- Preparation method of tert-butyl glycine
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The invention discloses a preparation method of tert-butyl glycine, and belongs to the technical field of organic synthesis. The raw materials are easily available, the process is simple, the process is simple, the reaction conditions are mild, the requirement for equipment is low, the total yield is up to 85 - 93%, and a significant amount of double-substituted by-products are effectively avoided in the direct reaction with ammonia in the traditional process.
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- A General Stereocontrolled Synthesis of Opines through Asymmetric Pd-Catalyzed N-Allylation of Amino Acid Esters
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A stereo-divergent synthesis of natural and unnatural opines in stereochemically pure form is based on the direct palladium-catalyzed N-allylation of α-amino acid esters (up to 97 % ee or 99 : 1 d.r.) using methyl (E)-2-penten-4-yl carbonate in the presence of only 1 mol% of a catalyst, prepared in-situ from the C2-symmetric diphosphine iPr-MediPhos and [Pd(allyl)Cl]2. Selected target compounds (incl. a derivative of the drug enalapril) were efficiently obtained from the N-allylated intermediates by oxidative cleavage (ozonolysis) of the allylic C=C bond under temporary N-Boc-protection.
- Albat, Dominik,Neud?rfl, J?rg-Martin,Schmalz, Hans-Günther
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supporting information
p. 2099 - 2102
(2021/07/22)
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- Single Electron Transfer-Induced Selective α-Oxygenation of Glycine Derivatives
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Modification of amino acids is an important strategy in organic and bioorganic chemistry. In contrast to common side-chain functionalization, backbone modification is much less explored. Especially glycine units seem to be attractive and versatile since a wide range of functionality can be potentially introduced. We report here oxidative modification of glycinates that are stable and enable further functionalization. Selective glycinate enolate oxidation by TEMPO or a FeCp2PF6/TEMPO reagent combination provides stable alkoxyamines in good to excellent yields. The methodology is expanded to glycine-containing dipeptides demonstrating selective oxygenation at the glycine unit. The orthogonal reactivity potential of oxygenated glycines for transformation to other amino acid derivatives is explored.
- Císa?ová, Ivana,Jahn, Ullrich,K?nig, Burkhard,Moser, Johannes,Venugopal, Navyasree,Vojtí?ková, Margaréta
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supporting information
(2021/11/03)
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- Overcoming the Deallylation Problem: Palladium(II)-Catalyzed Chemo-, Regio-, and Stereoselective Allylic Oxidation of Aryl Allyl Ether, Amine, and Amino Acids
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We report herein a Pd(II)/bis-sulfoxide-catalyzed intramolecular allylic C-H acetoxylation of aryl allyl ether, amine, and amino acids with the retention of a labile allyl moiety. Mechanistically, the reaction proceeds through a distinct double-bond isomerization from the allylic to the vinylic position followed by intramolecular carboxypalladation and the β-hydride elimination pathway. For the first time, C-H oxidation of N-allyl-protected amino acids to furnish five-membered heterocycles through 1,3-syn-addition is established with excellent diastereoselectivity.
- Begam, Hasina Mamataj,Jana, Ranjan,Manna, Kartic,Samanta, Krishanu
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supporting information
p. 7443 - 7449
(2020/10/09)
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- Multicomponent synthesis of pyroglutamic acid derivatives: Via Knoevenagel-Michael-hydrolysis-lactamization-decarboxylation (KMHL-D) sequence
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A novel and practical method for the synthesis of 3-substituted pyroglutamic acid derivatives is described. One pot multicomponent reaction of Meldrum's acid, aldehyde and Schiff's base followed an unprecedented chemoselective Knoevenagel-Michael-hydrolysis-lactamization domino sequence to afford 4-carboxy 3-substituted pyroglutamic acid derivatives under mild conditions. A carboxy intermediate formed appears to accelerate its own formation. The generality of the synthesis is exemplified by the use of a wide variety of aldehydes including enolizable aliphatic aldehydes, while substrates are stable under reaction conditions.
- Khopade, Tushar M.,Warghude, Prakash K.,Sonawane, Amol D.,Bhat, Ramakrishna G.
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supporting information
p. 561 - 566
(2019/01/24)
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- Simple and efficient Fmoc removal in ionic liquid
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A mild method for an efficient removal of the fluorenylmethoxycarbonyl (Fmoc) group in ionic liquid was developed. The combination of a weak base such as triethylamine and [Bmim][BF4] makes the entire system more efficient for the cleavage at room temperature of various amines and amino acid methyl esters in short reaction times. The procedure works well even in the case of N-Fmoc amino acids bearing acid-sensitive protecting groups and of N-alkylated amino acid methyl esters. The solvent-free condition provides a complementary method for Fmoc deprotection in solution phase peptide synthesis and modern organic synthesis.
- Di Gioia,Costanzo,De Nino,Maiuolo,Nardi,Olivito,Procopio
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p. 36482 - 36491
(2017/08/02)
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- Efficient Synthesis of 11C-Acrylesters, 11C-Acrylamides and Their Application in Michael Addition Reactions for PET Tracer Development
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Here we present a new Michael addition reaction utilizing carbon-11 labeled acrylic esters and amides. Subsequently, reactions of these synthons with commercially available Schiff base precursors are performed to produce [11C]glutamate and [11C]glutamine. This methodology is especially useful for the development of positron emission tomography (PET) imaging agents as it offers a new array of potential carbon-11 labeled compounds with this original 11C–C bond forming strategy.
- Filp, Ulrike,Pees, Anna L.,Taddei, Carlotta,Peko?ak, Aleksandra,Gee, Antony D.,Windhorst, Albert D.,Poot, Alex J.
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supporting information
p. 5154 - 5162
(2017/09/20)
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- Total synthesis of (-)-platensimycin by advancing oxocarbenium- and iminium-mediated catalytic methods
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(-)-Platensimycin is a potent inhibitor of fatty acid synthase that holds promise in the treatment of metabolic disorders (e.g., diabetes and "fatty liver") and pathogenic infections (e.g., those caused by drug-resistant bacteria). Herein, we describe its total synthesis through a four-step preparation of the aromatic amine fragment and an improved stereocontrolled assembly of the ketolide fragment, (-)-platensic acid. Key synthetic advances include 1) a modified Lieben haloform reaction to directly convert an aryl methyl ketone into its methyl ester within 30 seconds, 2) an experimentally improved dialkylation protocol to form platensic acid, 3) a sterically controlled chemo- and diastereoselective organocatalytic conjugate reduction of a spiro-cyclized cyclohexadienone by using the trifluoroacetic acid salt of α-amino di-tert-butyl malonate, 4) a tetrabutylammonium fluoride promoted spiro-alkylative para dearomatization of a free phenol to assemble the cagelike ketolide core with the moderate leaving-group ability of an early tosylate intermediate, and 5) a bismuth(III)-catalyzed Friedel-Crafts cyclization of a free lactol, with LiClO4 as an additive to liberate a more active oxocarbenium perchlorate species and suppress the Lewis basicity of the sulfonyloxy group. The longest linear sequence is 21 steps with an overall yield of 3.8% from commercially available eugenol. Relay tactics: The stereocontrolled assembly of the potent antibiotic (-)-platensimycin in 21 steps and 3.8% yield from eugenol is described (see scheme; TBAF: tetrabutylammonium fluoride; Ts: toluene-4-sulfonyl). Highlights are 1) a rapid oxidative esterification of an acyl aromatic, 2) a reliable dialkylation protocol to form platensic acid, 3) a π-facial conjugate reduction of a dienone, 4) a TBAF-promoted alkylative dearomatization of a free phenol, and 5) a Friedel-Crafts closure of a free lactol.
- Eey, Stanley T.-C.,Lear, Martin J.
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p. 11556 - 11573
(2015/01/16)
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- Chiral iminoesters derived from d-glyceraldehyde in [3+2] cycloaddition reactions. Asymmetric synthesis of a key intermediate in the synthesis of neuramidinase inhibitors
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Silver-catalyzed endo-selective and copper-catalyzed exo-selective asymmetric [3 + 2] cycloadditions of acrylates to chiral iminoesters derived from d-glyceraldehyde have been investigated. The reaction diastereoselectively provides highly functionalized pyrrolidines. This approach was used to develop the first asymmetric synthesis of a key intermediate in the synthesis of pyrrolidine influenza neuramidinase inhibitors.
- Galvez, Jose A.,Diaz-De-Villegas, Maria D.,Alias, Miriam,Badorrey, Ramon
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p. 11404 - 11413
(2013/12/04)
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- An efficient synthesis of tert-butyl ethers/esters of alcohols/amino acids using methyl tert-butyl ether
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A facile synthesis of a wide variety of tert-butyl ethers and tert-butyl ester derivatives under mild conditions is described. Alcohols etherified with tert-butyl methyl ether as tert-butyl source and solvent, in the presence of sulfuric acid. Many amino acid tert-butyl esters have been synthesized by this procedure. The reaction is simple, inexpensive, easily scaled up, and proceeds without observable racemization. A green method was developed for the deprotection of this group using Amberlite resin IR 120-H as catalyst.
- Mallesha,Prahlada Rao,Suhas,Channe Gowda
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experimental part
p. 641 - 645
(2012/02/15)
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- Haloenol pyranones and morpholinones as antineoplastic agents of prostate cancer
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Haloenol pyran-2-ones and morpholin-2-ones were synthesized and evaluated as inhibitors of cell growth in two different prostate human cancer cell lines (PC-3 and LNCaP). Analogs derived from l- and d-phenylglycine were found to be the most effective antagonists of LNCaP and PC-3 cell growth. Additional studies reveal that the inhibitors induced G2/M arrest and the (S)-enantiomer of the phenylglycine-based derivatives was a more potent inhibitor of cytosolic iPLA2β.
- Mock, Jason N.,Taliaferro, John P.,Lu, Xiao,Patel, Sravan Kumar,Cummings, Brian S.,Long, Timothy E.
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scheme or table
p. 4854 - 4858
(2012/08/13)
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- Toward the selective delivery of chemotherapeutics into tumor cells by targeting peptide transporters: Tailored gold-based anticancer peptidomimetics
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Complexes [AuIIIX2(dtc-Sar-AA-O(t-Bu))] (AA = Gly, X = Br (1)/Cl (2); AA = Aib, X = Br (3)/Cl (4); AA = l-Phe, X = Br (5)/Cl (6)) were designed on purpose in order to obtain gold(III)-based anticancer peptidomimetics that might specifically target two peptide transporters (namely, PEPT1 and PEPT2) upregulated in several tumor cells. All the compounds were characterized by means of FT-IR and mono- and multidimensional NMR spectroscopy, and the crystal structure of [AuIIIBr2(dtc-Sar-Aib-O(t- Bu))] (3) was solved and refined. According to in vitro cytotoxicity studies, the Aib-containing complexes 3 and 4 turned out to be the most effective toward all the human tumor cell lines evaluated (PC3, DU145, 2008, C13, and L540), reporting IC50 values much lower than that of cisplatin. Remarkably, they showed no cross-resistance with cisplatin itself and were proved to inhibit tumor cell proliferation by inducing either apoptosis or late apoptosis/necrosis depending on the cell lines. Biological results are here reported and discussed in terms of the structure-activity relationship.
- Negom Kouodom, Morelle,Ronconi, Luca,Celegato, Marta,Nardon, Chiara,Marchiò, Luciano,Dou, Q. Ping,Aldinucci, Donatella,Formaggio, Fernando,Fregona, Dolores
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scheme or table
p. 2212 - 2226
(2012/05/05)
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- A straightforward approach towards combined ?-amino and ?-hydroxy acids based on Passerini reactions
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Complex amino acids with an ?-acyloxycarbonyl functionality in the side chain are easily available through epoxide opening by chelated enolates and subsequent oxidation/Passerini reaction. This protocol works with both, aldehyde and ketone intermediates, as long as the ketones are activated by electron-withdrawing groups. In principle Ugi reactions are also possible, allowing the generation of diamino acid derivatives.
- Zahoor, Ameer F.,Thies, Sarah,Kazmaier, Uli
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supporting information; experimental part
p. 1299 - 1303
(2011/10/19)
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- (9H-fluoren-9-yl)methanesuIfonyl (Fms): An amino protecting group complementary to Fmoc
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A sulfonamide-based protecting group (PG), (9H-fluoren-9yl)methanesulfonyl (Fms), which can be used in a similar way to the well-established Fmoc PG, was developed. The advantages of this new PG were demonstrated in the successful formation of a phosphonamide between an N-Fmsprotected a-phosphonoalanine monoester and secondary alkylamines, including (R)-2-phenylethylamine, (S)-phenylalanine iert-butyl ester (H-Phe-OtBu), H-Pro-Gly-OtBu, and H-Phe-Phe-OtBu, without formation of oxazaphospholine, which is a serious problem associated with the Fmoc PG. The success should pave the way to the solid-phase synthesis of unnatural peptides substituted with a-amino phosphonic acid (AP) at essentially any arbitrary position without significant modification of the Fmoc-based chemistry that has been accumulated since Carpino's report in 1970. The N-Fms-AP monomer would attract much attention in the field of peptide mimetics.
- Ishibashi, Yoshitaka,Miyata, Kengo,Kitamura, Masato
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experimental part
p. 4201 - 4204
(2010/10/02)
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- CARBACEPHEM β-LACTAM ANTIBIOTICS
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Carbacephem β-lactam antibiotics having the following chemical structures (I) and (II) are disclosed, including stereoisomers, pharmaceutically acceptable salts, esters and prodrugs thereof, wherein Ar2, R1, R2 and R3 are as defined herein. The compounds are useful for the treatment of bacterial infections, in particular those caused by methicillin-resistant Staphylococcus spp.
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Page/Page column 75-76
(2009/05/30)
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- Synthesis and self-association properties of flexible guanidiniocarbonylpyrrole-carboxylate zwitterions in DMSO: Intra- versus intermolecular ion pairing
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(Chemical Equation Presented) We have synthesized a new class of flexible zwitterions 6a-e, in which a carboxylate is linked via an alkyl chain with variable length (one to five methylene groups) to a guanidiniocarbonylpyrrole cation. The self-association properties of these zwitterions were determined by NMR dilution studies in DMSO and by ESI-MS experiments. The stability and hence also the size of the aggregates formed via self-assembly is critically dependent on the length and therefore flexibility of the spacer. Whereas the smallest zwitterion 6a forms large aggregates already at low concentrations, the more flexible zwitterions only form small oligomers (6b) or dimers (6c-e) at much larger concentrations. The differences between the five zwitterions can be explained based on the different extent of intramolecular ion pairing within the monomers. Any intramolecular ion pairing, which becomes possible with increasing linker length, stabilizes the monomer and therefore destabilizes any oligomer.
- Schmuck, Carsten,Rehm, Thomas,Geiger, Lars,Schaefer, Mathias
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p. 6162 - 6170
(2008/02/10)
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- Preferred conformations of peptides containing tert-leucine, a sterically demanding, lipophilic α-amino acid with a quaternary side-chain C β atom
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Terminally protected homopeptides of tert-leucine, from the dimer to the bexamer, co-oligopeptides of tert-leucine in combination with α-aminoisobutyric acid or glycine residues up to the hexamer level, and simple dipeptides representing known scaffolds for catalysts in asymmetric organic reactions were prepared by solution methods and fully characterized. The results of conformation analysis, performed by use of FT-IR absorption, NMR, CD, and X-ray diffraction techniques, indicate that this Hydrophobic α-amino acid with tetrasubstitution at the Cβ atom is structurally versatile. We show that it prefers extended or semiextended conformations, but can also be accommodated in folded structures, pro vided that these are biased by the presence of helicogenic residues. The current large-scale production of Tle, combined with its conformational preferences unravelled in this work, should make this bulky, hydrophobic, C α-trisubstituted α-amino acid a regular building block of any strategy seeking to tailor peptides with improved catalytic and pharmacological properties.
- Formaggio, Fernando
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p. 2395 - 2404
(2007/10/03)
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- Selective removal of 2,2,2-trichloroethyl- and 2,2,2- trichloroethoxycarbonyl protecting groups with Zn-N-methylimidazole in the presence of reducible and acid-sensitive functionalities
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Activated zinc dust in the presence of N-methylimidazole in ethyl acetate or acetone at reflux or room temperature removes 2,2,2-trichloroethyl- and 2,2,2-trichloroethoxycarbonyl protecting groups while azido-, nitro-, chloro-, phenacyl-, and tert-butyl ester functionalities as well as double bonds remain intact.
- Somsák, László,Czifrák, Katalin,Veres, Edit
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p. 9095 - 9097
(2007/10/03)
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- Asymmetric synthesis of β-hydroxy amino acids via aldol reactions catalyzed by chiral ammonium salts
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The Cinchona alkaloid derived chiral ammonium salt developed by Park and Jew functions as an effective catalyst for the synthesis of β-hydroxy α-amino acids via asymmetric aldol reactions under homogeneous conditions. The syn diastereomers are obtained in good ee, and aryl-substituted aliphatic aldehydes are the best substrates for the reaction. These results represent the highest ee's obtained to date in direct aldol reactions of glycine equivalents catalyzed by inexpensive, readily prepared chiral ammonium salts.
- Mettath, Sashikumar,Srikanth,Dangerfield, Benjamin S.,Castle, Steven L.
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p. 6489 - 6492
(2007/10/03)
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- Preparation and Characterization of [5-13C]-(2S,4R)-Leucine and [4-13C]-(2S,3S)-Valine - Establishing Synthetic Schemes to Prepare Any Site-Directed Isotopomer of L-Leucine, L-Isoleucine and L-Valine
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In this paper a chemo-enzymatic method has been developed that gives access to any isotopomer of the essential amino acids isoleucine and valine. The method gives the correct introduction of the second chiral center in (2S,3S)-isoleucine and allows for discrimination between the two prochiral methyl groups in valine as shown by the preparation of (2S,3S)-[4- 13C] valine. For the preparation of (2S)-leucine in any isotopomeric form, the O'Donnell method to prepare optically active amino acids has been used. The protected glycine scaffold used in this method has been prepared by a strategy that allows access to any isotopomeric form. The preparation of [5-13C]-(2S,4R)-leucine shows that the O'Donnell method in combination with the Evans method to obtain chiral 2-methylpropyl iodide leads to a good discrimination between the two prochiral methyl groups. The O'Donnell strategy for the preparation of α-amino acids is preferred over other methods since the reaction conditions are mild, the chiral auxiliary can be easily recovered and the optically active product can be easily separated. For the preparation of isotopically enriched valine and isoleucine the O'Donnell method is not suitable, because the alkyl substituents involved have a secondary halide substituent which is sterically too hindered to give an effective reaction with the protected glycine. Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2003.
- Siebum, Arjan H. G.,Woo, Wei Sein,Lugtenburg, Johan
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p. 4664 - 4678
(2007/10/03)
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- Comparative conformational analysis of peptides based on the two Ca-tetrasubstituted, Cβ-branched, chiral α-amino acids (αMe) Dip and (αMe)Val
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For the first time a number of terminally protected model peptides (to the pentamer level) of the sterically demanding α-amino acid Cα-methyl, Cα-diphenylmethylglycine, (αMe)Dip, in combination with either Ala or Gly residues, have been synthesized (by solution methods) and fully characterized. In a parallel synthesis the corresponding peptides based on the related α-amino acid Cα-methyl, Cα-isopropylglycine, (αMe)Val, have also been prepared. The results of a comparative conformational analysis, performed by using FTIR absorption, 1H NMR, and X-ray diffraction techniques, favour the conclusion that, in contrast to the potent β-turn and 310-helix promoter (αMe)Val, (αMe)Dip may induce either a folded or a fully extended conformation. These findings indicate that, despite the common Cα-methylated and Cβ-branched features, (αMe)Dip and (αMe)Val are characterized by partially divergent conformational bias.
- Lapena, Yolanda,Lopez, Pilar,Cativiela, Carlos,Kaptein, Bernard,Broxterman, Quirinus B.,Kamphuis, Johan,Mossel, Eric,Peggion, Cristina,Formaggio, Fernando,Crisma, Marco,Toniolo, Claudio
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p. 631 - 636
(2007/10/03)
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- QUINAZOLINE DERIVATIVES AND APPLICATIONS THEREOF
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A chymase inhibitor containing as its effective ingredient a quinazoline derivative, or a pharmaceutically acceptable salt thereof, having the formula (1): STR1 and a pharmaceutical preparation for the prevention of cardiac and circulatory system diseases derived from abnormal exacerbation of Ang II production containing the same as its effective ingredient.
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- Compositions and methods for enhanced drug delivery
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The present invention relates to methods of delivering pharmaceutical agents across membranes, including the skin layer or mucosal membranes of a patient. A pharmaceutical agent is covalently bonded to a chemical modifier, via a physiologically cleavable bond, such that the membrane transport and delivery of the agent is enhanced.
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- Building Units for N-Backbone Cyclic Peptides. 3. Synthesis of Protected Nα-(ω-Aminoalkyl)amino Acids and Nα-(ω-Carboxyalkyl)amino Acids
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An improved synthesis of a family of amino acids that contain ω-aminoalkyl groups and of a new family containing ω-carboxyalkyl groups linked to the α-amine is described. The synthesis was performed by alkylation of suitably monoprotected alkylenediamines and protected ω-amino acids with triflates of α-hydroxy acid esters. The reaction proceeded with inversion of configuration yielding optically pure products. The Nα-(ω-aminoalkyl)amino acids and Nα-(ω-carboxyalkyl)amino acids were orthogonally protected to allow their incorporation into peptides by solid-phase peptide synthesis (SPPS) methodology.
- Muller, Dan,Zeltser, Irena,Bitan, Gal,Gilon, Chaim
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p. 411 - 416
(2007/10/03)
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- Synthesis of enantiomerically pure (2R,5S)- and (2R,5R)-5-hydroxypipecolic acid from glycinate Schiff bases
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An asymmetric synthesis of cis- and trans-5-hydroxy-(D)-pipecolic acid, starting from glycinate Schiff bases is described. The approach involves the stereoselective alkylation to generate an unsaturated side chain which on cyclisation leads to the desired trans- or cis-5-hydroxy-(D)-pipecolic acid.
- Hoarau, Sylvie,Fauchere, Jean Luc,Pappalardo, Louis,Roumestant, Marie Louise,Viallefont, Philippe
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p. 2585 - 2593
(2007/10/03)
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- An Approach to a Synthetic Carboxylate-binding Pocket Based on β-Avoparcin
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An approach to a macrocyclic lactam designed to bind to a carboxylate anion is described.The diaryl ether 8 was synthesised by Ullmann coupling of the protected 3-hydroxyphenylglycine derivative 7 and (E)-4-bromocinnamic acid methyl ester.Elaboration of an optically pure (R)-tyrosine synthon was achieved by transfer of electrophilic azide to the N-acyl oxazolidinone 12.The synthesis of a model system is also described.
- Stone, Martin J.,Dyk, Martha S. van,Booth, Paul M.,Williams, Dudley H.
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p. 1629 - 1635
(2007/10/02)
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- 4-Methoxy-2,3,6-trimethylbenzenesulfonyl (Mtr): a New Amino and Imidazole Protecting Group in Peptide Synthesis
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The 4-methoxy-2,3,6-trimethylbenzenesulfonyl (Mtr) group was introduced as a protecting group for the amino function, especially the ε-amino function of lysine, and the imidazole ring of histidine.The Nε-Mtr group was removable by dilute methanesulfonic acid-containing trifluoroacetic acid-thioanisole, but was stable to trifluoroacetic acid or catalytic hydrogenation.The Nim-Mtr group was removable by trifluoroacetic acid-dimethylsulfide or 1-hydroxybenzotriazole, but was more stable than the Nim-Tos or the Nim-Mbs group with triethylamine.To examine the usefulness of the Mtr group as a protecting group for use in peptide synthesis, mastoparan X and chicken gastrin releasing peptide (c-GRP) were synthesized, and this group was found to be very convenient for general solution synthesis.In particular, the introduction of Lys(Mtr) made possible a new strategy in peptide synthesis.Keywords-4-methoxy-2,3,6-trimethylbenzenesulfonyl (Mtr); Nε-4-methoxy-2,3,6-trimethylbenzenesulfonyllysine; Nim-4-methoxy-2,3,6-trimethylbenzenesulfonylhistidine; methanesulfonic acid-trifluoroacetic acid-thioanisole deprotection; trifluoroacetic acid-dimethylsulfide deprotection; mastoparan X; chicken gastrin releasing peptide
- Wakimasu, Mitsuhiro,Kitada, Chieko,Fujino, Masahiko
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p. 2766 - 2779
(2007/10/02)
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- Process for the preparation of 6-hydroxymethyl-2-(β-aminoethylthio)-1-carbadethiapen-2-em-3-carboxylic acid
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Diclosed is a process for preparing the antibiotic 6-hydroxymethyl-2-(β-aminoethylthio)-1-carbadethiapen-2-em-3-carboxylic acid (I) STR1 and its pharmaceutically acceptable salt and ester derivatives.
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