The one-pot three-component reaction of 2-aminobenzothiazole, benzaldehyde derivatives and β-ketoester, β-diketone or malonate derivatives in solvent-free conditions provides the corresponding pyrimido [2,1-b] benzo...The one-pot three-component reaction of 2-aminobenzothiazole, benzaldehyde derivatives and β-ketoester, β-diketone or malonate derivatives in solvent-free conditions provides the corresponding pyrimido [2,1-b] benzothiazole derivatives at 60?C in 60% - 72% yields without using any catalyst in an optimistic time.展开更多
A series of pyrido[2,3-d]pyrimidines derivatives have been prepared by one-pot three-component reaction of 4(6)-aminouracil, malononitrile and aromatic aldehydes. This efficient synthesis was done under microwave irra...A series of pyrido[2,3-d]pyrimidines derivatives have been prepared by one-pot three-component reaction of 4(6)-aminouracil, malononitrile and aromatic aldehydes. This efficient synthesis was done under microwave irradiation conditions (method A) and also using catalytic amount of diammonium hydrogen phosphate [(NH4)2HPO4] (DAHP) in aqueous media (method B). This procedure has the advantages of good yields, easy work-up, and benign environmentally friendly character. Reaction could proceed via domino Knoevenagel-Michael-cyclization reactions.展开更多
A simple and fastthree-component synthesis of new and biologically active hexahydro-2-quinolinecarboxylic acid scaf-fold 4 was carried out using cyclocondensation reaction of arylmethylidenepyruvic acids 1, 1,3-cycloh...A simple and fastthree-component synthesis of new and biologically active hexahydro-2-quinolinecarboxylic acid scaf-fold 4 was carried out using cyclocondensation reaction of arylmethylidenepyruvic acids 1, 1,3-cyclohexandiones 2 and ammonium acetate 3 under solvent-free conditions and at room temperature. This protocol has the advantages of facility, easy work-up, high yields, short reaction time and environmentally friendly character.展开更多
We wish to report a mild and efficient Crossed-Aldol reaction for the synthesis of α, ?-bis(substituted-ben- zylidene)cycloalkanones in the presence of catalytic amounts of covalently anchored sulfonic acid onto sil-...We wish to report a mild and efficient Crossed-Aldol reaction for the synthesis of α, ?-bis(substituted-ben- zylidene)cycloalkanones in the presence of catalytic amounts of covalently anchored sulfonic acid onto sil- ica gel under heterogeneous and solvent-free conditions. The present methodology offers several advantages such as excellent yields, simple procedure and work up steps, short reaction times and easy recovery of the catalyst. We have also demonstrated that the catalyst can be reused successfully.展开更多
Peptide bond formation has drawn more and more attention due to its importance in medicinal chemistry and drug discovery.Using active esters to construct peptide bonds is an indispensable strategy in this field.We her...Peptide bond formation has drawn more and more attention due to its importance in medicinal chemistry and drug discovery.Using active esters to construct peptide bonds is an indispensable strategy in this field.We herein report a fast and efficient amination reaction to synthesize peptides from catechol diesters.Catechol monoesters are good active esters in peptide synthesis due to the anchimeric assistance effect.In previously reported work,the amination reaction was inactivated if the 2-hydroxyl group in the catechol esters was functionalized.However,we found an unusual acceleration of the amination reactivity when the 2-hydroxyl group was functionalized as an ester group.The reaction can be complete in 2−3 min in some cases.This acceleration was found through experimental studies to not result from the anchimeric assistance effect.We proposed aπ*−π*interaction pathway between the two proximal ester groups.Some computational studies were made to support this assumption.展开更多
Dear Editor,Tumor angiogenesis is regulated by the binding of VEGF to receptors(VEGFRs).The major mediator of tumor angiogenesis is VEGFA,more commonly referred to as VEGF.VEGFR1 binds VEGF with higher affinity(10 tim...Dear Editor,Tumor angiogenesis is regulated by the binding of VEGF to receptors(VEGFRs).The major mediator of tumor angiogenesis is VEGFA,more commonly referred to as VEGF.VEGFR1 binds VEGF with higher affinity(10 times)than VEGFR2.1 However,the role of the VEGFR1 in VEGF-mediated angiogenesis remains a mystery.展开更多
文摘The one-pot three-component reaction of 2-aminobenzothiazole, benzaldehyde derivatives and β-ketoester, β-diketone or malonate derivatives in solvent-free conditions provides the corresponding pyrimido [2,1-b] benzothiazole derivatives at 60?C in 60% - 72% yields without using any catalyst in an optimistic time.
文摘A series of pyrido[2,3-d]pyrimidines derivatives have been prepared by one-pot three-component reaction of 4(6)-aminouracil, malononitrile and aromatic aldehydes. This efficient synthesis was done under microwave irradiation conditions (method A) and also using catalytic amount of diammonium hydrogen phosphate [(NH4)2HPO4] (DAHP) in aqueous media (method B). This procedure has the advantages of good yields, easy work-up, and benign environmentally friendly character. Reaction could proceed via domino Knoevenagel-Michael-cyclization reactions.
文摘A simple and fastthree-component synthesis of new and biologically active hexahydro-2-quinolinecarboxylic acid scaf-fold 4 was carried out using cyclocondensation reaction of arylmethylidenepyruvic acids 1, 1,3-cyclohexandiones 2 and ammonium acetate 3 under solvent-free conditions and at room temperature. This protocol has the advantages of facility, easy work-up, high yields, short reaction time and environmentally friendly character.
文摘We wish to report a mild and efficient Crossed-Aldol reaction for the synthesis of α, ?-bis(substituted-ben- zylidene)cycloalkanones in the presence of catalytic amounts of covalently anchored sulfonic acid onto sil- ica gel under heterogeneous and solvent-free conditions. The present methodology offers several advantages such as excellent yields, simple procedure and work up steps, short reaction times and easy recovery of the catalyst. We have also demonstrated that the catalyst can be reused successfully.
基金supported by Grant-in-Aid for Scientific Research from the New Energy and Industrial Technology Development Organization(NEDO)project(JPNP14004)and The Naito Foundation.
文摘Peptide bond formation has drawn more and more attention due to its importance in medicinal chemistry and drug discovery.Using active esters to construct peptide bonds is an indispensable strategy in this field.We herein report a fast and efficient amination reaction to synthesize peptides from catechol diesters.Catechol monoesters are good active esters in peptide synthesis due to the anchimeric assistance effect.In previously reported work,the amination reaction was inactivated if the 2-hydroxyl group in the catechol esters was functionalized.However,we found an unusual acceleration of the amination reactivity when the 2-hydroxyl group was functionalized as an ester group.The reaction can be complete in 2−3 min in some cases.This acceleration was found through experimental studies to not result from the anchimeric assistance effect.We proposed aπ*−π*interaction pathway between the two proximal ester groups.Some computational studies were made to support this assumption.
文摘Dear Editor,Tumor angiogenesis is regulated by the binding of VEGF to receptors(VEGFRs).The major mediator of tumor angiogenesis is VEGFA,more commonly referred to as VEGF.VEGFR1 binds VEGF with higher affinity(10 times)than VEGFR2.1 However,the role of the VEGFR1 in VEGF-mediated angiogenesis remains a mystery.
