Buchi Reddy Reguri - Academia.edu (original) (raw)
Papers by Buchi Reddy Reguri
Journal of chemical and pharmaceutical research, 2014
We report asynthesis of analogues of trifenagrel using selected substituted benzaldehydes namely ... more We report asynthesis of analogues of trifenagrel using selected substituted benzaldehydes namely 3-hydroxy benzaldehyde, 4-hydroxybenzaldehyde and vanillin. Condensation of aminoethoxy benzaldehydes with benzil and ammonium acetate using catalytic amount of tetrabutylammonium hydrogen sulphate (TBAHS) resulted in the desirable analogues of trifenagrel. Nine analogues were synthesized and characterized by their IR,
ChemInform, Dec 9, 2011
The complex acts as mild and nontoxic reagent for the conversion of ketoximes into the correspond... more The complex acts as mild and nontoxic reagent for the conversion of ketoximes into the corresponding amides within a relatively short reaction time.
This paper describes the direct N-alkylation of amines with alcohols through oxidation/imination/... more This paper describes the direct N-alkylation of amines with alcohols through oxidation/imination/reduction sequence using a catalytic amount of nanocrystalline CuO as a recyclable catalyst and K2CO3 as the base in toluene at 110 °C. This method is found to be applicable for wide range of amines and alcohols. The operational simplicity and the mild reaction conditions add to the value of this method as a practical alternative to the N-alkylation of amines with alcohols.
La presente invention concerne un procede de purification du compose rabeprazole de formule (I) o... more La presente invention concerne un procede de purification du compose rabeprazole de formule (I) ou de son sel de sodium. Formule (I)
La presente invention concerne un nouveau procede de recuperation et de recyclage d'enantiome... more La presente invention concerne un nouveau procede de recuperation et de recyclage d'enantiomeres indesirables de derives de 2-aminopropyl-indoline, des intermediaires utiles, en particulier, pour la preparation de silodosine ou de ses sels. La presente invention concerne egalement de nouveaux composes de formule II, de formule III, de formule IV et de formule V.
![Research paper thumbnail of Synthesis of 3,4-dihydro-3,3-dimethyl-13-aryl-2H-indazolo [1,2-b]pthalazine-1,6,11(13H)-triones using tungstated zirconia (WO3/ZrO2)](https://attachments.academia-assets.com/98218324/thumbnails/1.jpg)
](A New, robust and fasile route for the three-component synthesis of 2H-indazolo [2,1-b]phthalazin... more A New, robust and fasile route for the three-component synthesis of 2H-indazolo [2,1-b]phthalazine-triones in the presence of a catalytic amount of Tungstated Zirconia (WO3/ZrO2) Lewis acid has been developed. Short reaction time, simple operation, and high yields are the advantages of this protocol
La presente invention concerne une amelioration du procede d'elaboration de l'iloperidone... more La presente invention concerne une amelioration du procede d'elaboration de l'iloperidone representee par la formule (I). L'invention concerne egalement un nouveau polymorphe de sels d'addition acides de l'iloperidone representee par la formule (I).
Journal of chemical and pharmaceutical research, 2014
In view of several synthetic and biological, pharmacological applications of benzocycloheptene-5-... more In view of several synthetic and biological, pharmacological applications of benzocycloheptene-5-one derivatives, the present work aimed to achieve 2,3-dimethyl-6-(1-phenyl but-3-enyl)-6,7,8,9-tetrahydro benzocyclohepten-5-ones (9a-c);1-(9,10-dimethyl-4-phenyl-6,7,-dihydro-5H-benzo[6,7]cyclohepta[1,2-d]pyrimidin-2-yl)pyrrolidine-2,5-dione (11) and 2-(9,10-dimethyl-4-phenyl-6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-d] pyridine-2-yl) isoindole-1,3-dione (12).
![Research paper thumbnail of Synthesis of 11,12-dimethoxy-9-p-toluene sulphonyl-6,7,8,9-tetrahydro-5Hbenzo[2,3]azepino[5,4-c]quinolin-5-one using MCM-41(H)](https://attachments.academia-assets.com/98218325/thumbnails/1.jpg)
](The development in the benzazepine field for medicinal interests, attention has been paid almost ... more The development in the benzazepine field for medicinal interests, attention has been paid almost exclusively to substituent changes, with the adjustment of open chain and cyclic groups attached to both the aromatic and the azepine ring. In some instances the benzene ring has been replaced with other aromatic ring systems, e.g. Indoles1,2 which is particularly true in the benzodiazepine field. Herein, we report the New Synthesis of 11,12-dimethoxy-9-(4- phenylsulphonyl)-6,7,8,9-terahydro-5H-benzo[2,3]azepino[5,4-c]quinolin-5-one.
Asian Journal of Chemistry, 2014
A mild and efficient ligand-free Hiyama cross-coupling reaction using Pd/C as a catalyst under aq... more A mild and efficient ligand-free Hiyama cross-coupling reaction using Pd/C as a catalyst under aqueous conditions has been developed. A wide variety of aryl bromides undergo the cross-coupling with aryl siloxanes in excellent yields without the use of any additives. The operational simplicity and the mild reaction conditions add to the value of this method as a practical alternative to the Hiyama crosscoupling of aryl and heteroaryl halides.
An alternative synthesis of amidoalkyl naphthols, employing a three-component condensation reacti... more An alternative synthesis of amidoalkyl naphthols, employing a three-component condensation reaction of β- naphthol, aromatic aldehyde, amides or urea in the presence of polyaniline sulphate salt under solvent free conditions has been described. The present procedure offers advantages such as shorter reaction time, simple workup, excellent yields, recovery and reusability of catalyst
Asian Journal of Chemistry, 2013
The ever increasing demand for the novel medicinally active compounds and the laborious process o... more The ever increasing demand for the novel medicinally active compounds and the laborious process of lead discovery and optimization have resulted in the continuous search for simple and efficient methods for generation of libraries for biological screening. Click chemistry has emerged as a fast and efficient approach to synthesize novel compounds with desired function making use of selected "near perfect" reactions 1. The Huisgen 1,3-dipolar cycloaddition 2 of azides and alkynes resulting in 1,2,3-triazoles is one of the most powerful click reactions. Copper catalyzed ligation of organic azides and terminal alkynes has enjoyed much use since its discovery. Exclusive regioselectivity, wide substrate scope, mild reaction conditions and very high yields 3 have made it the method of choice for making permanent connections by means of 1,4-disubstituted 1,2,3-triazoles. Since then, this reaction has been used for the construction of a variety of multivalent structures such as sugar heterodimers, glycoconjugates 4 , calix-sugars 5 and dendritic and polymeric materials 6. Furthermore, the one-pot multistep reaction involving the Wittig olefination, the Knoevenagel condensation, the Diels-Alder cyclization and Cu(I)-catalyzed alkyne-azide coupling has been explored 7. Gratifyingly, the same level of success has been found when compared to the traditional methodology. In another variation, microwaveassisted one-pot reaction has generated a variety of triazoles directly from activated aryl halides and sodium azide 8. In a similar fashion, taking advantage of anomeric activation, rapid
L'invention concerne une nouvelle forme cristalline de 2-methyl-4-(4-methyl-piperazinyl)-10H-... more L'invention concerne une nouvelle forme cristalline de 2-methyl-4-(4-methyl-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine, et un procede de preparation de ladite forme cristalline. La methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine (Olanzapine) selon l'invention est representee par la structure (I).
La presente invention a pour objet un procede ameliore pour la preparation de paliperidone pure d... more La presente invention a pour objet un procede ameliore pour la preparation de paliperidone pure de formule (I). La presente invention concerne plus specifiquement un procede ameliore pour la preparation de paliperidone pure qui peut contenir des impuretes au niveau acceptable de lexigence de la pharmacopee, specifiquement de la 3-{2-[4-(5-fluoro-benzo [d] isoxazol-3-yle]-piperidin-1-yle]-ethyle}-2- methyl-7,8-dihydro-6H-pyrido [1,2-a] pyrimidine-4,9-dione de formule (IV).
L'invention concerne des nouvelles formes amorphes anhydres de [R-(E)-1-[[[l-[3-[2-[7-chloro-... more L'invention concerne des nouvelles formes amorphes anhydres de [R-(E)-1-[[[l-[3-[2-[7-chloro-2-quinolinyle] ethenyle] phenyle]-3-[2-(1-hydroxy-l-methylethyle) phenyle] propyle] thio] methyle] sels alcalins d'acide cyclopropane acetique (sels alcalins de montelukast), leurs procedes de preparation, des compositions les contenant, et des procedes de traitement les mettant en oeuvre. Le montelukast est un agoniste de leucotriene, utile en tant qu'anti-asthmatique, anti-inflammatoire et agent cytoprotecteur. Le montelukast est represente par la formule (I).
La presente invention a pour objet un nouveau solvate du dexlansoprazole (ou du R-lansoprazole), ... more La presente invention a pour objet un nouveau solvate du dexlansoprazole (ou du R-lansoprazole), en particulier un solvate diol et sa forme hydrate du dexlansoprazole (ou du R-lansoprazole) qui est chimiquement connu sous le nom du compose (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyle] methyle]sulfmyle]-1H-benzimidazole de formule (I), ainsi que des procedes pour sa preparation. Lesdits solvates sont utiles dans la preparation du dexlansoprazole avec une purete chirale accrue et une meilleure purete HPLC avec une moindre teneur en impuretes de type sulfone.
Journal of chemical and pharmaceutical research, 2014
We report asynthesis of analogues of trifenagrel using selected substituted benzaldehydes namely ... more We report asynthesis of analogues of trifenagrel using selected substituted benzaldehydes namely 3-hydroxy benzaldehyde, 4-hydroxybenzaldehyde and vanillin. Condensation of aminoethoxy benzaldehydes with benzil and ammonium acetate using catalytic amount of tetrabutylammonium hydrogen sulphate (TBAHS) resulted in the desirable analogues of trifenagrel. Nine analogues were synthesized and characterized by their IR,
ChemInform, Dec 9, 2011
The complex acts as mild and nontoxic reagent for the conversion of ketoximes into the correspond... more The complex acts as mild and nontoxic reagent for the conversion of ketoximes into the corresponding amides within a relatively short reaction time.
This paper describes the direct N-alkylation of amines with alcohols through oxidation/imination/... more This paper describes the direct N-alkylation of amines with alcohols through oxidation/imination/reduction sequence using a catalytic amount of nanocrystalline CuO as a recyclable catalyst and K2CO3 as the base in toluene at 110 °C. This method is found to be applicable for wide range of amines and alcohols. The operational simplicity and the mild reaction conditions add to the value of this method as a practical alternative to the N-alkylation of amines with alcohols.
La presente invention concerne un procede de purification du compose rabeprazole de formule (I) o... more La presente invention concerne un procede de purification du compose rabeprazole de formule (I) ou de son sel de sodium. Formule (I)
La presente invention concerne un nouveau procede de recuperation et de recyclage d'enantiome... more La presente invention concerne un nouveau procede de recuperation et de recyclage d'enantiomeres indesirables de derives de 2-aminopropyl-indoline, des intermediaires utiles, en particulier, pour la preparation de silodosine ou de ses sels. La presente invention concerne egalement de nouveaux composes de formule II, de formule III, de formule IV et de formule V.
A New, robust and fasile route for the three-component synthesis of 2H-indazolo [2,1-b]phthalazin... more A New, robust and fasile route for the three-component synthesis of 2H-indazolo [2,1-b]phthalazine-triones in the presence of a catalytic amount of Tungstated Zirconia (WO3/ZrO2) Lewis acid has been developed. Short reaction time, simple operation, and high yields are the advantages of this protocol
La presente invention concerne une amelioration du procede d'elaboration de l'iloperidone... more La presente invention concerne une amelioration du procede d'elaboration de l'iloperidone representee par la formule (I). L'invention concerne egalement un nouveau polymorphe de sels d'addition acides de l'iloperidone representee par la formule (I).
Journal of chemical and pharmaceutical research, 2014
In view of several synthetic and biological, pharmacological applications of benzocycloheptene-5-... more In view of several synthetic and biological, pharmacological applications of benzocycloheptene-5-one derivatives, the present work aimed to achieve 2,3-dimethyl-6-(1-phenyl but-3-enyl)-6,7,8,9-tetrahydro benzocyclohepten-5-ones (9a-c);1-(9,10-dimethyl-4-phenyl-6,7,-dihydro-5H-benzo[6,7]cyclohepta[1,2-d]pyrimidin-2-yl)pyrrolidine-2,5-dione (11) and 2-(9,10-dimethyl-4-phenyl-6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-d] pyridine-2-yl) isoindole-1,3-dione (12).
The development in the benzazepine field for medicinal interests, attention has been paid almost ... more The development in the benzazepine field for medicinal interests, attention has been paid almost exclusively to substituent changes, with the adjustment of open chain and cyclic groups attached to both the aromatic and the azepine ring. In some instances the benzene ring has been replaced with other aromatic ring systems, e.g. Indoles1,2 which is particularly true in the benzodiazepine field. Herein, we report the New Synthesis of 11,12-dimethoxy-9-(4- phenylsulphonyl)-6,7,8,9-terahydro-5H-benzo[2,3]azepino[5,4-c]quinolin-5-one.
Asian Journal of Chemistry, 2014
A mild and efficient ligand-free Hiyama cross-coupling reaction using Pd/C as a catalyst under aq... more A mild and efficient ligand-free Hiyama cross-coupling reaction using Pd/C as a catalyst under aqueous conditions has been developed. A wide variety of aryl bromides undergo the cross-coupling with aryl siloxanes in excellent yields without the use of any additives. The operational simplicity and the mild reaction conditions add to the value of this method as a practical alternative to the Hiyama crosscoupling of aryl and heteroaryl halides.
An alternative synthesis of amidoalkyl naphthols, employing a three-component condensation reacti... more An alternative synthesis of amidoalkyl naphthols, employing a three-component condensation reaction of β- naphthol, aromatic aldehyde, amides or urea in the presence of polyaniline sulphate salt under solvent free conditions has been described. The present procedure offers advantages such as shorter reaction time, simple workup, excellent yields, recovery and reusability of catalyst
Asian Journal of Chemistry, 2013
The ever increasing demand for the novel medicinally active compounds and the laborious process o... more The ever increasing demand for the novel medicinally active compounds and the laborious process of lead discovery and optimization have resulted in the continuous search for simple and efficient methods for generation of libraries for biological screening. Click chemistry has emerged as a fast and efficient approach to synthesize novel compounds with desired function making use of selected "near perfect" reactions 1. The Huisgen 1,3-dipolar cycloaddition 2 of azides and alkynes resulting in 1,2,3-triazoles is one of the most powerful click reactions. Copper catalyzed ligation of organic azides and terminal alkynes has enjoyed much use since its discovery. Exclusive regioselectivity, wide substrate scope, mild reaction conditions and very high yields 3 have made it the method of choice for making permanent connections by means of 1,4-disubstituted 1,2,3-triazoles. Since then, this reaction has been used for the construction of a variety of multivalent structures such as sugar heterodimers, glycoconjugates 4 , calix-sugars 5 and dendritic and polymeric materials 6. Furthermore, the one-pot multistep reaction involving the Wittig olefination, the Knoevenagel condensation, the Diels-Alder cyclization and Cu(I)-catalyzed alkyne-azide coupling has been explored 7. Gratifyingly, the same level of success has been found when compared to the traditional methodology. In another variation, microwaveassisted one-pot reaction has generated a variety of triazoles directly from activated aryl halides and sodium azide 8. In a similar fashion, taking advantage of anomeric activation, rapid
L'invention concerne une nouvelle forme cristalline de 2-methyl-4-(4-methyl-piperazinyl)-10H-... more L'invention concerne une nouvelle forme cristalline de 2-methyl-4-(4-methyl-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine, et un procede de preparation de ladite forme cristalline. La methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine (Olanzapine) selon l'invention est representee par la structure (I).
La presente invention a pour objet un procede ameliore pour la preparation de paliperidone pure d... more La presente invention a pour objet un procede ameliore pour la preparation de paliperidone pure de formule (I). La presente invention concerne plus specifiquement un procede ameliore pour la preparation de paliperidone pure qui peut contenir des impuretes au niveau acceptable de lexigence de la pharmacopee, specifiquement de la 3-{2-[4-(5-fluoro-benzo [d] isoxazol-3-yle]-piperidin-1-yle]-ethyle}-2- methyl-7,8-dihydro-6H-pyrido [1,2-a] pyrimidine-4,9-dione de formule (IV).
L'invention concerne des nouvelles formes amorphes anhydres de [R-(E)-1-[[[l-[3-[2-[7-chloro-... more L'invention concerne des nouvelles formes amorphes anhydres de [R-(E)-1-[[[l-[3-[2-[7-chloro-2-quinolinyle] ethenyle] phenyle]-3-[2-(1-hydroxy-l-methylethyle) phenyle] propyle] thio] methyle] sels alcalins d'acide cyclopropane acetique (sels alcalins de montelukast), leurs procedes de preparation, des compositions les contenant, et des procedes de traitement les mettant en oeuvre. Le montelukast est un agoniste de leucotriene, utile en tant qu'anti-asthmatique, anti-inflammatoire et agent cytoprotecteur. Le montelukast est represente par la formule (I).
La presente invention a pour objet un nouveau solvate du dexlansoprazole (ou du R-lansoprazole), ... more La presente invention a pour objet un nouveau solvate du dexlansoprazole (ou du R-lansoprazole), en particulier un solvate diol et sa forme hydrate du dexlansoprazole (ou du R-lansoprazole) qui est chimiquement connu sous le nom du compose (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyle] methyle]sulfmyle]-1H-benzimidazole de formule (I), ainsi que des procedes pour sa preparation. Lesdits solvates sont utiles dans la preparation du dexlansoprazole avec une purete chirale accrue et une meilleure purete HPLC avec une moindre teneur en impuretes de type sulfone.