4 -alkanoyl if n=0, and R is C1 -C8 -alkyl, C6 -C14 -aryl-C1 -C4 -alkanoyl or C5 -C12 -heteroaryl-C1 -C4 -alkanoyl, which comprises reacting a compound of the formula X--(A)n --NH--NH--CO--NH2, in which X, A and n have the abovementioned meanings, with a primary or secondary alcohol and excess DEAD, and a tri-C1 -C6 -alkylphosphine, tri-C6 -C14 -arylphosphine or pyridyl-di-C6 -C14 -arylphosphine, it being possible for the aryl moiety to be optionally substituted by di-C1 -C4 -alkylamino, in an ether at 0° C. to 30° C. and optionally removing the amino protective group X, with the proviso that X is not Fmoc when tri-n-butylphosphine is used.
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- Benzothiazepines
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A compound selected from the group consisting of all possible isomeric forms, racemic or optically active of a compound of the formula STR1 wherein the substituents are defined in the specification, and their non-toxic, pharmaceutically acceptable acid addition salts having antiarhythmic activity.
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- SYNTHESIS OF AZOBIS(FORMAMIDOACETIC ACID) AND SOME OF ITS DERIVATIVES
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Synthesis of azobis(formamidoacetic acid) (AFA acid) by the condensation of diethyl azodicarboxylate with glycine is described.By treatment with PCl5 and acetyl chloride the AFA acid chloride is obtained, which gives the corresponding amide in ammonia solution.
- Simonescu, Cristofor I.,Comanita, Eugenia,Pastravanu, Mariana,Comanita, Bogdan
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- AN IMPROVED SYNTHESIS OF ETHYL AZODICARBOXYLATE AND 1,2,4-TRIAZOLINE-3,5-DIONES USING HYPERVALENT IODINE OXIDATION
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Hypervalent iodine oxidation of 1,2-dicarbethoxy hydrazine (1) and 4-substituted urazoles (3) using iodobenzene diacetate or pentafluoroiodobenzene bis-trifluoroacetate in CH2Cl2 at room temperature proceeds smoothly to yield ethyl azodicarboxylate (2) and 4-substituted 1,2,4-triazoline-3,5-diones (4) in excellent yields.
- Moriarty, Robert M.,Prakash, Indra,Penmasta, Raju
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p. 409 - 414
(2007/10/02)
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- Attempts to Synthesize Derivatives of the 2,3-Diazabicycloocta-5,7-diene System
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The 2,3-diazabicycloocta-5,7-diene derivatives 1a and b could neither be obtained by a photoaromatization reaction of 8 nor by an electrolytic oxidation of the dicarboxylic acids 13a,b.Cycloadditions to 21 lead to derivatives of the title system.At temperatures above -10 deg C these undergo a -cycloreversion to produce the tetrahydrophthalazines 22.The thermal transformation of 21 to 22 is rationalized on the basis of a chain mechanism.
- Askani, Rainer,Schneider, Wilfried
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p. 2355 - 2365
(2007/10/02)
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