- A highly efficient flow reactor process for the synthesis of N-Boc-3,4-dehydro-l-proline methyl ester
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The multi-step preparation of N-Boc-3,4-dehydro-l-proline methyl ester using a modular flow reactor is reported. The use of immobilised reagents and scavengers in pre-packed glass tubes allows us to obtain the pure product in 87% overall yield, 97% purity, and >98% enantiomeric excess without any additional purification step. Our flow-based protocol enables the rapid multi-gram synthesis (about 9 g/12 h) of the desired product.
- Tamborini, Lucia,Conti, Paola,Pinto, Andrea,Micheli, Carlo De
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Read Online
- Synthesis of acylhydrazino-peptomers, a new class of peptidomimetics, by consecutive Ugi and hydrazino-Ugi reactions
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Herein we describe a versatile approach for the synthesis of acylhydrazino-peptomers, a new class of peptidomimetics. The key idea in this approach is based on a simple route using a one-pot hydrazino-Ugi four-component reaction followed by a hydrazinolysis or hydrolysis reaction and subsequent hydrazino-Ugi reaction or classical Ugi reaction for the construction of acyclic acylhydrazino-peptomers. The consecutive multicomponent reactions produced a variety of acylhydrazino-peptomers in moderate to excellent yields (47-90%). These compounds are multifunctional intermediates that can be further functionalized to obtain new peptidomimetics with potential biological activity.
- Barreto, Angélica De Fátima S.,Dos Santos, Veronica Alves,Andrade, Carlos Kleber Z.
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Read Online
- Preparation method of carboxylic ester compound
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The invention relates to a preparation method of a carboxylic ester compound, which comprises the following steps: reacting carboxylic acid with methanol in air under the catalysis of nitrite to obtain an ester compound, the preparation method disclosed by the invention has the advantages of rich raw material sources, cheap and easily available catalyst, mild reaction conditions, simplicity and convenience in operation and the like, a series of fatty carboxylic acids can be modified with high yield, and particularly, the traditional esterification method is generally not suitable for esterification of drug molecules. By utilizing the method, a series of known drug molecules can be modified, so that a shortcut is provided for discovering new drug molecules.
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Paragraph 0042-0043
(2021/03/30)
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- Green Esterification of Carboxylic Acids Promoted by tert-Butyl Nitrite
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In this work, the green esterification of carboxylic acids promoted by tert-butyl nitrite has been well developed. This transformation is compatible with a broad range of substrates and exhibits excellent functional group tolerance. Various drugs and substituted amino acids are applicable to this reaction under near neutral conditions, with good to excellent yields.
- Cheng, Xionglve,Jiang, Gangzhong,Li, Xingxing,Tao, Suyan,Wan, Xiaobing,Zhao, Yanwei,Zheng, Yonggao
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supporting information
p. 2713 - 2718
(2021/06/25)
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- Electrochemical Dimethyl Sulfide-Mediated Esterification of Amino Acids
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Dimethyl sulfide-mediated electrochemical synthetic strategy for esterification of amino acids has been reported. A series of amino acids could react smoothly with alcohols, affording the desired esterification products with good efficiency. Importantly, the tolerance of peptides and gram-scale synthesis shed light on the utility of this protocol. Mechanistically, the dimethyl sulfide as a mediator plays an essential role in the transformation of amino acids.
- Li, Yongli,Wang, Huamin,Zhang, Heng,Lei, Aiwen
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supporting information
p. 3023 - 3028
(2021/08/30)
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- N-Alkenylation of hydroxamic acid derivatives with ethynyl benziodoxolone to synthesizecis-enamides through vinyl benziodoxolones
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The stereoselective synthesis ofcis-β-N-alkoxyamidevinyl benziodoxolones (cis-β-N-RO-amide-VBXs) fromO-alkyl hydroxamic acids in the presence of an ethynyl benziodoxolone-acetonitrile complex (EBX-MeCN) is reported herein. The reaction was performed under mild conditions including an aqueous solvent, a mild base, and room temperature. The reaction tolerated variousO-alkyl hydroxamic acids derived from carboxylic acids, such as amino acids, pharmaceuticals, and natural products. Vinyl dideuteratedcis-β-N-MeO-amide-VBXs were also synthesized using deuterium oxide as the deuterium source. Valine-derivedcis-β-N-MeO-amide-VBX was stereospecifically derivatized to hydroxamic acid-derivedcis-enamides without the loss of stereoselectivity or reduction in the deuterium/hydrogen ratio.
- Shimbo, Daisuke,Maruyama, Toshifumi,Tada, Norihiro,Itoh, Akichika
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supporting information
p. 2442 - 2447
(2021/04/02)
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- An efficient, stereocontrolled and versatile synthetic route to bicyclic partially saturated privileged scaffolds
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Herein, we describe the development of a simple, high yielding and stereocontrolled strategy for the synthesis of a series of triazolopiperazines and other biologically relevant fused scaffolds from optically active amino acids. This route was applied to the synthesis of 22 scaffolds containing new, previously inaccessible vectors and used to access a novel analogue of ganaplacide.
- Bond, Andrew D.,Hanby, Abigail R.,King, Thomas A.,Moss, Thomas A.,Sore, Hannah F.,Spring, David R.,Stewart, Hannah L.
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supporting information
p. 6818 - 6821
(2020/07/04)
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- Selective conversion of primary amides to esters promoted by KHSO4
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Primary amides, either aliphatic or aromatic, are easily converted to the corresponding esters via reflux in lower primary alcohols in the presence of KHSO4. Secondary amides lead to complicated mixtures under analogous conditions, whereastertiary amides were inert. Use of isopropyl alcohol resulted inthe formation of product atslower rate and lower yieldalong withside products, whereas, use of tertiary alcoholsdid not give successful conversion andallyl and benzyl alcohol provided complex mixtures.
- Sattenapally, Narsimha,Sharma, Jhanvi,Hou, Yuqing
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p. 174 - 183
(2018/09/10)
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- Consecutive hydrazino-Ugi-azide reactions: Synthesis of acylhydrazines bearing 1,5-disubstituted tetrazoles
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Isocyanide-based multicomponent reactions (IMCRs) allow the construction of relatively complex molecules through a one-pot synthesis. The combination of IMCRs in a consecutive or sequential fashion further extends the complexity of the molecules obtained. Herein, we report the efficient application of this approach to the synthesis of acylhydrazines bearing 1,5-disubstituted tetrazoles. Our strategy was accomplished in only three steps: first, a one-pot hydrazino-Ugi-azide four-component reaction; second a hydrazinolysis and finally an additional hydrazino-Ugi-azide reaction. This sequence provides the title compounds in moderate to excellent yields. The products synthesized herein contain functional groups within their structures that can be easily modified to obtain new acylhydrazino 1,5-disubstituted tetrazoles.
- De Fátima Barreto, Angélica S.,Dos Santos, Veronica Alves,Zandrade, Carlos Kleber
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p. 2596 - 2602
(2018/01/17)
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- A Simple, efficient, Catalyst-Free and Solvent-Less Microwave-Assisted process for N-Cbz Protection of Several amines
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A simple, green and chemo-selective method for the N-benzyloxycarbonylation of amines, β-amino alcohols, α-amino esters and sulfonamides has been developed under microwave irradiation. Good to excellent yields of the N-benzyloxy-carbamates compounds were obtained in short times without any side products.
- Aouf, Zineb,Mansouri, Rachida,Lakrout, Salah,Berredjem, Malika,Aouf, Nour-Eddine
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p. 151 - 156
(2017/08/02)
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- N-Urethane protection of amines and amino acids in an ionic liquid
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An efficient, solvent-free protocol for the N-fluorenylmethoxycarbonylation and N-benzyloxycarbonylation of amines is described. The reaction of aliphatic and aromatic amines with FmocOSu and Cbz-Osu in [Bmim][BF4] at room temperature afforded the corresponding N-urethane derivatives in excellent yields and do not require any further purification. The method has been extended to the N-Fmoc and N-Cbz protection of amino acids. Absence of bases, very short reaction times, high yields, selectivity and ease of product separation are some advantages of this protocol.
- Di Gioia,Gagliardi,Leggio,Leotta,Romio,Liguori
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p. 63407 - 63420
(2015/08/11)
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- Synthesis and applications in Henry reactions of novel chiral thiazoline tridentate ligands
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Several novel chiral tridentate ligands containing thiazoline were efficiently synthesized from commercially available l=cysteine in high yield. These ligands were subsequently applied to the asymmetric Henry reaction of nitromethane and various aldehydes. It was found that the structures of the thiazoline ligands had a significant influence on the enantioselectivity. It was shown that the optimal catalyst for this reaction was a ligand complexed with CuCl, which was formed from chiral thiazoline with chiral aminoalcohol. At -20°C, with 10 mol% of this ligand, a product with (S)-configuration was isolated in 93% yield and 98% enantiomeric excess.
- Shi, Ye,Li, Yang,Sun, Jingbo,Lai, Qi,Wei, Chiyu,Gong, Zhiyong,Gu, Qiang,Song, Zhiguang
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p. 661 - 667
(2015/09/28)
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- One-step C-terminal deprotection and activation of peptides with peptide amidase from stenotrophomonas maltophilia in neat organic solvent
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Chemoenzymatic peptide synthesis is a rapidly developing technology for cost effective peptide production on a large scale. As an alternative to the traditional C→N strategy, which employs expensive N-protected building blocks in each step, we have investigated an N→C extension route that is based on activation of a peptide C-terminal amide protecting group to the corresponding methyl ester. We found that this conversion is efficiently catalysed by Stenotrophomonas maltophilia peptide amidase in neat organic media. The system excludes the possibility of internal peptide cleavage as the enzyme lacks intrinsic protease activity. The produced peptide methyl ester was used for peptide chain extension in a kinetically controlled reaction by a thermostable protease.
- Arif, Muhammad I.,Toplak, Ana,Szymanski, Wiktor,Feringa, Ben L.,Nuijens, Timo,Quaedflieg, Peter J. L. M.,Wu, Bian,Janssen, Dick B.
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p. 2197 - 2202
(2014/07/21)
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- Solventless mechanosynthesis of N-protected amino esters
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Mechanochemical derivatizations of N- or C-protected amino acids were performed in a ball mill under solvent-free conditions. A vibrational ball mill was used for the preparation of N-protected α- and β-amino esters starting from the corresponding N-unmasked precursors via a carbamoylation reaction in the presence of di-tert-butyl dicarbonate (Boc2O), benzyl chloroformate (Z-Cl) or 9-fluorenylmethoxycarbonyl chloroformate (Fmoc-Cl). A planetary ball mill proved to be more suitable for the synthesis of amino esters from N-protected amino acids via a one-pot activation/esterification reaction in the presence of various dialkyl dicarbonates or chloroformates. The spot-to-spot reactions were straightforward, leading to the final products in reduced reaction times with improved yields and simplified work-up procedures.
- Konnert, Laure,Lamaty, Frederic,Martinez, Jean,Colacino, Evelina
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p. 4008 - 4017
(2014/05/20)
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- Total synthesis of PDE-I and -II by copper-mediated double aryl amination This paper is dedicated to Professor Teruaki Mukaiyama in celebration of the 40th anniversary of the Mukaiyama aldol reaction
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A concise total synthesis of PDE-I and -II featuring copper-mediated double aryl amination with the combination of CuI, CsOAc, and Cs2CO 3 is described. The highly substituted pyrroloindole skeleton was constructed by a one-pot five-step sequence including double aryl amination, β-elimination, deprotection of a Cbz group, and unexpected formation of an indole via removal of an Ns group followed by rearomatization. The undesired elimination of the protecting group (Ns group) was hampered by using the Boc group as a protecting group in the second-generation synthesis, which excluded the reduction of the indole required in the first-generation synthesis.
- Okano, Kentaro,Mitsuhashi, Nakako,Tokuyama, Hidetoshi
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p. 10946 - 10954
(2014/01/06)
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- Enantioselective synthesis of anti-β-hydroxy-α-amido esters by asymmetric transfer hydrogenation in emulsions
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Herein, we present two methods for an asymmetric transfer hydrogenation through the dynamic kinetic resolution of α-amido-β-ketoesters. These procedures yield the corresponding anti-β-hydroxy-α-amido esters in good yields and with good diastereo- and enantioselectivities. First, the scope of the reduction of α-amido-β-ketoesters by using triethylammonium formate azeotrope is examined. Then, an emulsion technology with sodium formate is explored, which allows for broader substrate scope, faster reaction times, and lower catalyst loading. Furthermore, these reactions are operationally simple and can be set up in air.
- Seashore-Ludlow, Brinton,Villo, Piret,Somfai, Peter
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supporting information; experimental part
p. 7219 - 7223
(2012/07/13)
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- Mild construction of 3-methyl tetramic acids enabling a formal synthesis of palau'imide
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A general method to construct 3-methyl-4-O-methylated tetramic acids displaying a C-5 stereocenter is presented. The synthetic sequence employs a SmI2-mediated cyclization, whereby the chirality of the emerging tetramic acid core is retained from the starting chiral amino acid. Application to palau'imide is discussed.
- Bai, Wen-Ju,Jackson, Stephen K.,Pettus, Thomas R. R.
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supporting information; experimental part
p. 3862 - 3865
(2012/09/22)
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- On the reactivity of imidazole carbamates and ureas and their use as esterification and amidation reagents
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The optimization, substrate scope, and mechanism of esterification and amidation of carboxylic acids mediated by imidazole-based reagents are discussed. The innate reactivity of carbonylimidazole reagents with a range of nucleophiles is also explored. New reagents developed for the synthesis of α,β-unsaturated esters are described, as are reagents for the preparation of tertiary amides directly from carboxylic acids.
- Heller, Stephen T.,Sarpong, Richmond
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experimental part
p. 8851 - 8859
(2011/12/02)
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- Parallel synthesis of an oligomeric imidazole-4, 5-dicarboxamide library
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A library of oligomeric compounds was synthesized based on the imidazole-4, 5-dicarboxylic acid scaffold along with amino acid esters and chiral diamines derived from amino acids. The final compounds incorporate nonpolar amino acids (Leu, Phe, Trp), polar amino acids (Ser, Asp, Arg), and neutral amino acids (Gly, Ala), and were designed to be useful in screening for inhibitors of protein-protein interactions. Many of the protected and deprotected oligomers show evidence of conformational isomers persistent at room temperature in aqueous solution. A total of 317 final oligomers, out of 441 targeted compounds, were obtained in high analytical purity and of sufficient quantity to submit them for high-throughput screening as part of the NIH Roadmap.
- Xu, Zhigang,DiCesare, John C.,Baures, Paul W.
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supporting information; experimental part
p. 248 - 254
(2010/08/19)
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- Total synthesis of PDE-II by copper-mediated double amination
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A concise total synthesis of PDE-II featuring copper-mediated double aryl amination with the combination of CuI, CsOAc, and Cs2CO3 is described. The highly substituted pyrroloindole skeleton was constructed by a one-pot five-step sequence including double aryl amination, β-elimination, deprotection of a Cbz group, and removal of an Ns group followed by rearomatization.
- Okano, Kentaro,Mitsuhashi, Nakako,Tokuyama, Hidetoshi
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supporting information; experimental part
p. 2641 - 2643
(2010/07/09)
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- Chemoselective esterification and amidation of carboxylic acids with imidazole carbamates and ureas
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Imidazole carbamates and ureas were found to be chemoselective esterification and amidation reagents. A wide variety of carboxylic acids were converted to their ester or amide analogues by a simple synthetic procedure in high yields.
- Heller, Stephen T.,Sarpong, Richmond
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supporting information; experimental part
p. 4572 - 4575
(2010/12/25)
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- Synthesis and characterisation of some new N-glycosides containing substituted pyridopyrimidinone, pyrimidopyridazinone, thiazolopyrimidinone and quinolizin-4-one moiety
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A series of new N-glycosides (D-glucosides, D-mannosides, L-and D-arabinosides, D-xylosides and one D-galactoside) containing heterocyclic moiety have been prepared by reaction of the corresponding heterocyclic amines with pyranoses in boiling methanol. The structures of the prepared compounds have been studied by means of proton and carbon NMR spectroscopy. In the most cases the products existed in DMSO solution as the single anomers. The Japan Institute of Heterocyclic Chemistry.
- Simunek, Petr,Svete, Jurij,Stanovnik, Branko
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experimental part
p. 2477 - 2491
(2011/04/17)
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- Synthesis of proline-modified analogues of the neuroprotective agent glycyl-L-prolyl-glutamic acid (GPE)
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The synthesis of ten proline-modified analogues of the neuroprotective tripeptide GPE is described. Five of the analogues incorporate a proline residue with a hydrophobic group at C-2 and two further analogues have this side chain locked into a spirolactam ring system. The pyrrolidine ring was also modified by replacing the γ-CH2 group with sulfur and/or incorporation of two methyl groups at C-5.
- Harris, Paul W.R.,Brimble, Margaret A.,Muir, Victoria J.,Lai, Michelle Y.H.,Trotter, Nicholas S.,Callis, David J.
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p. 10018 - 10035
(2007/10/03)
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- Broadening of the substrate tolerance of α-chymotrypsin by using the carbamoylmethyl ester as an acyl donor in kinetically controlled peptide synthesis
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In the kinetically controlled approach of peptide synthesis mediated by α-chymotrypsin, the broadening of the protease's substrate tolerance is achieved by switching the acyl donor from the conventional methyl ester to the carbamoylmethyl ester. Thus, as a typical example, the extremely low coupling efficiency obtained by employing the methyl ester of an inherently poor amino acid substrate, Ala, is significantly improved by the use of this particular ester. Its ameliorating effect is observed also in the couplings of other amino acid residues such as Gly and Ser as carboxy components.
- Miyazawa, Toshifumi,Tanaka, Kayoko,Ensatsu, Eiichi,Yanagihara, Ryoji,Yamada, Takashi
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- The synthesis of methyl 2-(benzyloxycarbonyl)amino-3- dimethylaminopropenoate. The synthesis of trisubstituted pyrroles, 3-amino- 2H-pyran-2-ones, fused 2H-pyran-2-ones and 4H-pyridin-4-ones
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Methyl 2-(benzyloxycarbonyl)amino-3-dimethylaminopropenoate (2) was prepared from methyl N-(benzyloxycarbonyl)glycinate (1) and t- butoxybis(dimethylamino)methane, and used as a reagent for preparation of substituted 3-(benzyloxycarbonyl)amino-4H-quinolizin-4-ones 5 and 6, -2H- pyran-2-ones 17-19, -2H-1-benzopyran-2-ones 28-31, and -naphthopyrans 32-35, -2H-pyrano[3,2-c]pyridine-2,5-dione 46, -pyrano[4,3-b]pyran-2,5-dione 47, - pyrano[3,2-c]benzopyran-2,5-dione 48, -pyrano[2,3-c]pyrazol-6-ones 49 and 50, -pyrano[2,3-d]pyrimidin-7-ones 51 and 52 derivatives. In the reaction of 2 with 1,3-diketones trisubstituted pyrroles 14-16 were formed. Selective removal of benzyloxycarbonyl group was achieved by catalytic transfer hydrogenation with Pd/C in the presence of cyclohexene to afford free 3- amino compounds 7, 8, 20, 36-38 and 53-57 in yields better than 80%.
- Toplak, Renata,Svete, Jurij,Stanovnik, Branko,Golic Grdadolnik, Simona
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p. 225 - 235
(2007/10/03)
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- A Convenient synthesis of phosphonic anhydrides - Trimers [RPO2]3 (R = tert-butyl, 2-methylphenyl, 2,4,6-trimethylphenyl): Their structures and reaction products
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By reaction of RP(O)Cl2 with RP(O)(OSiMe3)2, phosphonic anhydrides (RPO2)3 (R = tBu, 2-methylphenyl, 2,4,6-trimethylphenyl) 1a-c are conveniently obtained. In contrast to 1b and 1c, compound 1a is remarkably stable against protolysis. Intermediates of hydrolysis of 1a, namely tris(tert-butyl)triphosphonic acid (2) and bis(tert-butyl)diphosphonic acid (3), can also be isolated in good yield. The structures of 1-3 were determined mainly by NMR spectroscopy (1H, 13C, 31P). Assuming an energetic preference for the chair conformations in solution, and considering the steric requirements of the bulky substituents R, configurations Ia (point group Cs, two R in equatorial positions) for 1a and b, and IIa (point group C3vi all R equatorial) for 1c are suggested. - Reaction of 1a with N-benzyloxycarbonylglycine (4) in methanol affords strong evidence that in the first step of peptide synthesis with (RPO2)3, a mixed anhydride of triphosphonic acid and the N-protected amino acid is formed. - The crystal structure of 1a (monoclinic, space group P21/n) widely corresponds to the suggested configuration Ia, but reveals an envelope conformation for the six-membered ring with a P3O2 plane in the crystal. In the crystal structure of the octahydrate of the disodium salt of 2 (monoclinic, space group P21/c), it can be seen that the polar end groups of the anions [tBu3P3O7]2- together with the water molecules and the Na+ cations form hydrogen-bonded double-layers, strictly separated from each other by the non-polar tert-butyl groups of the anions.
- Diemert, Klaus,Kuchen, Wilhelm,Poll, Wolfgang,Sandt, Frank
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p. 361 - 366
(2007/10/03)
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- N-(benzyloxycarbonyl)glycine esters and amides as new anticonvulsants
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Glycine is a small neutral amino acid exhibiting weak anticonvulsant activities in vivo. Recently, studies have demonstrated that N- (benzyloxycarbonyl)glycine (1) antagonized seizures superior to glycine in addition to activity in the maximal electroshock (MES) test, a convulsive model where glycine is inactive. In the present study a series of ester and amide derivatives of 1 as well as esters of N-(3-phenylpropanoyl)glycine (5) have been prepared. The compounds were evaluated in the MES test as well as in several chemically induced seizure models. Among the derivatives investigated, N-(benzyloxycarbonyl)glycine benzylamide (16) was the most potent compound exhibiting an anticonvulsant activity in the MES test comparable to the drug phenytoin. Median effective doses (ED50) of 4.8 and 11.6 mg/kg were determined at 30 min and 3 h after ip administration, respectively. Compound 16 also effectively suppressed tonic seizures in different chemically induced models such as the strychnine, 3- mercaptopropionic acid, and pentylenetetrazole tests. Moreover, the compound studied here did not show acute neurotoxicity in the rotorod test up to a dose of 150 mg/kg. It is concluded that N-(benzyloxycarbonyl)glycine amides, especially 16, are potent anticonvulsant agents.
- Geurts, Muriel,Poupaert, Jacques H.,Scriba, Gerhard K. E.,Lambert, Didier M.
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- Conversion of carbonimidodithioates to carbamates
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Carbonimidodithioates derived from primary amines or α-amino acid esters have been converted to N-benzyloxycarbonyl derivatives under mild conditions by treatment first with sodium benzyl alcoholate and then with water. N-Benzyloxycarbonyl α-amino acids have been generated from the methyl esters by alkaline hydrolysis or from the allyl esters by Pd0-catalysed de-allylation.
- Anbazhagan, Mariappan,Reddy, T. Indrasena,Rajappa, Srinivasachari
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p. 1623 - 1627
(2007/10/03)
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- Preparation of protected α-alkoxyglycines
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N-Carbobenzoxy-α-alkoxyglycine esters were synthesized by H2SO4-catalyzed O-alkylation of N-carbobenzoxy-α-hydroxyglycine and also by base treatment of N-carbobenzoxy-N-chloroglycine methyl ester in the corresponding alcohol. Saponification of the protected α-alkoxyglycines gave free acids which can be used for the synthesis of α-alkoxyglycine residue-containing peptides.
- Kawai, Masao,Hosoda, Kouji,Omori, Yoshimasa,Yamada, Keiichi,Hayakawa, Shoko,Yamamura, Hatsuo,Butsugan, Yasuo
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p. 1545 - 1554
(2007/10/03)
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- Single-step enzymatic conversion of peptide amides to esters
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It is shown that the C-terminal amide groups in N-protected peptides could be efficiently replaced by ester groups via kinetically-controlled papain-catalyzed acyl transfer reactions in aqueous methanol. The specificity of papain was substantially shifted towards the cleavage of C-terminal amide bond in dipeptide substrates by methanol, thus suppressing undesired peptide bond cleavage during esterification.
- Meos, Helle,Haga, Mati,Tougu, Vello
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p. 2343 - 2346
(2007/10/02)
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- Alkoxycarbonyl groups transfer to amines by the N,N'-dibenzyl- and N,N'-di-tert-butyl-carbamates of cyclic thioureas
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The use of the dicarbamates of cyclic thioureas as alkoxycarbonyl-transfer reagents for the protection of amino groups is described.
- Matsumura, Noboru,Noguchi, Akiko,Kitayoshi, Aya,Inoue, Hiroo
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p. 2953 - 2954
(2007/10/03)
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- Novel esterifying agents, and their production and use
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A process for esterifying organic carboxylic acids which comprises reacting an organic carboxylic acid with a carbonic acid ester of the formula: EQU1 wherein R is an organic group and X and Y are each a negative group in the presence of a basic substance to make esterified the carboxyl group in the organic carboxylic acid. The process is advantageous in affording the objective carboxylic ester in a good yield within a short time by a simple operation under a mild reaction condition.
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