- Practical synthesis of (1 s,4 s)-4-(methylamino)-1′ H-spiro[cyclohexane-1,3′-furo[3,4-c]pyridin]-1′-one
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A practical and scalable process for the preparation of (1s,4s)-4-(methylamino)-1′H-spiro[cyclohexane-1,3′-furo[3,4-c] pyridin]-1′-one 2a, a highly functionalized and potentially useful building block for pharmaceutical research is described. The material
- Bish, Gerwyn,De Koning, Pieter D.,Dubant, Stephane P. A.,Fengas, David,Fray, M. Jonathan
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Read Online
- Diverse, Potent, and Efficacious Inhibitors That Target the EED Subunit of the Polycomb Repressive Complex 2 Methyltransferase
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Aberrant activity of the histone methyltransferase polycomb repressive complex 2 (PRC2) has been linked to several cancers, with small-molecule inhibitors of the catalytic subunit of the PRC2 enhancer of zeste homologue 2 (EZH2) being recently approved fo
- Bagal, Sharan K.,Barton, Peter,Bloecher, Andrew,Borodovsky, Alexandra,Code, Erin,Fillery, Shaun M.,Gregson, Clare,Hsu, Jessie Hao-Ru,Kawatkar, Sameer P.,Li, Chengzhi,Longmire, David,Nai, Youfeng,Nash, Samuel C.,O' Donovan, Daniel H.,Pike, Andrew,Pike, Kurt G.,Rawlins, Phillip B.,Read, Jon A.,Robinson, James,Shen, Minhui,Tang, Jia,Wang, Peng,Williamson, Beth,Woods, Haley
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p. 17146 - 17183
(2021/12/06)
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- Designing Metallogelators Derived from NSAID-based Zn(II) Coordination Complexes for Drug-Delivery Applications
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A crystal engineering approach has been invoked to design a new series of eight Zn(II) coordination complexes derived from various non-steroidal anti-inflammatory drugs (NSAIDs), namely diclofenac (DIC), ibuprofen (IBU), naproxen (NAP), flufenamic acid (FLU) and meclofenamic acid (MEC), and two co-ligands, namely N-phenyl-3-pyridylamide (3-Py) and N-phenyl-4-pyridylamide (4-Py), and Zn(NO3)2 as potential supramolecular gelators. Half of the coordination complexes thus synthesized were able to form aqueous gels (MG-3-PyMEC, MG-3-PyDIC, MG-4-PyNAP and MG-4-PyMEC). Single-crystal structures of all eight complexes revealed that they possessed a gelation-inducing 1D hydrogen-bonded network including amide…amide synthon in some cases, which supported strongly the design principles based on which these complexes were synthesized. Interestingly, one such metallogelator complex, namely 3-PyMEC, showed an intriguing anticancer property against a human breast cancer cell line (MDA-MB-231), as revealed by both MTT and cell migration assays.
- Mondal, Swapneswar,Dastidar, Parthasarathi
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p. 3558 - 3567
(2020/09/23)
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- Clickable coupling of carboxylic acids and amines at room temperature mediated by SO2F2: A significant breakthrough for the construction of amides and peptide linkages
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The construction of amide bonds and peptide linkages is one of the most fundamental transformations in all life processes and organic synthesis. The synthesis of structurally ubiquitous amide motifs is essential in the assembly of numerous important molecules such as peptides, proteins, alkaloids, pharmaceutical agents, polymers, ligands and agrochemicals. A method of SO2F2-mediated direct clickable coupling of carboxylic acids with amines was developed for the synthesis of a broad scope of amides in a simple, mild, highly efficient, robust and practical manner (>110 examples, >90% yields in most cases). The direct click reactions of acids and amines on a gram scale are also demonstrated using an extremely easy work-up and purification process of washing with 1 M aqueous HCl to provide the desired amides in greater than 99% purity and excellent yields.
- Wang, Shi-Meng,Zhao, Chuang,Zhang, Xu,Qin, Hua-Li
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p. 4087 - 4101
(2019/04/30)
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- Synthesis of N -Aryl Amides by Ligand-Free Copper-Catalyzed ipso -Amidation of Arylboronic Acids with Nitriles
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A facile copper-catalyzed ipso-amidation of arylboronic acids with nitriles has been developed. The method provides a highly efficient and economical synthesis of N-aryl amides with a broad substrate scope.
- Qiao, Yan,Li, Gaoqiang,Liu, Sha,Yangkai, Yujie,Tu, Jingxuan,Xu, Feng
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supporting information
p. 1834 - 1838
(2017/04/06)
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- AZA-A-RING INDENOISOQUINOLINE TOPOISOMERASE I POISONS
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The invention described herein pertains to four series of aza-A-ring indenoisoquinolines, which are inhibitors of topoisomerase IB (Top1), and the processes for preparing said aza-A-ring indenoisoquinolines. Also described are methods for treating cancer
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Paragraph 00105; 00125
(2017/10/13)
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- Manganese-catalyzed directed methylation of C(sp2)-H bonds at 25 °C with high catalytic turnover
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We report here a manganese-catalyzed C-H methylation reaction of considerable substrate scope, using MeMgBr, a catalytic amount of MnCl2· 2LiCl, and an organic dihalide oxidant. The reaction features ambient temperature, low catalyst loading, typically 1%, high catalytic turnover reaching 5.9 × 103, and no need for an extraneous ligand and illustrates a unique catalytic use of simple manganese salts for C-H activation, which so far has relied on catalysis by manganese carbonyls.
- Sato, Takenari,Yoshida, Takumi,Al Mamari, Hamad H.,Ilies, Laurean,Nakamura, Eiichi
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supporting information
p. 5458 - 5461
(2017/11/06)
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- Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 2. Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives
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Following the discovery of cell penetrant pyridine-4-carboxylate inhibitors of the KDM4 (JMJD2) and KDM5 (JARID1) families of histone lysine demethylases (e.g., 1), further optimization led to the identification of non-carboxylate inhibitors derived from pyrido[3,4-d]pyrimidin-4(3H)-one. A number of exemplars such as compound 41 possess interesting activity profiles in KDM4C and KDM5C biochemical and target-specific, cellular mechanistic assays.
- Westaway, Susan M.,Preston, Alex G. S.,Barker, Michael D.,Brown, Fiona,Brown, Jack A.,Campbell, Matthew,Chung, Chun-Wa,Drewes, Gerard,Eagle, Robert,Garton, Neil,Gordon, Laurie,Haslam, Carl,Hayhow, Thomas G.,Humphreys, Philip G.,Joberty, Gerard,Katso, Roy,Kruidenier, Laurens,Leveridge, Melanie,Pemberton, Michelle,Rioja, Inma,Seal, Gail A.,Shipley, Tracy,Singh, Onkar,Suckling, Colin J.,Taylor, Joanna,Thomas, Pamela,Wilson, David M.,Lee, Kevin,Prinjha, Rab K.
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p. 1370 - 1387
(2016/03/05)
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- Amine Activation: Synthesis of N-(Hetero)arylamides from Isothioureas and Carboxylic Acids
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A novel method for N-(hetero)arylamide synthesis based on rarely explored amine activation, rather than classical acid activation, is reported. The activated amines are easily prepared using a three-component reaction with commercial reagents. The new method shows a broad scope including challenging amides not (efficiently) accessible via classical protocols.
- Zhu, Yan-Ping,Sergeyev, Sergey,Franck, Philippe,Orru, Romano V. A.,Maes, Bert U. W.
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supporting information
p. 4602 - 4605
(2016/09/28)
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- Investigation of the Structure-Activity Relationships of Aza-A-Ring Indenoisoquinoline Topoisomerase i Poisons
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Several indenoisoquinolines have shown promise as anticancer agents in clinical trials. Incorporation of a nitrogen atom into the indenoisoquinoline scaffold offers the possibility of favorably modulating ligand-binding site interactions, physicochemical properties, and biological activities. Four series of aza-A-ring indenoisoquinolines were synthesized in which the nitrogen atom was systematically rotated through positions 1, 2, 3, and 4. The resulting compounds were tested to establish the optimal nitrogen position for topoisomerase IB (Top1) enzyme poisoning activity and cytotoxicity to human cancer cells. The 4-aza compounds were the most likely to yield derivatives with high Top1 inhibitory activity. However, the relationship between structure and cytotoxicity was more complicated since the potency was influenced strongly by the side chains on the lactam nitrogen. The most cytotoxic azaindenoisoquinolines 45 and 46 had nitrogen in the 2- or 3-positions and a 3′-dimethylaminopropyl side chain, and they had MGM GI50 values that were slightly better than the corresponding indenoisoquinoline 64.
- Beck, Daniel E.,Reddy, P. V. Narasimha,Lv, Wei,Abdelmalak, Monica,Tender, Gabrielle S.,Lopez, Sophia,Agama, Keli,Marchand, Christophe,Pommier, Yves,Cushman, Mark
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p. 3840 - 3853
(2016/05/24)
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- H-β-zeolite catalyzed transamidation of carboxamides, phthalimide, formamides and thioamides with amines under neat conditions
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Efficient transamidation of unactivated carboxamides, phthalimides, formamides and thioamides with amines under solvent-free conditions using H-β-zeolite as a green and recyclable heterogeneous catalyst is described. Easy work up, high purity of the products, recyclability and environmentally-friendly nature of the catalyst are the attractive features of the present methodology. This is the first report for the transamidation of thioamides under heterogeneous conditions.
- Rao, Sadu Nageswara,Chandra Mohan, Darapaneni,Adimurthy, Subbarayappa
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p. 95313 - 95317
(2015/11/24)
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- 1,2,3,9b-Tetrahydro-5H-imidazo[2,1-a]isoindol-5-ones as a new class of respiratory syncytial virus (RSV) fusion inhibitors. Part 2: Identification of BTA9881 as a preclinical candidate
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Respiratory syncytial virus (RSV) is a major cause of respiratory tract infections in infants, young children and adults. 1,2,3,9b-Tetrahydro-5H-imidazo[2,1-a]isoindol-5-ones with general structure 1 were previously identified as promising inhibitors of RSV targeting the fusion glycoprotein. In particular, the introduction of a nitrogen at the 8-position of the tricyclic core yielded lead compounds 2 and 3. Extensive exploration of the R2 group established that certain heterocyclic amides conferred potent RSV A&B activity and a good balance of physicochemical and pharmacokinetic properties. The antiviral activity was found to reside in a single enantiomer and compound 33a, (9bS)-9b-(4-chlorophenyl)-1-(pyridin-3-ylcarbonyl)-1,2,3,9b-tetrahydro-5H-imidazo[1′,2′:1,2]pyrrolo[3,4-c]pyridin-5-one (known as BTA9881), was identified as a candidate for preclinical development.
- Bond, Silas,Draffan, Alistair G.,Fenner, Jennifer E.,Lambert, John,Lim, Chin Yu,Lin, Bo,Luttick, Angela,Mitchell, Jeffrey P.,Morton, Craig J.,Nearn, Roland H.,Sanford, Vanessa,Anderson, Kelly H.,Mayes, Penelope A.,Tucker, Simon P.
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p. 976 - 981
(2015/02/19)
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- Effective nitration of anilides and acrylamides by tert-butyl nitrite
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Nitro compounds are important intermediates in synthetic organic chemistry and the chemical industry. Herein, the efficient copper-catalyzed [10% Cu(NO3)2·3H2O] nitration of anilides was developed by using TBN (tert-butyl nitrite) as a nitrating reagent to give the corresponding nitro-substituted aromatic products in good to excellent yields. The use of TBN also led to the selective nitration of acrylamides at room temperature to afford only the (E) isomer of the nitration product. A series of anilides and acrylamides with a broad array of functional groups were well-tolerated by this procedure. This synthetic method has many advantages, which include inexpensive starting materials, mild reaction conditions, a fast reaction rate, and high yields. A mechanistic investigation indicates that a nitro radical, which is generated from the thermal homolysis of TBN, is involved in the two nitration processes. The efficient nitration of both anilides and acrylamides was achieved by using TBN (tert-butyl nitrite) as a metal-free nitrating reagent. This synthetic method has many advantages such as mild reaction conditions, a fast reaction rate, good to excellent yields, and a broad substrate scope. Our investigation indicates that a nitro radical is involved in the reaction mechanism.
- Ji, Yi-Fei,Yan, Hong,Jiang, Qi-Bai
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p. 2051 - 2060
(2015/03/18)
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- Pyridyl-decorated self-folding heptaamide cavitands as ligands in the rhodium-catalyzed hydrogenation of norbornadiene
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The different binding geometries exhibited in solution by the Rh I cationic complexes of three regioisomeric self-folding heptaamide cavitands, each decorated with one pyridyl group at the upper rim, are taken into account to explain the diverse distributions of products obtained when these complexes are employed as catalysts for the hydrogenation of norbornadiene. Copyright
- Korom, Sasa,Ballester, Pablo
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p. 4276 - 4282
(2014/07/21)
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- Rh(III)-catalyzed cascade oxidative olefination/cyclization of picolinamides and alkenes via C-H activation
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Rh(III)-catalyzed cascade oxidative alkenylation/cyclization of picolinamides and alkenes to furnish pyrido pyrrolone derivatives is described, in which three C-H bonds and one N-H bond broke, while one C-C bond and one C-N bond formed. The reaction proceeded with high yield and high regioselectivity and stereoselectivity. Moreover, copper acetate can also be used in catalytic amounts with O2 serving as the terminal oxidant.
- Cai, Shangjun,Chen, Chao,Shao, Peng,Xi, Chanjuan
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supporting information
p. 3142 - 3145
(2014/06/23)
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- Tert-butoxide-assisted amidation of esters under green conditions
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Efficient and green amidation reactions are of great importance. In this work, we demonstrate the tert-butoxide-assisted amidation of esters with amines under ambient conditions. Aliphatic and/or aromatic esters were converted into the corresponding amides under mild conditions in good to excellent yields. It is noteworthy that the reaction is highly efficient, rapid, versatile, green and economical, and will find great practical application in organic synthesis, biochemistry, and industrial chemistry. Georg Thieme Verlag Stuttgart. New York.
- Kim, Bo Ram,Lee, Hyung-Geun,Kang, Seung-Beom,Sung, Gi Hyeon,Kim, Jeum-Jong,Park, Jong Keun,Lee, Sang-Gyeong,Yoon, Yong-Jin
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experimental part
p. 42 - 50
(2012/03/26)
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- Efficient amide formation from arylamines and esters promoted by AlCl 3/Et3N: An experimental and computational investigation
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Efficient and selective preparation of amides from arylamines and esters has been achieved with an AlCl3/Et3N pair under mild conditions. A large number of arylamines were successfully acylated to the corresponding amides in high yields and short reaction times. For instance, a 94% yield of p-bromoacetanilide was obtained from p-bromoaniline and ethyl acetate in 10 min at room temperature. In addition, a computational study on the N-acylation of amines was performed using density functional theory. It was found that the energy barrier for N-acylation of aniline is 10 kcal/mol higher than that of methylamine. In the presence of AlCl3, the activation energy for the N-acylation of aniline was reduced by 27.7 kcal/mol with the endothermic process becoming exothermic. Springer Science+Business Media B.V. 2012.
- Tong, Xinli,Ren, Zhangshun,Que, Xiaolong,Yang, Qiwu,Zhang, Wenqin
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p. 1961 - 1968
(2013/02/22)
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- Nano-sulfated titania (TiO2/SO2-4) as a new solid acid catalyst for Friedel-Crafts acylation and Beckman rearrangement in solvent-free conditions
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The present work describes a novel application of nano-sulfated titania (nano-ST) as a solid acid catalyst for Friedel-Crafts acylation and Beckmann rearrangement. A nano-ST catalyst has been synthesized and characterized using various techniques such as XRD, scanning electron morphology, transmission electron microscopy, FT-IR, measurement of the specific surface area by Brunauer-Emmett-Teller theory and thermal analysis. The influences of various reaction parameters such as reaction temperature, molar ratio of reactants, reaction time and solvent effects have been investigated. [image omitted].
- Hosseini-Sarvari, Mona,Safary, Ensieh
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experimental part
p. 463 - 473
(2012/06/16)
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- Pd0/PR3-catalyzed arylation of nicotinic and isonicotinic acid derivatives
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(Chemical Eqation Presented) Good for your health: Intermolecular C-H functionalization of pyridine rings at the 3- and 4-positions is described using a Pd0/PR3/ArBr catalytic system. This reaction provides a powerful method for the preparation of structurally diverse nicotinic and isonicotinic acids that are of great importance in drug discovery.
- Wasa, Masayuki,Worrell, Brady T.,Yu, Jin-Quan
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experimental part
p. 1275 - 1277
(2010/05/02)
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- Pyridinium cationic-dimer antimalarials, unlike chloroquine, act selectively between the schizont stage and the ring stage of Plasmodium falciparum
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Malaria is a leading cause of death in developing countries, and the emergence of strains resistant to the main therapeutic agent, chloroquine, has become a serious problem. We have developed cationic-dimer type antimalarials, MAP-610 and PMAP-H10, which
- Yoshikawa, Mai,Motoshima, Kazunori,Fujimoto, Kanji,Tai, Akihiro,Kakuta, Hiroki,Sasaki, Kenji
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p. 6027 - 6033
(2008/12/22)
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- PIPERIDINE COMPOUND AND PROCESS FOR PREPARING THE SAME
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The present invention is to provide a piperidine compound represented by the formula [I]: wherein Ring A is an optionally substituted benzene ring, Ring B is an optionally substituted benzene ring, R1 is hydrogen atom or a substituent for amino
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Page/Page column 73; 132
(2008/06/13)
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- Behaviour of N-pyridylbenzamides versus benzanilides in the ortho-directed lithiation of masked aromatic carboxylic acids
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The reaction of N-pyridylbenzamides 1-3 with n-butyllithium or sec-butyllithium has been examined. The perfect selectivity that has been observed until now in the lithiation of anilides, a reaction used for ortho-functionalisation of masked aromatic carboxylic acids, has been broken; our results indicate that the pyridine ring at the position ortho to the directed metallation group is more susceptible to lithiation than the homoaromatic ring itself. This was proved in an intermolecular comparative study of benz-, picolin- and isonicotinanilides 14-16, and N-cumylbenzamide (17). Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2004.
- Jozwiak, Andrzej,Brzezinski, Jacek Z.,Plotka, Mieczyslaw W.,Szczesniak, Aleksandra K.,Malinowski, Zbigniew,Epsztajn, Jan
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p. 3254 - 3261
(2007/10/03)
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- α-nitrogen activating effect in the room temperature copper-promoted N-arylation of heteroarylcarboxamides with phenyl siloxane or p-toluylboronic acid
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Heteroarylcarboxamides containing α-nitrogens undergo copper-promoted N-phenylation with hypervalent phenyl trimethylsiloxane at room temperature, in the absence of base and in air. Arylboronic acid can substitute for phenyl trimethylsiloxane as the organ
- Lam, Patrick Y.S.,Deudon, Sophie,Hauptman, Elisabeth,Clark, Charles G.
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p. 2427 - 2429
(2007/10/03)
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- Synthesis of 2-pyridinylbenzoxazole: Mechanism for the intramolecular photosubstitution of the haloarene with the carbonyl oxygen of the amide bond in basic medium
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2-Pyridinylbenzoxazole derivatives have been synthesized by the intramolecular photosubstitution reaction of N-(2- halophenyl)pyridinecarboxamide (1 and 2) with its amide bond in basic medium. In neutral medium both intramolecular photosubstitution and photoreduction reactions occurred. In the photosubstitution reaction a singlet state of the o-haloarene is involved, whereas in the photoreduction a triplet state of the o-haloarene is involved; oxygen inhibited the photoreduction but not the photosubstitution. The relative rate studies showed that a base accelerates the photosubstitution reaction but decelerates the photoreduction. o- Iodoarenecarboxamide is more reactive than o-bromoarenecarboxamide, which in turn is more reacitive than o-chloroarenecarboxamide. UV-vis absorption change in the presence of a base showed that an imidol and/or imidolate anion is involved in the reaction. Several transient species, such as charge- transfer excited states and a cyclohexadienyl anion radical, have been identified from the photolysis of 1 and 2 in basic medium by laser flash photolysis. In neutral medium dibromide anion radical and a phenyl radical were identified in addition to the above intermediates. On the basis of the photokinetic and laser flash photolysis studies, an intramolecular photosubstitution of N-(o-halophenyl)pyridinecarboxamide with its amide bond occurs via an intramolecular S(N)(ET)Ar* mechanism to afford 2- pyridinylbenzoxazole derivative, and the photoreduction proceeds via a free radical mechanism to give N-phenylpyridinecarboxamide.
- Park, Yong-Tae,Jung, Chang-Hee,Kim, Kwang-Wook,Kim, Ho Sik
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p. 8546 - 8556
(2007/10/03)
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- HIV protease inhibitors
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HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.
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- HIV protease inhibitors
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HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.
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- Intermediate and process for making
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The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection and/or AIDS.
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- APPLICATION OF ORGANOLITHIUM AND RELATED REAGENTS IN SYNTHESIS. PART 7. SYNTHESIS AND METALLATION OF 4-METHOXYPICOLIN- AND 2-METHOXYISONICOTIN-ANILIDES. A USEFUL METHOD FOR PREPARATION OF 2,3,4-TRISUBSTITUTED PYRIDINES
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The synthesis and metallation of 4-methoxypicolin- and 2-methoxyisonicotin-anilides as a way of regiospecific transformation of picolinic and isonicotinic acids into 2,3,4-trisubstituted pyridines, is described.The resulted C-alkylated derivatives underwent smooth acid - catalysed conversion into the corresponding pyridones.
- Epsztajn, Jan,Bieniek, Adam,Plotka, Mieczyslaw W.,Suwald, Krzysztof
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p. 7469 - 7476
(2007/10/02)
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- 2,4-Diamino-6,7-dimethoxyquinazolines. 2. 2-(4-Carbamoylpiperidino) Derivatives as α1-Adrenoceptor Antagonists and Antihypertensive Agents
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A series of 4-amino-2-(4-carbamoylpiperidino)-6,7-dimethoxyquinazolines (2) were synthesized and evaluated for α-adrenoceptor affinity and antihypertensive activity.These compounds displayed high binding affinity (Ki, 10-9-10-10
- Alabaster, Valerie A.,Campbell, Simon F.,Danilewicz, John C.,Greengrass, Colin W.,Plews, Rhona M.
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p. 999 - 1003
(2007/10/02)
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- APPLICATIONS of ORGANOLITHIUM and RELATED REAGENTS in SYNTHESIS. Part V. Directed Metallation of Secondary Picolin- and Isonicotinamides. A Useful Method for the Synthesis of 2,3- and 3,4-Disubstituted Pyridines, Including Furopyridin-3(1H)-one and Furopyridine-1(3H)-one
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The metallation reaction of N-methyl-, N-benzyl- and N-phenyl-amides (1a-c) and (2a-c) derived from picolinic and isonicotinic acids by BunLi in THF leading to the corresponding bis(N- and 3-)lithiated amides (3a-c) and (4a-c), are described.The N-phenylamides (anilides) (1c) and (2c), in comparison with the other aliphatic derivatives, demonstrate greater abilities to direct ortho lithiation at the 3-position of the pyridine ring, and give with very good yields bis(N- and 3-)lithiated anilides (3c) and (4c), respectively.The N-benzylamides (1b) and (2b) are ortho metallated under kinetic control at -78 deg C to form the bis(N- and 3-)lithiated benzylamides (3b) and (4b), but the organometallic intermediates rearrange at room temperature to give the thermodynamically more stable bis(N- and α-)lithiated amides (3g) and (4g) (benzyl-type anions).The generated carbanions (3c), (4c), (3g) and (4g) were trapped by a variety of electrophiles (e.g. alkyl halides and aldehydes).The synthesis of furopyridin-3(1H)-one (18) and furopyridin-(3H)-one (19) is included.
- Epsztajn, Jan,Bieniek, Adam,Plotka, Mieczyslaw W.
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p. 442 - 474
(2007/10/02)
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- Derivatives of 1,3,5-Triazine: Part III - Cyanuric Chloride-Dimethylformamide as a New Reagent for Synthesis of Amides, Esters, Aldehydes and for Dehydration Reactions
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Cyanuric chloride reacts with dimethylformamide to form a complex (I), which can be used directly for the synthesis of amides, esters, relatively simple peptides, aldehydes and for dehydration reactions.
- Lahoti, R. J.,Wagle, D. R.
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p. 1007 - 1008
(2007/10/02)
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- Heteroacyl Azides as Acylating Agents for Aromatic or Heteroatomic Amines (1)
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The possibility of formation of substituted heterocyclic amides from heteroacyl azides and aromatic or heteroatomic amines was investigated.Although acylation proceeded in some cases under mild reaction conditions, formation of N,N'-disubstituted ureas was the main process at elevated temperatures.
- Stanovnik, B.,Tisler, M.,Golob, V.,Hvala, I.,Nikolic, O.
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p. 733 - 736
(2007/10/02)
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