bluuebunny/crossref_metadata_2025_split huggingface dataset:
Preparation of deuterated toluidines and xylidines
Authors: Frischkorn C. G. B. , Kohler H. , Rose B. , Unterlugauer D. , Conrad H. M. 
Published: October 2006

AbstractDeuteration in definite positions of the aromatic ring system or in the side chain of different methyl anilines is achieved in D2O under different conditions: at 150°C and pH 3 deuteration occurs in ortho/para positions; whereas at 250°C and pH 3 a total deuteration of the aromatic system takes place (overall deuteration 82–99%). Perdeuteration (81–99% in the aromatic ring, 60–99% in the side chain) is obtained in high acidic medium (pH ⩽ 1) and at 250°C. The yield of the deuterated methyl anilines is generally high (40–100%) so that this reaction is a more attractive route for preparing methyl anilines and their derivatives than the conventional ways of synthesis. By using T2O instead of D2O it should be possible to prepare the appropriate tritium‐labelled compounds.
Stereospecific introduction of tritium in the 16α or 16β position of cholesterol
Authors: Ronchetti F. , Russo G. , Longhi R. , Sportoletti G. 
Published: October 2006

AbstractReduction of cholest‐5‐en‐3β‐ol‐16‐one with KB3 H4 afforded a mix ture of [16α‐3H]‐cholest‐5‐en‐3β, 16β‐diol and [16β‐3H]‐cholest‐5‐en‐3β, 16α‐diol, which were separated and converted, respectively, into [16β‐3H]‐cholest‐5‐en‐3β‐ol and [16α‐3H]‐cholest‐5‐en‐3β‐ol.
High specific activity tritium labelled O‐benzoyl ecgonine
Authors: Muccino Richard R. , Serico Lucia 
Published: October 2006

AbstractThrough the use of an O‐(o‐iodobenzoyl) ecgonine derivative (3), tritium labelled O‐benzoyl ecgonine has been prepared, by catalytic hydrogenolysis, in sufficiently high specific activity for use in radioimmunoassay studies for cocaine metabolites. The ease of converting O‐benzoyl ecgonine to cocaine also makes this labelled substrate potentially useful in metabolism studies of the latter.
Cannabis XI. synthesis of cannabigerorcinic‐carboxyl‐14C acid, cannabigero‐varinic‐carboxyl‐14C acid, cannabidivarinic‐carboxyl‐14C acid and dl‐cannabi‐chromevarinic‐carboxyl‐14C acid
Authors: Shoyama Yukihiro , Hirano Hitotoshi , Nishioka Itsuo 
Published: October 2006

AbstractThe preparation of cannabigerorcinic‐carboxyl‐14C acid, cannabigerovarinic‐carboxyl‐14C acid, cannabidivarinic‐carboxyl‐14C acid and dl‐cannabichromevarinic‐carboxyl‐14C acid is described. The 14C‐label was introduced into the carboxyl carbon via methyl magnesium carbonate‐14C.
Synthesis of [2‐14C(U)tyrosine]arginine vasotocin with high specific radio and biological activities
Authors: Stahl Glenn L. , Walter Roderich 
Published: October 2006

AbstractThe synthesis of [2‐14C(U)tyrosine]arginine vasotocin at a specific activity of 102 mCi/mMole was performed using the solid‐phase approach of Merrifield for peptide synthesis. Following purification by gel filtrations the labeled hormone was recovered at an average yield of 40% with an avian vasodepressor activity of 408 ± 24 U/mg.
14C‐ and 2H‐labelled 7‐methylbenz[c]acridine
Authors: Cheung H. T. A. , Holder G. M. , Moldovan L. 
Published: October 2006

Abstract7‐Methylbenz[c]acridine‐7‐14C, specific activity 12.2 mCi/mmole, and deuterated 7‐methylbenz[c]acridine were prepared from acetic anhydride‐1‐14C and aceticanhydride‐2‐2H6 respectively. The deuterated compound was not specifically labelled at the 7‐methyl group because isotopic exchange of the hydrogen atoms occurred during synthesis.
Syntheses of 14C‐mustard‐labelled and 14C‐leucine‐labelled Asaley
Authors: Farquhar D. , Lu K. , Loo T. L. 
Published: October 2006

AbstractThe synthesis of Asaley labelled with 14C in the mustard (Asaley‐must‐14C) or the leucine (Asaley‐leu‐14C) moiety is described. In the former, ethyl pamino‐Nα‐acetyl‐DL‐phenylalanyl‐L‐leucinate was reacted with ethylene oxide(U)‐14C to give the bis(hydroxyethyl)amino analogue, which was converted to Asaley by treatment with thionyl chloride. Asaley labelled in the leucine moiety was prepared by condensation of N‐acetylsarcolysin with ethyl leucinate(U)‐14C in the presence of dicyclohexylcarbodiimide. The identity of the products was established by spectroscopic, chemical, and chromatographic techniques.
Synthesis of lidocaine‐d3
Authors: Hignite Charles E. , Tschanz Christian , Huffman David H. , Azarnoff Daniel L. 
Published: October 2006

AbstractA simple two step synthetic procedure has been developed for the preparation of deuterated lidocaine. The deuterium was incorporated into the 6′‐methyl group which is a metabolically stable position. The overall yield of the synthetic procedure was 41.3%.
Marquage Par 14C Du (chloro‐2 ethyl)‐3 Nitroso‐3 Ureido‐l′ O‐isopropylidene‐2′, 3′ O‐p‐nitrobenzoyl‐5′ α ET β ‐D‐ribo Furannose Ou Rfcnu
Authors: Madelmont J. C. , Moreau M. F. , Parry D. , Godeneche D. , Imbach J. L. 
Published: October 2006

AbstractRFCNU was labelled by 14C on three positions.
On the carboxyl of the para nitro benzol'c group
On urea carbonyl
On the carbone 1 of the 2, chloro éthyl group.
Synthesis of [17α, 16α] oxazolino steroids specifically labelled in C‐2′ of the oxazoline ring with 14C
Authors: Sartori Giuseppe , Winters Giorgio 
Published: October 2006

AbstractThe preparation of 14C‐labelled 11β, 21‐dihydroxy‐3,20‐dioxy‐pregna‐1,4‐dieno[ 17α, 16α‐d]‐2′‐methyloxazoline‐21‐acetate and of 9α‐fluoro‐11β,21‐dihydroxy‐3,20‐dioxopregna‐l,4‐dieno[ 17α,16α ]‐2′‐methyloxazoline‐21‐acetatelNote that [17α., 160α‐d] does not refer to deuterium labelling
is described. Specific labelling at the C‐2′ position was achieved reacting the corresponding 17α‐amino‐16α‐alcohols with [1‐14C]‐acetic anhydride.
Synthesis of DL‐[2‐14C]octan‐2‐sulphate and [35S]‐labelled D(+)‐and L(−)‐octan‐2‐sulphate
Authors: Maggs James L. , Olavesen Anthony H. , James Colin T. 
Published: October 2006

AbstractDL‐[2‐14C]Octan‐2‐sulPhate was prepared by sulphating DL‐[2‐14C]octan‐2‐ol with pyridine‐SO3 adduct. Synthesis of the DL‐[2‐14C]alkanol started with carboxylation of hexyl magnesium bromide with 14CO2. Subsequent methylation with diazomethane and reduction of the ester with lithium aluminium hydride Yieled [1‐14C]heptan‐1‐ol. The latter was oxidized to 1‐14C heptanal with Seloxcette. The [1‐14C]heptanal was reacted with methyl magnesium iodide to give DL‐[2‐14C]octan‐2‐ol. D(+)‐ and L(−)‐Octan‐2‐[35S]sulphate were synthesized by sulphating the stereochemically pure alcohols with pyridine‐35SO3 prepared from 35SO3. These synthetic routes provided specifically radiolabelled secondary alkyl sulphates of high chemical and radiochemical purity. The identity and purity of the products was confirmed by mass spectrometry, infrared spectroscopy, t.l.c. and stereospecific enzymic hydrolysis.
Synthese Du Methyl‐2 Dinitro‐4,6 Phenol (Noyau 14C‐U) (DNOC, DINOC NOYAU 14C‐U)
Authors: Noël J. P. , Pichat L. 
Published: October 2006

AbstractSYNTHESIS OF 2‐METHYL‐4,6 DINITRO PHENOL (RING U‐14C) (DNOC, DINOC ring U‐14C)O‐methoxymethylphenol (ring U‐14C) 3 Was prepared in 82 % yieltd from phenol (ring U‐14C) and methylal in presence of p‐toluene sulfonic acid and molecular sieve. Ortholithiation of 3 with n Buli + TMEDA in hexane offorded a lithioderivative 4 which was methylated with methyl iodide in ether ‐ hexane. Deprotection of phenol group lead to o ‐ cresol (ring U‐14C) : 6 purified on a silicagal column with a 52% yield based on 3. Nitration of 6 provided DNOC (ring U‐14C) with a 28% overall yield from phenol (ring U‐14C) ‐ Specific activity was: 70 mCi/mMole.
Marquage A Haute Activite Specifique Par 125I, Radiolyse Et Conservation Du 3‐5,3′‐5′, Tetraiodo‐L‐Tyrosyl‐L‐Tyrosine
Authors: Maurizis J. C. , Nicolas C. , Michelot J. 
Published: October 2006

AbstractNous décrivons le marquage ù haute activité spécifique (1.000 – 1.200 μCi/μg) par 125I, la purification et l'étude des conditions de conservation du 3‐5, 3′‐5′, tetraiodo‐1‐tyrosyl‐1‐tyrosine. Mots clés: 3‐5, 3′‐5′, tetraiodo‐1‐tyrosyl‐1‐tyrosine, iodination, conservation.
Synthese De La Beta‐naphtoflavone 14C‐4 OU 14C‐5 A Partir De L'Acide Phenylpropiolique (CARBOXYLE14C) Ou Du β‐Naphtol 14C‐8
Authors: Nam Nguyen‐Hoang , Thang Do‐Cao , Queval P. , Pichat L. 
Published: October 2006

AbstractCarbonation with 14CO2 of penylethynyl‐lithium has given rise to (carboxyl‐14C) phenylpropiolic acid with 75 % yield based on 14CO2. The latter condensed with 2‐naphthol by treating with polyphosphoric acid afforded (4‐14C) β‐naphthoflavone, purified by silicagel low pressure liquid chromatography; 22 % overall yield based on 14CO2, SA = 13 mCi/mM. Similar run of 2‐(8‐14C) naphthol with phenylpropiolic acid gave (5‐ 14C) β‐naphthoflavone; 28 % yield based on radioactive 2‐naphthol, SA = 7.2 mCi/mM.
An enzymatic method for the preparation in high yield of [5‐14C]‐ and [4,5,6‐14C] glucose
Authors: Longenecker J. P. , Williams J. F. 
Published: October 2006

Abstract[5‐14C]‐ and [4,5,6‐14C] glucose were prepared from [2‐14C]‐ and [U‐14C] glycerol and fructose 6‐phosphate by reactions involving the enzymes glycerokinase, glycerol 3‐phosphate dehydrogenase, triose phosphate isomerase, transaldolase, lactate dehydrogenase and phosphoglucose isomerase. The authenticity of each of the 14C‐labelled sugars was verified by chromatographic and enzymic procedures and the distribution of 14C isotope confirmed by specific degradative procedures. These specifically labelled substrates are required for the quantitative estimation of the new pentose pathway reactions in liver, photosynthetic and some tumour tissues.
The preparation of specifically 2H‐labeled benz[A]anthracenes and 7,12‐dimethylbenz[A]anthracenes1
Authors: Hallmark Richard K. , Manning Wayne B. , Muschik Gary M. 
Published: October 2006

AbstractThe 2 + 4 cycloaddition reaction of 1,4‐naphthoquinone and substituted styrenes was used to prepare 1‐, 2‐, 3‐, and 4‐bromobenz[a]anthracene‐7,12‐diones (BADs). The corresponding bromobenz[a]anthracenes (BAs) were prepared by aluminum tricyclohexoxide reduction of the diones. Lithiation with t‐butyllithium followed by quenching with deuterium oxide gave the specifically 2H‐labeled BAs with deuterium incorporations of >95%. The 2‐, 3‐, and 4‐bromo‐7,12‐dimethylbenz‐[a]anthracenes (DMBAs) were prepared from the bromo BADs in moderate yield by the classical Grignard procedure. Lithium aluminum deuteride reduction gave the 2H‐DMBAs. An alternate synthesis from 3,4‐dihydrobenz[a]anthracene 1‐(2H)‐one was used for the preparation of 1‐ and 2‐2H BAs and DMBAs.
1‐dehydrohexestrol. Synthesis of a precursor for the preparation of tritium‐labeled hexestrol derivatives and its use in a new, convenient synthesis of tritium‐labeled o‐azido‐hexestrol
Authors: Goswami Ramanuj , Kilbourn Michael R. , Katzenellenbogen John A. 
Published: October 2006

AbstractErthro‐1‐dehydrohexestrol (4a), an analog of the nonsteroidal estrogen meso‐hexestrol containing a double bond in the side chain, has been synthesized as a general precursor for the preparation of tritium‐labeled hexestrol derivatives. It can be functionalized further as needed, and upon catalytic hydrogenation with tritium gas, it furnishes the desired erythro or meso diastereomer of the hexestrol derivatives. Its use is exemplified in the synthesis of 3H‐o‐azidohexestrol (9c) with high specific activity.
A synthetic scheme for the preparation of carbon labelled furan compounds
Authors: Jennings Paul W. , Campbell William H. , Gingerich Samuel B. 
Published: October 2006

AbstractA facile synthesis for the efficient incorporation of 14C or 13C into trisubstituted furan compounds has been elaborated. 3‐Methyl‐4,5,6,7‐tetrahydrobenzofuran was prepared in five steps from methyl‐ and ethyl‐2‐oxo‐1 cyclohexanecarboxylate with overall yield of 65%. Radioactive label was nearly quantitatively incorporated. One new compound, 7, has been prepared in elaborating the synthetic sequence.
Syntheses du Bergaptene [0 — methyl 14C et 3H] et de la Tabernanthine [0‐methyl 14C]
Authors: Bac N. V. , Audinot M. , Pichat L. , Herbert M. , Xuong N. Dat 
Published: October 2006

Abstract{0‐methyl 14C} and {0‐methyl 3H} bergaptene were prepared by methylation of bergaptol with {14C} methyl iodide and {3H} methyl iodide in radioactive yields respectively 77 % and 59 %. {14C} methyl iodide and 11‐hydroxy ibogamine gave {0‐methyl C} tabernanthine with a 60 % radioactive yield.
Synthesis of [11C]‐3‐quinuclidinylbenzilate (QNB)
Authors: Prenant C. , Barre L. , Crouzel C. 
Published: October 2006

AbstractA method is described by which 1.11 to 1.48 GBq (30 to 40 mCi) of [11C]QNB can be obtained from approximately 55.5 GBq (1.5 Ci) of 11CO2 in 40 minutes.The product, purified by HPLC chromatogaphy, is obtained with a specific activity of 18.5 to 33.3 GBq/μmol (500 to 900 mCi/μmol).Carbon‐11 labelling is performed in two stages:
Formation of [11C]benzilic acid by carbonation by 11CO2 of the the pre‐prepared benzophenone dianion.
Esterification of [11C]benzilic acid by 3‐quinuclidinol in the presence of carbonyldiimidazole.
Synthesis of [2H5]arecoline for use as internal standard in mass spectrometric assay
Authors: Umesha Shetty H. , Soncrant Timothy T. , Greig Nigel H. , Rapoport Stanley I. 
Published: October 2006

AbstractFive deuterium atoms, three in the N‐methyl group and one each in positions 2 and 6, were incorporated into the cholinergic agonist, arecoline (1), methyl 1‐methyl‐1,2,5,6‐tetrahydropyridine‐3‐carboxylate, with 96% efficiency. Trideuterated pyridinium iodide (2) was reduced with sodium borodeuteride or sodium cyanoborodeuteride in acidic medium to yield [2H5]arecoline (3). Significantly greater deuterium incorporation occurred when 2 was reduced with sodium cyanoborodeuteride. This reduction process is discussed. The synthesized labelled compound was determined to be a suitable internal standard for mass spectrometric assays.
An efficient synthesis of 2‐ [ carbonyl‐ 11C]acetamido‐2‐deoxy‐D‐glucopyranose (N‐[carbonyl‐11C]acetyl‐D‐glucosamine)
Authors: Tada Masao , Oikawa Atsushi , Iwata Ren , Sato Kazunori , Sugiyama Hiroshi , Kubota Kazuo , Ishiwata Kiichi , Takahashi Hiromu , Wakui Akira , Abe Yoshinao , Yamaguchi Tatsuo , Fujiwara Takehiko , Sato Tachio , Ido Tatsuo 
Published: October 2006

AbstractA rapid chemical synthesis of 2‐[carbonyl‐11C]acetamido‐2‐deoxy‐D‐glucopyranose (N‐[carbonyl‐11C]acetyl‐D‐glucosamine) starting from [11C]carbon dioxide is described. The total time required for the synthesis, the radiochemical yield, and purity of the titled sugar are ca. 60 min, 49.5% (based on [carbonyl‐11C]acetic acid), and >98%, respectively.
A general procedure for isotopic (deuterium) labelling of non‐steroidal antiinflammatory 2‐arylpropionic acids
Authors: Castell José V. , Martínez Luis A. , Miranda Miguel A. , Tárrega Pilar 
Published: October 2006

AbstractAlkaline treatment of nonsteroidal antiinflammatory 2‐arylpropionic acids in deuterium oxide led in all cases to isotopic exchange of the proton located at the α‐position of the side chain. Monodeuteration was observed in the case of carprofen, ibuprofen, ketoprofen, fenoprofen, flurbiprofen and naproxen. Additional exchange of one or two protons of the heterocyclic ring occurred in indoprofen, suprofen and tiaprofenic acid. The isotopic labelling survived under the conditions required to perform in vitro photoallergic studies (photolysis in non‐deuterated aqueous media).
A novel synthesis of fumaric acid‐1‐14C
Authors: Rutner Herman , Rapun Raul 
Published: October 2006

AbstractA simple, two‐step synthesis of fumaric acid‐1‐14C from radioactive potassium cyanide and methyl 2‐chloroacrylate is described. The intermediate products, methyl cis and trans 3‐cyanoacrylates and the cis and trans 3‐cyanoacrylic acids, were hydrolyzed directly to fumaric acid‐1‐14C in 55‐60% yields. D, L‐malic acid‐COOH‐14C was also obtained as a byproduct in 9% yield. A reaction mechanism is proposed.
Synthese et purification de la 6‐furfurylaminopurine‐11‐H3 (kinetine) a haute activite specifique
Authors: Buchman O. , Milstein D. , Shimoni M. 
Published: October 2006

AbstractLa microsynthèse et la purification de la kinéine, marquée au tritium dans le group méthylène, sont décrites. L'activitéspécifique obtenue est de 2.4 Ci/mmole.
Labelling of 2‐hydroxy ‐5‐carbomethoxybenzyloxyamine hydrochloride with 14c isotope
Authors: Engler J. , Kasztreiner E. 
Published: October 2006

AbstractRadioisotopic labelling of a novel histamine level reducing and antiinflammatory agent is described. The 2‐hydroxy‐5‐carbomethoxybenzy ‐14C‐oxyamine hydrochloride was prepared for the purpose of radioisotopic indication and further for pharmacological and action mechanism studies.
Calcium homeostasis in pregnancy
Authors: Hosking D. J. 
Published: October 2006

SummaryThe demands of fetal growth lead to an adaptation of maternal homeostasis In order to provide the required calcium from enhanced intestinal absorption rather than from mobilization of maternal skeletal reserves. In large part this adaptive process depends on the interrelationship between PTH and 1,25(OH)2D which shows quantitative rather than qualitative changes from the non‐pregnant state. In contrast the maintenance of fetal mineral homeostasis largely depends on PTHrP which regulates active placental calcium transfer and the calcium fluxes across the kidney and bone. The major source of PTHrP is the fetal parathyroid gland although some is provided by the placenta. It may be this latter component which passes Into the maternal circulation where It may play a role in calcium homeostasis by acting through the PTH receptor.
Role of magnetic resonance imaging in the diagnosis and prognosis of growth hormone deficiency
Authors: Bozzola M. , Adamsbaum C. , Biscaldi I. , Zecca M. , Cisternino M. , Genovese E. , Richard I. , Kalifa G. , Chaussaln J. L. 
Published: October 2006

SummaryOBJECTIVE In patients with congenital GH deficiency (GHD), magnetic resonance Imaging (MRI) has revealed morphological abnormalities such as pituitary hypoplasia, absence of the stalk and ectopia of the posterior pituitary (PPE). Our study was aimed at investigating the possible relationship between neuroradioiogical Images and the presence of Isolated GH or multiple pituitary hormone deficiency.DESIGN We studied 121 patients, aged 0.3–25 years, with Isolated GHD (IGHD, 81 cases) or multiple pituitary hormone deficiency (MPHD, 40 cases). Of 81 IGHD patients, 50 were at prepubertal and 22 at pubertal age, while 9 had a delayed onset of puberty. Out of 40 MPHD patients, 25 were at prepubertal age and 15 at the age of puberty.RESULTS Pituitary hypoplasia, defined as a gland with a height of less than −2 SD for age, was observed more frequently in prepubertal (66%) than pubertal (18%) IGHD patients. It was also found in the majority of MPHD patients of prepubertal (76%) and pubertal age (80%), and of IGHD patients with delayed onset of puberty (100%). Mean ± SEM pituitary height was significantly lower (P < 0.001) In both prepubertal IGHD (−2.70 ± 0.20 SD) and MPHD children (−3.10 ± 0.39 SD) than in IGHD patients with normal onset of puberty (−1.55 ± 0.2 SD). A significantly greater pituitary height was observed in IGHD patients with normal onset of puberty (−1.55 ± 0.20 SD) than In MPHD patients at the age of puberty (−4.38 ± 0.61 SD, P < 0.001) and in IGHD subjects with delayed onset of puberty (−4.06 ± 0.41 SD, P < 0.001). An Important Increase (P < 0.02) in the height of the pituitary gland was found in 6 of the 9 patients with delayed puberty when they were re‐evaluated after completing their spontaneous pubertal development. The frequency of other MRI abnormalities (PPE, stalk transection) was significantly higher in MPHD patients than In IGHD patients (P < 0.001).CONCLUSION Our results confirm the usefulness of MRI In the evaluation of children affected by GH deficiency. The association of gland hypoplasia with other MR abnormalities could suggest the presence of multiple anterior pituitary deficiencies. Finally, puberty seems to play an important role in the increase of pituitary size in multiple pituitary hormone deficiency and isolated GH deficiency patients.
Uebersicht der wichtigsten Erfahrungen im Felde der Toxikologie
Authors: Witting E. , Stomeyer Fr. 
Published: October 2006

AbstractUebersicht der wichtigsten Erfahrungen im Felde der Toxikologie, besonders der chemisch‐gerichtlichen Untersuchung durch eine große Reihe eigener Beobachtungen über den Einfluß vegetabilischer und thierischer Substanzen auf metallische Gifte bereichert. Herausgegeben von Dr. B. Wittung, mit einem Vorwort von Dr. Fr. Stromeyer. 1. Band. Mit einem Kupfer. Hannover 1827. Im Verlage der Hahnschen Hofbuchhandlung.
Quantitative Trennung und Bestimmung von Arzneistoffgemischen aus der Gruppe der Analgetika/Antipyretika
Authors: Dibbern H.‐W. , Scholz G. 
Published: October 2006

AbstractMit je einem Kationen‐ und Anionenaustauscher gelingt es, durch Beladung mit verschiedenen Gegenionen bzw. durch selektive Elutionsverfahren Analgetika‐Gemischen in 5 Fraktionen quantitativ aufzutrennen. Für die Trennung von Gemischen aus 2–5 Komponenten durch Austauscher‐ und Adsorptionschromatographie werden Beispiele mitgeteilt.
Zur photometrischen Aloinbestimmung nach H. Möhrle. II. Mitt. über Methoden zur Wertbestimmung von Aloe
Authors: Böhme H. , Kreutzig L. 
Published: October 2006

AbstractDie von H. Möhrle vorgeschlagene photometrische Bestimmung von Aloin in Aloe und Aloe‐Extrakt führt zu 20–25% über dem tatsächlichen Gehalt liegenden Werten. Es gelingt, das Verfahren so abzuwandeln, daß man zu Ergebnissen kommt, die befriedigend übereinstimmen mit den durch quantitative Papier‐ und Dünnschichtchromatographie erhaltenen. In der neuen Form wird die photometrische Aloinbestimmung zur Aufnahme in das DAB 7 empfohlen.
Darstellung einiger Benzimidazol‐ und Benzthiazol‐2‐sulfonamide
Authors: Stanovnik B. , Tišler M. 
Published: October 2006

AbstractDie Darstellung verschiedener Benzimidazol‐ und Benzthiazol‐2‐sulfonamide aus Sulfonylchloriden wurde untersucht. Die Sulfonylchloride konnten durch oxydierende Chlorierung entsprechender Thione (I), Disulfide (V), Bishydroxymethyl‐Verbindungen oder Mannichbasen (IV) gewonnen werden. Die Über‐führung in die Sulfonamide (III) erfolgte auf übliche Weise. Hydroxy‐ und Aminomethylierung erfolgte beim Benzimidazolin‐2‐thion stets an beiden Stickstoff‐Atomen. Die Struktur wurde durch Überführung der Bishydroxymethyl‐Verbindung über die Bischlormethyl‐Verbindung in das bekannte 1,3‐Dimethyl‐Derivat bewiesen.
Synthese und pharmakologische Aktivität einiger Nitroindolderivate
Authors: Hiremath S. P. , Siddappa S. , Sirsi M. 
Published: October 2006

AbstractEs wurden Nitroindol‐3‐aldehyd‐thiosemicarbazone, ‐semicarbazone und Nitroindol‐2‐carbohydrazide hergestellt und ihre Wirkung auf das Wachstum von Mycobacterium tuberculosis untersucht.
Beiträge zur Chemie der 3,5‐Pyrazolidindione
Authors: Mustafa A. , Sammour A. , Kira M. , Hilmy M. K. , Anwar M. , Nakhla S. N. 
Published: October 2006

AbstractEs werden Kondensationen zwischen 1‐Phenyl‐3,5‐pyrazolidindion und Aldehyden, substituierten Benzoinen, 1,2‐ und 1,3‐Dicarbonylverbindungen beschrieben.Grignardreagenzien geben nach Reaktion mit der exocyclischen Doppelbindung der stark farbigen in 4‐Stellung methylierten 3,5‐Pyrazolidindione nach Hydrolyse farblose Produkte der wahrscheinlichen Struktur X.Blausäure, ebenso wie Thiole, ergeben nach Addition an die exocyclische Doppelbindung ebenfalls farblose Produkte: XI und XVII. Während die Einwirkung von Hydrazinen bei einer Anzahl substituierter 3,5‐Pyrazolidindione Ringöffnung bewirkt, führt sie bei anderen substituierten 3,5‐Pyrazolidindionen zu Addition an die Doppelbindung. Substituierte 3,5‐Pyrazolidindione, die an der Position 4 eine Carbonylgruppe in der Seitenkette besitzen, ergeben das Hydrazon XVI.Reaktionen zwischen heterocyclischen Verbindungen und 4‐Benzyliden‐1,2‐diphenyl‐3,5‐pyrazolidindionen führen zu XVIIIb bis c.Es wird über die Synthese des 4,4′‐Bis(1,2‐diphenyl‐3,5‐pyrazolidindion) (XVIIId) und 4,4′‐Methyliden‐bis(1‐phenyl‐ und 1,2‐diphenyl)‐3,5‐pyrazolidindion) (XIX) berichtet.