An efficient and novel procedure for the preparation of pyrazolo[3,4-b]pyridine derivatives through multi-component reaction of aldehyde, 5-amino-3-methyl-1-phenylpyrazole and malononitrile or cyanoacetate in [bmim][B...An efficient and novel procedure for the preparation of pyrazolo[3,4-b]pyridine derivatives through multi-component reaction of aldehyde, 5-amino-3-methyl-1-phenylpyrazole and malononitrile or cyanoacetate in [bmim][BF4] is described in this paper. Advantages of the method presented here include mild conditions, high yields together with a green nature and ease of recovery and reuse of the reaction medium.展开更多
Oxonium ylide intermediates generated from α-diazocarbonyl compounds and water were trapped by Zn（Ⅱ）-activated α- dicarbonyl compounds. The reaction gave α,β-dihydroxyl acid derivatives in moderate yield.
Peptide nucleic acids (PNA) oligomers were synthesized in most cases by peptide synthesis from N-protected monomers. In this work a new method of obtaining PNA monomer by Ugi four-component condensation reaction was t...Peptide nucleic acids (PNA) oligomers were synthesized in most cases by peptide synthesis from N-protected monomers. In this work a new method of obtaining PNA monomer by Ugi four-component condensation reaction was tested by solid-phase synthesis. The Fmoc protected PNA monomer was build up with thymin-1-yl acetic acid, 3-methylbutyl aldehyde, Fmoc protected aminoethyl isocyanide and Gly-Wang resin.展开更多
The Ugi four-component reaction (U-4CR) was utilized to prepare divalent and trivalent cluster mannosides. Thus, two target compounds 6 and 8 were obtained efficiently using carboxymethyl 2, 3, 4, 6-tetra-O-acetyl--D-...The Ugi four-component reaction (U-4CR) was utilized to prepare divalent and trivalent cluster mannosides. Thus, two target compounds 6 and 8 were obtained efficiently using carboxymethyl 2, 3, 4, 6-tetra-O-acetyl--D-mannopyranoside 4 as acid component, and 1, 6-hexanediamine or tris(2-aminoethyl)amine as the multivalent scaffolds.展开更多
It is discovered a new three-, four-component Petasis, Passerini, Hantzsch, Kabachnic-Fields, Ugi reactions with of arsine, stibine and bismuthine in organometallic chemistry. Modifications were replaced to a nitrogen...It is discovered a new three-, four-component Petasis, Passerini, Hantzsch, Kabachnic-Fields, Ugi reactions with of arsine, stibine and bismuthine in organometallic chemistry. Modifications were replaced to a nitrogen atom of classical reactions of atoms of phosphorus, arsenic, antimony and bismuth. It has been proposed a new mechanism for possible reactions.展开更多
A thermally-induced multi-component reaction of CF_(3)-substituted imidoyl sulfoxonium ylides(TFISYs),amines and(triphenylphosphonio)difluoroacetate(PDFA)has been developed,allowing a facile access to 2-trifluoromethy...A thermally-induced multi-component reaction of CF_(3)-substituted imidoyl sulfoxonium ylides(TFISYs),amines and(triphenylphosphonio)difluoroacetate(PDFA)has been developed,allowing a facile access to 2-trifluoromethyl-4-aminoquinolines in high yields.The reaction proceeds smoothly with or without the addition of sulfur and utilizes difluorocarbene as a C1 synthon under simply heating conditions.Mechanistic study reveals that in-situ generated thiocarbonyl fluoride,isothiocyanate or gem-difluoroalkene might act as the key reaction intermediates.展开更多
Paclitaxel(Taxol^(@))as a cornerstone of chemotherapy remains in high demand.The semi-synthesis of paclitaxel via coupling of Taxus leaf-produced baccatin III and manually synthesized isoserine(C-13 side chain)is one ...Paclitaxel(Taxol^(@))as a cornerstone of chemotherapy remains in high demand.The semi-synthesis of paclitaxel via coupling of Taxus leaf-produced baccatin III and manually synthesized isoserine(C-13 side chain)is one of the solutions to avoid environmental damage caused by the sacrifice of the whole Taxus brevifolia.A green synthesis of the C-13 side chain is pivotal to the green production of paclitaxel.We herein report a green synthesis of isoserine derivatives and the semi-synthesis of paclitaxel via a straightforward assembly of isoserines based on an Rh2(TPA)3(OAc)/CPA1 co-catalyzed asymmetric multi-component reaction of ethyl diazoacetate,triethyl silanol and N-(anthrancen-9-ylmethyl)benzaldimine.The method is featured by improved atom economy,effective mass yield,and environmental factors compared to our previous racemic method and BMS company's semi-synthesis method.And the method allows for rapid access to paclitaxel derivatives with varied C-13 side chains.展开更多
基金the National Natural Science Foundation of China(No.20573034).
文摘An efficient and novel procedure for the preparation of pyrazolo[3,4-b]pyridine derivatives through multi-component reaction of aldehyde, 5-amino-3-methyl-1-phenylpyrazole and malononitrile or cyanoacetate in [bmim][BF4] is described in this paper. Advantages of the method presented here include mild conditions, high yields together with a green nature and ease of recovery and reuse of the reaction medium.
基金supported by National Science Foundation of China(No.20772033)China postdoctoral Science Foundation(No.20080440607)
文摘Oxonium ylide intermediates generated from α-diazocarbonyl compounds and water were trapped by Zn（Ⅱ）-activated α- dicarbonyl compounds. The reaction gave α,β-dihydroxyl acid derivatives in moderate yield.
基金This work was supposed by the National Basic Research Program(973 Program)from the Ministry of Science and Technology of China(G1998051114)the National Natural Science Foundation of China(20272004)
文摘Peptide nucleic acids (PNA) oligomers were synthesized in most cases by peptide synthesis from N-protected monomers. In this work a new method of obtaining PNA monomer by Ugi four-component condensation reaction was tested by solid-phase synthesis. The Fmoc protected PNA monomer was build up with thymin-1-yl acetic acid, 3-methylbutyl aldehyde, Fmoc protected aminoethyl isocyanide and Gly-Wang resin.
文摘The Ugi four-component reaction (U-4CR) was utilized to prepare divalent and trivalent cluster mannosides. Thus, two target compounds 6 and 8 were obtained efficiently using carboxymethyl 2, 3, 4, 6-tetra-O-acetyl--D-mannopyranoside 4 as acid component, and 1, 6-hexanediamine or tris(2-aminoethyl)amine as the multivalent scaffolds.
文摘It is discovered a new three-, four-component Petasis, Passerini, Hantzsch, Kabachnic-Fields, Ugi reactions with of arsine, stibine and bismuthine in organometallic chemistry. Modifications were replaced to a nitrogen atom of classical reactions of atoms of phosphorus, arsenic, antimony and bismuth. It has been proposed a new mechanism for possible reactions.
基金Foundation of the Key Laboratory of Pesticide Chemistry and Application,Ministry of Agriculture ( MOA ) ( No. MOAPCA200903)National Natural Science Foundation of China ( Nos. 20872071,20911120069 )+5 种基金Key Project of the Tianjin Natural Science Foundation ( 10JCZDJC17500 )The National Key Project for Basic Research ( 2010CB126105 )National Key Technology Research and Development Program ( 2011BAE06B05 )Common Specialized Research Fund of China Agriculture ( nyhyzx3-21,201103016 and 201003029)The Russian Foundation for Basic Research ( Nos RFBR 08-03-00376 a and RFBR /NNSF 08-03-92208 a)the Foundation of Achievements Transformation and Spreading of Tianjin Agricultural Science and Technology ( No. 201002250)
基金financial support from K.C.Wong Education Foundation(GJTD-2020-08).
文摘A thermally-induced multi-component reaction of CF_(3)-substituted imidoyl sulfoxonium ylides(TFISYs),amines and(triphenylphosphonio)difluoroacetate(PDFA)has been developed,allowing a facile access to 2-trifluoromethyl-4-aminoquinolines in high yields.The reaction proceeds smoothly with or without the addition of sulfur and utilizes difluorocarbene as a C1 synthon under simply heating conditions.Mechanistic study reveals that in-situ generated thiocarbonyl fluoride,isothiocyanate or gem-difluoroalkene might act as the key reaction intermediates.
基金Support for this research from the National Natural Science Foundation of China(Nos.92056201 and 82003592)Guangdong Provincial Key Laboratory of Chiral Molecule and Drug Discovery(No.2019B030301005)The Program for Guangdong Introducing Innovative and Entrepreneurial Teams(No.2016ZT06Y337)and Zhujiang Talent Program Postdoctoral Funding Project is greatly acknowledged。
文摘Paclitaxel(Taxol^(@))as a cornerstone of chemotherapy remains in high demand.The semi-synthesis of paclitaxel via coupling of Taxus leaf-produced baccatin III and manually synthesized isoserine(C-13 side chain)is one of the solutions to avoid environmental damage caused by the sacrifice of the whole Taxus brevifolia.A green synthesis of the C-13 side chain is pivotal to the green production of paclitaxel.We herein report a green synthesis of isoserine derivatives and the semi-synthesis of paclitaxel via a straightforward assembly of isoserines based on an Rh2(TPA)3(OAc)/CPA1 co-catalyzed asymmetric multi-component reaction of ethyl diazoacetate,triethyl silanol and N-(anthrancen-9-ylmethyl)benzaldimine.The method is featured by improved atom economy,effective mass yield,and environmental factors compared to our previous racemic method and BMS company's semi-synthesis method.And the method allows for rapid access to paclitaxel derivatives with varied C-13 side chains.
