- On-resin N-formylation of peptides: a head-to-head comparison of reagents in solid-phase synthesis of ligands for formyl peptide receptors
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General conditions for efficient on-resin N-formylation of peptides were identified by screening of a number of reagents comprising aliphatic formates (ethyl formate, 2,2,2-trifluoroethyl formate, and cyanomethyl formate), aromatic esters (phenyl formate and p-nitrophenyl formate), and N-formylimidazole and in situ activation of formic acid with the coupling reagent 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide. Initially, reaction time and influence of solvent were examined for the formylation of a short model peptide. The most efficient reagents were examined further by using different linkers and solid supports in the synthesis of an array of longer formyl peptide ligands. For p-nitrophenyl formate and N-formylimidazole, almost complete conversion was reached within 2?h, albeit longer peptides attached to Tentagel resins via different linkers required an extended reaction time. Overall, the commercially available activated ester p-nitrophenyl formate proved to be most convenient and versatile as high formylation degrees were obtained after 1–3?h at room temperature, while either conventional or microwave-assisted heating allowed reduction of the formylation time to 20?min. Copyright
- Christensen, Simon Bendt,Hansen, Anna Mette,Franzyk, Henrik
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Read Online
- Synthesis of new five-membered N-heterocycle derivatives of mono- and bis-phosphonic acids
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The new functionalized hydroxymethylphosphonic and methylenebis(phosphonic) acids are synthesized via reaction of tris(trimethylsilyl) phosphite and N-formyl derivatives of five-membered N-heterocycles in the presence of trimethylsilyl triflate.
- Prishchenko, Andrey A.,Livantsov, Mikhail V.,Novikova, Olga P.,Livantsova, Ludmila I.,Petrosyan, Valery S.
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Read Online
- Preparation method of iguratimod intermediate
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The invention discloses a preparation method of an iguratimod intermediate. The preparation method comprises the following steps: by using formic acid as a starting raw material, subjecting formic acid to reacting with N,N-carbonyldiimidazole (CDI) via an
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Paragraph 0011; 0019-0023; 0025
(2021/01/24)
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- UiO-66 as an efficient catalyst for N-formylation of amines with CO2 and dimethylamine borane as a reducing agent
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The most effective way to make the best use of CO2, is the reductive formylation of amines, as formamides have many applications in industry. A new protocol has been developed for reductive N-formylation of amines with CO2 as a C1 carbon source and DMAB (Dimethylamine borane) as a reducing agent in the presence of Zr-containing metal–organic framework (MOF) as an efficient, heterogeneous recyclable catalyst. We used UiO-66 and UiO-66-NH2 as catalysts for N-formylation of amines and observed that both the catalyst performs equally. Therefore, we continued our studies with UiO-66 as a catalyst. The UiO-66 MOF shows good catalytic activity and affording the desired formamides in good to excellent yield. This catalytic system is very efficient for several amines including primary and secondary aliphatic cyclic and aromatic amines. Moreover, the prepared catalyst was recycled up to four recycled without a considerable decrease in catalytic activity.
- Phatake, Vishal V.,Mishra, Ashish A.,Bhanage, Bhalchandra M.
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supporting information
(2019/12/11)
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- A NHC-silyliumylidene cation for catalytic N?formylation of amines using carbon dioxide
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This study describes the use of a silicon(II) complex, namely, the NHC-silyliumylidene cation complex [(IMe)2SiH]I (1, IMe =:C{N(Me)C(Me)}2), to catalyze the chemoselective N-formylation of primary and secondary amines using CO2 and PhSiH3 under mild conditions to afford the corresponding formamides as a sole product (average reaction time: 4.5 h; primary amines, average yield: 95%, average TOF: 8 h?1; secondary amines, average yield: 98%, average TOF: 17 h?1). The activity of 1 and product yields outperform the currently available non-transition-metal catalysts used for this catalysis. Mechanistic studies show that the silicon(II) center in complex 1 catalyzes the C?N bond formation via a different pathway in comparison with non-transition-metal catalysts. It sequentially activates CO2, PhSiH3, and amines, which proceeds via a dihydrogen elimination mechanism, to form formamides, siloxanes, and dihydrogen gas.
- Leong, Bi-Xiang,Teo, Yeow-Chuan,Condamines, Cloe,Yang, Ming-Chung,Su, Ming-Der,So, Cheuk-Wai
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p. 14824 - 14833
(2020/12/21)
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- Tris(trimethylsilyl) phosphite as key synthon for convenient synthesis of new organosilicon(phosphorus)-containing N-heterocycles
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The new functionalized hydroxymethylphosphonic and methylenediphosphonic acids are synthesized via unique reaction of tris(trimethylsilyl) phosphite and N-formyl N-heterocycles, N-substituted 4-piperidones, 3-quinuclidone, and 2-adamantanone at the presence of effective catalyst – trimethylsilyl triflate under mild conditions.
- Prishchenko, Andrey A.,Alekseyev, Roman S.,Livantsov, Mikhail V.,Novikova, Olga P.,Livantsova, Ludmila I.,Petrosyan, Valery S.
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p. 149 - 154
(2017/10/31)
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- MEPicides: α,β-Unsaturated Fosmidomycin Analogues as DXR Inhibitors against Malaria
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Severe malaria due to Plasmodium falciparum remains a significant global health threat. DXR, the second enzyme in the MEP pathway, plays an important role to synthesize building blocks for isoprenoids. This enzyme is a promising drug target for malaria due to its essentiality as well as its absence in humans. In this study, we designed and synthesized a series of α,β-unsaturated analogues of fosmidomycin, a natural product that inhibits DXR in P. falciparum. All compounds were evaluated as inhibitors of P. falciparum. The most promising compound, 18a, displays on-target, potent inhibition against the growth of P. falciparum (IC50 = 13 nM) without significant inhibition of HepG2 cells (IC50 > 50 μM). 18a was also tested in a luciferase-based Plasmodium berghei mouse model of malaria and showed exceptional in vivo efficacy. Together, the data support MEPicide 18a as a novel, potent, and promising drug candidate for the treatment of malaria.
- Wang, Xu,Edwards, Rachel L.,Ball, Haley,Johnson, Claire,Haymond, Amanda,Girma, Misgina,Manikkam, Michelle,Brothers, Robert C.,McKay, Kyle T.,Arnett, Stacy D.,Osbourn, Damon M.,Alvarez, Sophie,Boshoff, Helena I.,Meyers, Marvin J.,Couch, Robin D.,Odom John, Audrey R.,Dowd, Cynthia S.
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supporting information
p. 8847 - 8858
(2018/10/05)
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- Polymer Meets Frustrated Lewis Pair: Second-Generation CO2-Responsive Nanosystem for Sustainable CO2 Conversion
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Frustrated Lewis pairs (FLP), a couple comprising a sterically encumbered Lewis acid and Lewis base, can offer latent reactivity for activating inert gas molecules. However, their use as a platform for fabricating gas-responsive materials has not yet developed. Merging the FLP concept with polymers, we report a new generation CO2-responsive system, differing from the first-generation ones based on an acid–base equilibrium mechanism. Two complementary Lewis acidic and basic block copolymers, installing bulky borane- and phosphine-containing blocks, were built as the macromolecular FLP. They can bind CO2 to drive micellar formation, in which CO2 as a cross-linker bridges the block chains. This dative bonding endows the assembly with ultrafast response (2 can function as nanocatalysts for recyclable C1 catalysis, opening a new direction of sustainable CO2 conversion.
- Chen, Liang,Liu, Renjie,Yan, Qiang
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supporting information
p. 9336 - 9340
(2018/07/25)
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- Sulfated polyborate-catalyzed N-formylation of amines: a rapid, green and efficient protocol
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Abstract: A rapid, green and efficient method for N-formylation reaction of various amines with formic acid in the presence of sulfated polyborate catalyst under solvent-free conditions has been described. The catalyst has the advantage of mild Bronsted as well as Lewis acid character. The catalyst is recyclable with no significant loss in catalytic activity. The present protocol is advantageous due to its solvent-free condition, short reaction time, high yields, easy workup and ability to tolerate a variety of functional groups.
- Khatri, Chetan K.,Chaturbhuj, Ganesh U.
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p. 2513 - 2519
(2017/11/06)
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- Synthesis of new functionalized mono- and diphosphonic acids with five-membered aza-heterocycles moieties
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The new functionalized hydroxymethylphosphonic and methylenediphosphonic acids are synthesized via unique reaction of tris(trimethylsilyl)phosphite and N-formyl derivatives of five-membered aza-heterocycles at the presence of effective catalyst—trimethylsilyl triflate.
- Prishchenko, Andrey A.,Alekseyev, Roman S.,Livantsov, Mikhail V.,Novikova, Olga P.,Livantsova, Ludmila I.,Terenin, Vladimir I.,Petrosyan, Valery S.
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- New functionalized derivatives of mono- and diphosphonic acids substituted with five-membered nitrogen heterocycles
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New types of (hydroxymethyl)phosphonic and (methylene)diphosphonic acids bearing heterocyclic fragments were synthesized by addition of tris(trimethylsilyl) phosphite to N-formyl derivatives of five-membered nitrogen heterocycles.
- Prishchenko,Livantsov,Novikova,Livantsova,Alekseyev,Terenin,Petrosyan
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p. 342 - 345
(2017/07/12)
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- A Continuous-Flow Process for Palladium-Catalyzed Olefin Cleavage by using Oxygen within the Explosive Regime
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A continuous-flow protocol for Pd-catalyzed olefin cleavage by using molecular oxygen as the sole oxidant to give carbonyl compounds was explored. The developed flow protocol allowed the use of a low catalyst loading (0.1 mol %), and decomposition of the active catalyst was prevented through stabilization by poly(ethylene glycol)-400 (PEG-400), which was present as a cosolvent. Radical scavengers inhibited the reaction, which indicated the involvement of a free-radical path in the reaction mechanism. The applicability of the continuous-flow protocol was demonstrated on several olefin substrates. The continuous-flow process enabled safe and scalable olefin cleavage.
- Hone, Christopher A.,O'Kearney-McMullan, Anne,Munday, Rachel,Kappe, C. Oliver
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p. 3298 - 3302
(2017/09/13)
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- Acidic ionic liquid immobilized on nanoporous Na+-montmorillonite as an efficient and reusable catalyst for the formylation of amines and alcohols
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In this work, nanoporous sodium montmorillonite clay (Na+-MMT) was used as a support for the immobilization of 1-methyl-3-(trimethoxysilylpropyl)-imidazolium hydrogen sulfate. The Na+-MMT chemical modification ([Na+-MMT-[pmim]HSO4) was confirmed by a variety of techniques including Fourier transform infrared spectroscopy (FT-IR), X-ray diffraction (XRD), thermogravimetric analysis (TGA), scanning electron microscopy and potentiometric titration. The catalytic performance of this immobilized acidic ionic liquid was probed for the N-formylation of a variety of amines using formic acid under solvent-free conditions. This reagent is also useful for the formylation of benzylic alcohols. The procedure gave the products in excellent yields in very short reaction times. Also, this catalyst can be reused ten times without loss of its catalytic activity.
- Shirini, Farhad,Mazloumi, Masoumeh,Seddighi, Mohadeseh
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p. 1759 - 1776
(2016/03/16)
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- Solid poly-N-heterocyclic carbene catalyzed CO2 reduction with hydrosilanes
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The utility of solid poly-N-heterocyclic carbene (poly-NHC) materials as organocatalysts for carbon dioxide reduction was studied. These poly-NHC particles were demonstrated to be useful as heterogeneous organocatalysts for the reduction of carbon dioxide to methanol and for the formylation of N–H bonds with hydrosilanes as a hydride donor. These solid catalysts could potentially be useful in large-scale syntheses due to the ease of catalyst recycle and reuse, providing cost savings and environmental sustainability in the long run.
- Riduan, Siti Nurhanna,Ying, Jackie Y.,Zhang, Yugen
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- An efficient method for the synthesis of formamidine and formamide derivatives promoted by sulfonated rice husk ash (RHA-SO3H)
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A mild, simple and efficient method has been developed for the promotion of the preparation of N,N′-diphenylformamidines from various aromatic amines and ethyl orthoformate using sulfonated rice husk ash (RHA-SO3H) solid acid catalyst. This reagent has also been used for the N-formylation of a variety of amines using formic acid under solvent-free conditions. The procedures gave the products in very short reaction times and good-to-high yields. Also this catalyst can be reused for five times without loss of its catalytic activity.
- Seddighi, Mohadeseh,Shirini, Farhad,Mamaghani, Manouchehr
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p. 433 - 439
(2015/02/05)
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- Br?nsted acidic ionic liquid supported on rice husk ash (RHA-[pmim]HSO4): A highly efficient and reusable catalyst for the formylation of amines and alcohols
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In this work, rice husk ash (RHA), as a natural source of amorphous silica, was used as a support for the immobilization of 1-methyl-3-(trimethoxysilylpropyl)-imidazolium hydrogen sulfate. The immobilized acidic ionic liquid was characterized with a variety of techniques including infrared spectroscopy (FT-IR), X-ray diffraction (XRD), thermogravimetric analysis (TGA), scanning electron microscopy (SEM) and pH analysis. The catalytic performance of this heterogeneous ionic liquid was probed for the N-formylation of a variety of amines using formic acid under solvent free conditions. It is also useful for the formylation of benzylic alcohols. The procedure gave the products in excellent yields in very short reaction times. Also this catalyst can be reused ten times without loss of its catalytic activity.
- Shirini, Farhad,Seddighi, Mohadeseh,Mamaghani, Manouchehr
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p. 50631 - 50638
(2014/12/10)
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- An eco-benign and highly efficient procedure for N-acylation catalyzed by heteropolyanion-based ionic liquids using carboxylic acid under solvent-free conditions
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An eco-benign and highly efficient route for N-acylation of amines has been developed by treating amines with corresponding carboxylic acids in the presence of 2 mol % of heteropolyanion-based ionic liquids as catalysts under solvent-free conditions. This practical reaction could tolerate a wide range of substrates. Thus, various N-acylation products including N-acyl α-amino acid derivatives were obtained in moderate to excellent yields at 70 C to 120 C. Moreover, recycling studies revealed that heteropolyanion-based ionic liquids were easily reusable for this N-acylation. This method provides a green and much improved protocol over the existing methods.
- Chen, Zhikai,Fu, Renzhong,Chai, Wen,Zheng, Hao,Sun, Lin,Lu, Qiang,Yuan, Rongxin
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p. 2237 - 2245
(2014/03/21)
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- Heteropolyanion-based sulfated ionic liquid catalyzed formamides synthesis by grindstone chemistry
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A novel heteropolyanion-based sulfated ionic liquid (HIL-[Ch-OSO 3H]3W12PO40) was prepared by pairing sulfate functionalized cholinium cation [N,N,N-trimethyl-2-(sulfooxy) ethanaminium] with catalytically active phosphotungstic acid anion (W 12PO403-). It was characterized by 1H NMR, FT-IR, EDX, XRD, TGA and elemental analysis. Catalytic activity of thus prepared HIL was studied in N-formylation of amines under solvent-free grinding condition. The methodology provided cleaner conversion over shorter reaction time with high turnover frequency (TOF) and chemoselectivity.
- Satasia, Shailesh P.,Kalaria, Piyush N.,Raval, Dipak K.
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- Method for Preparing Formamide Compounds
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The present invention relates to a method for preparing formamide compounds using carbon dioxide, and to the use of said method for manufacturing vitamins, pharmaceutical products, adhesives, acrylic fibres, synthetic leathers, pesticides and fertilisers. The invention also relates to a method for manufacturing vitamins, pharmaceutical products, adhesives, acrylic fibres, synthetic leathers, pesticides and fertilisers which includes a step of preparing formamide compounds by the method according to the invention.
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Paragraph 0126-0136
(2014/02/16)
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- Formylation of amines catalysed by protic ionic liquids under solvent-free condition
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A fast, efficient and simple route for the N-formylation of amines has been developed by treating amines with 85% formic acid at 70°C in the presence of 5 mol % of protic ionic liquid as catalyst under solvent-free condition. This method provides a green and much improved protocol over the existing methods.
- Majumdar, Swapan,De, Jhinuk,Hossain, Jewel,Basak, Ajoy
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p. 262 - 266
(2013/02/22)
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- Nano rod-shaped and reusable basic Al2O3 catalyst for N-formylation of amines under solvent-free conditions: A novel, practical and convenient 'NOSE' approach
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An expeditious, simple, highly efficient, practical and green protocol for the N-formylation of alkyl/aryl amines and indole derivatives catalyzed by novel nano rod-shaped basic Al2O3 under solvent-free conditions has been developed. The catalyst is efficiently recycled up to the 5th run, an important point in the domain of green chemistry. The methodology provides cleaner conversion, shorter reaction times and high selectivity which makes the protocol attractive. The Royal Society of Chemistry 2012.
- Das, Vijay Kumar,Devi, Rashmi Rekha,Raul, Prasanta Kumar,Thakur, Ashim Jyoti
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supporting information; experimental part
p. 847 - 854
(2012/04/23)
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- Recycling of carbon and silicon wastes: Room temperature formylation of N-H bonds using carbon dioxide and polymethylhydrosiloxane
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A highly active organocatalytic system based on N-heterocyclic carbenes has been designed for the formylation of N-H bonds in a large variety of nitrogen molecules and heterocycles, using two chemical wastes: CO2 and polymethylhydrosiloxane (PMHS).
- Jacquet, Olivier,Das Neves Gomes, Christophe,Ephritikhine, Michel,Cantat, Thibault
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supporting information; experimental part
p. 2934 - 2937
(2012/03/27)
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- 3,5,5-Trisubstituted hydantoins from activated (benzyloxycarbonylamino) malonic acids
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Diethyl 2-alkyl-2-(benzyloxycarbonylamino)malonates were saponified, activated with oxalyl chloride, and treated with primary aromatic amines. This gave 3,5-disubstituted hydantoin-5-carboxamides. As second products, 2-alkyl-2-formamido-N1,Nsu
- Hroch, Lukas,Hruskova, Marie,Schmitz, Janina,Schnakenburg, Gregor,Guetschow, Michael
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experimental part
p. 1907 - 1914
(2012/08/07)
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- Formylation of amines and alcohols using aminopropylated mesoporous SBA-15 silica (APMS) as an efficient and recyclable catalyst
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Aminopropylated mesoporous SBA-15 silica (APMS) is introduced as a new, recyclable and efficient catalyst for the formylation of a variety of amines and alcohols by using readily available formic acid under solvent-free conditions.
- Malakooti, Reihaneh,Sobhani, Sara,Razavi, Nasrin,Shafiei, Soheila,Mokhtari, Rezvan
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experimental part
p. 1979 - 1990
(2012/04/17)
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- Sulfonic acid supported on hydroxyapatite-encapsulated-γ-Fe2O3 nanocrystallites as a magnetically Br?nsted acid for N-formylation of amines
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Treatment of aqueous formic acid (85%) with structurally diverse amines in the presence of a catalytic amount of sulfonic acid supported on hydroxyapatite-encapsulated-γ-Fe2O3 [HAp@-γ-Fe2O3] (0.9 mol.%) as a heterogeneous, reusable and highly efficient catalyst gave the corresponding formamides in good to excellent yields at room temperature. The magnetically catalytic system was recovered by-passing time consuming filtration operation by using an external magnet device. In addition to facility, this methodology, it also enhances product purity and promises economic as well as environmental benefits.
- Ma'mani, Leila,Sheykhan, Mehdi,Heydari, Akbar,Faraji, Mohammad,Yamini, Yadollah
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experimental part
p. 64 - 69
(2010/07/05)
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- Total synthesis of proximicin A - C and synthesis of new furan-based DNA binding agents
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The total synthesis of the natural occurring polyamides proximicin A-C (3-5) has been accomplished. A short and efficient synthesis of a thus far unknown 4-amino-2-furan carboxylic acid was developed. Furthermore, this unique heterocyclic γ-amino-acid was
- Wolter, Falko E.,Schneider, Kathrin,Davies, Brian P.,Socher, Elke R.,Nicholson, Graeme,Seitz, Oliver,Suessmuth, Roderich D.
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supporting information; experimental part
p. 2804 - 2807
(2009/12/05)
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- Enantioselective total synthesis of the oral contraceptive desogestrel by a double heck reaction
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A novel enantioselective total synthesis of the oral contraceptive desogestrel (2) is described, in which the tetracyclic steroid core is formed by a sequence of two consecutive Heck reactions. Conversion of the known enantiopure diketone 7 led to the chiral bicycle 6 which was used for a diastereoselective intermolecular Heck reaction with vinyliodide 5 to give 15. In the following intramolecular Heck reaction, the tetracyclic ring system was formed to give 4, from which the synthesis of desogestrel (2) was furnished.
- Tietze, Lutz F.,Krimmelbein, Ilga K.
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experimental part
p. 1541 - 1551
(2009/04/04)
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- 2-AMINO- AND 2-THIO-SUBSTITUTED 1,3-DIAMINOPROPANES
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Disclosed are compounds of the formula: where variables Q, Z, X, R15, R2, R3, and Rc are defined herein. Compounds disclosed herein are inhibitors of the beta-secretase enzyme and are therefore useful in the treatment of Alzheimer’s disease and other diseases characterized by deposition of A beta peptide in a mammal.
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Page/Page column 196-197
(2008/06/13)
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- METHODS OF TREATMENT OF AMYLOIDOSIS USING ASPARTYL-PROTEASE INHIBITORS
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The invention relates to acetyl 2-hydroxy-1,3-diaminospirocyclohexanes and derivatives thereof that are useful in treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.
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Page/Page column 171
(2010/02/13)
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- Synthesis and Biological Activity of Hydroxamic Acid-Derived Vasopeptidase Inhibitor Analogues
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(Equation Presented) Syntheses of novel hydroxamic acid-derived azepinones containing pendant mercaptoacyl groups or formyl hydroxamates are described. These new analogues of therapeutically important ACE and NEP inhibitors include unprecedented changes a
- Walz, Andrew J.,Miller, Marvin J.
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p. 2047 - 2050
(2007/10/03)
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- Conjugate addition to 3-arylsulfinylchromones as a synthetic route to homochiral 2-substituted chromanones: Scope and limitations
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A route to homochiral 2-substituted chromanones via the diastereoselective conjugate addition of organocopper reagents to 3-(p-tolylsulfinyl)chromones has been improved and used to prepare 2,6-dimethylchromanone (S)-4 and LL-D253α methyl ether (S)-6. The attempted preparation of a 2-phenylchromanone (flavanone) using this strategy was unsuccessful due to the lability of the intermediate 2-phenyl-3-(p-tolylsulfinyl)chromanone, which underwent sulfoxide elimination at room temperature to give the corresponding 2-phenylchromone (flavone).
- Hodgetts, Kevin J,Maragkou, Konstantina I,Wallace, Timothy W,Wootton, Robert C.R
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p. 6793 - 6804
(2007/10/03)
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- Synthesis of (+)-(R)-5-hydroxy-6-hydroxymethyl-7-methoxy-8-methylflavanone
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The synthesis of (+)-(R)-5-hydroxy-6-hydroxymethyl-7-methoxy-8-methylflavanone is described. A new chromylation method of β-ketosulfoxide 9 leading to the Michael acceptor 12 has been developed. Dilithium tetra-chlorocuprate was shown to be a very efficie
- Solladie, Guy,Gehrold, Nicolai,Maignan, Jean
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p. 2739 - 2747
(2007/10/03)
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- Benzimidazole derivatives
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Disclosed are compounds represented by the following chemical formula (I) and pharmacologically acceptable salts thereof which are novel compounds useful as anticancer agents, antiviral agents or antimicrobial agents. STR1
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- Convenient one-pot method for formylation of amines and alcohols using formic acid and 1,1'-oxalyldiimidazole
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1,1'-Oxalyldiimidazole (7) reacts with formic acid (8) in acetonitrile at room temperature to give N-formylimidazole (5), which promptly undergoes aminolysis and alcoholysis to yield formamides (2) or formates (4).
- Kitagawa,Arita,Nagahata
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p. 1655 - 1657
(2007/10/02)
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- A palladium-catalyzed, abnormal hydrogenolytic ring-cleavage reaction of fused β-lactams
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Bicyclic β-lactams, such as 1-oxa- and 1-carba-penams, are reductively cleaved between the lactam carbonyl group and the α-carbon by palladium catalysts to give formamide derivatives.
- Konosu,Oida
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p. 609 - 611
(2007/10/02)
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- 6-Substituted 1,3,4,5-tetrahydrobenz[cd]indol-4-amines: Potent serotonin agonists
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A series of 6-substituted tricyclic ergoline partial structures has been synthesized and found to possess very strong serotonin agonist activity. A methoxy group at the 6-position greatly enhances activity, but at the expense of compound stability. Substi
- Flaugh,Mullen,Fuller,Mason
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p. 1746 - 1753
(2007/10/02)
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- Inhibitors of Porcine Pancreatic Elastase. Peptides Incorporating &α-Aza-amino Acid Residues in the P1 Position
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Inhibitors of porcine pancreatic elastase based on one of the repeating peptide sequences (Gly-Val-Gly-Val-Ala) present in elastin have been prepared.Most of these contain an α-aza-amino acid benzyl ester group at the C-terminus and an N-(1-methoxycarbon
- Dutta, Anand S.,Giles, Michael B.,Williams, Joseph C.
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p. 1655 - 1664
(2007/10/02)
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- Efficient Total Syntheses of the Oligopeptide Antibiotics Netropsin and Distamycin
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New and efficient total syntheses of the natural oligopeptide antiviral antibiotics netropsin and distamycin are described.These procedures feature a different strategy of introduction of the terminal groups from that used hitherto, high yield coupling steps, improvements in the Pinner reaction for introducing the amidine moiety, and the novel use of N-formylimidazole for introduction of the formyl moiety in distamycin.The methods also avoid column chromatography with the attendant contamination of the oligopeptide hydrochlorides with inorganic salts eluted from adsorbents.The synthetic procedures are general and may be adapted to the synthesis of related oligopeptide structures.
- Lown, J. William,Krowicki, Krzysztof
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p. 3774 - 3779
(2007/10/02)
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