An efficient protocol was developed for the synthesis of 3-aminoalkylated indoles using 3- chlorophenylboronic acid as a catalyst under ambient temperature conditions.The three-component reaction of indoles,aromatic a...An efficient protocol was developed for the synthesis of 3-aminoalkylated indoles using 3- chlorophenylboronic acid as a catalyst under ambient temperature conditions.The three-component reaction of indoles,aromatic aldehydes and N-methyl aniline offered corresponding 3-aminoalkylated indoles in excellent yields.This protocol presents some remarkable features such as mild reaction conditions,simple workup procedure and excellent yields.展开更多
A new series of 1H-pyrazole derivatives 5a-j bearing an aryl sulfonate moiety have been synthesized by a one-pot cyclo-condensation reaction of 2-（3-（dimethylamino）acryloyl）phenyl-4-methyl benzene sulfonates 4a-e ...A new series of 1H-pyrazole derivatives 5a-j bearing an aryl sulfonate moiety have been synthesized by a one-pot cyclo-condensation reaction of 2-（3-（dimethylamino）acryloyl）phenyl-4-methyl benzene sulfonates 4a-e and hydrazine hydrate or phenyl hydrazine in ethanol under reflux conditions. Some of the newly synthesized compounds were screened for their anti-inflammatory activity. All synthesized compounds were screened against Gram positive and Gram negative bacterial and fungal strains. The compound 5b was found to be a potent anti-inflammatory agent while the majority of the compounds were found to be active against microbial strains.展开更多
The proline based chiral organocatalyst has been found to be an efficient catalyst for the facile synthesis of substituted 2-aryl-2 H-chromenes-3-carbaldehyde. We envisioned that the iminium interaction between chiral...The proline based chiral organocatalyst has been found to be an efficient catalyst for the facile synthesis of substituted 2-aryl-2 H-chromenes-3-carbaldehyde. We envisioned that the iminium interaction between chiral amino catalysts and a,b-unsaturated carbonyl group was beneficial along with thiourea group as hydrogen bond donor, heterocyclic amines as general base in the domino oxa-Michael-aldol reaction. This catalytic system provided the products in good to high yields（73%–96%） with excellent enantioselectivity（up to 97%） and reasonable reaction time. The atom economy, high yield and mild reaction conditions are some of the important features of this protocol.展开更多
基金Dr.P.L.More and Dr.W.N.Jadhav,Dnyanopasak College,Parbhani for providing necessary facilities and Financial support for this work by DST-SERC,New Delhi(SR/FT/CS- 023/2008) is highly appreciated
文摘An efficient protocol was developed for the synthesis of 3-aminoalkylated indoles using 3- chlorophenylboronic acid as a catalyst under ambient temperature conditions.The three-component reaction of indoles,aromatic aldehydes and N-methyl aniline offered corresponding 3-aminoalkylated indoles in excellent yields.This protocol presents some remarkable features such as mild reaction conditions,simple workup procedure and excellent yields.
文摘A new series of 1H-pyrazole derivatives 5a-j bearing an aryl sulfonate moiety have been synthesized by a one-pot cyclo-condensation reaction of 2-（3-（dimethylamino）acryloyl）phenyl-4-methyl benzene sulfonates 4a-e and hydrazine hydrate or phenyl hydrazine in ethanol under reflux conditions. Some of the newly synthesized compounds were screened for their anti-inflammatory activity. All synthesized compounds were screened against Gram positive and Gram negative bacterial and fungal strains. The compound 5b was found to be a potent anti-inflammatory agent while the majority of the compounds were found to be active against microbial strains.
文摘The proline based chiral organocatalyst has been found to be an efficient catalyst for the facile synthesis of substituted 2-aryl-2 H-chromenes-3-carbaldehyde. We envisioned that the iminium interaction between chiral amino catalysts and a,b-unsaturated carbonyl group was beneficial along with thiourea group as hydrogen bond donor, heterocyclic amines as general base in the domino oxa-Michael-aldol reaction. This catalytic system provided the products in good to high yields（73%–96%） with excellent enantioselectivity（up to 97%） and reasonable reaction time. The atom economy, high yield and mild reaction conditions are some of the important features of this protocol.
