- Manganese-Catalyzed Anti-Markovnikov Hydroamination of Allyl Alcohols via Hydrogen-Borrowing Catalysis
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Controlling the selectivity in a hydroamination reaction is an extremely challenging yet highly desirable task for the diversification of amines. In this article, a selective formal anti-Markovnikov hydroamination of allyl alcohols is presented. It enables the versatile synthesis of valuable γ-amino alcohol building blocks. A phosphine-free Earth's abundant manganese(I) complex catalyzed the reaction under hydrogen-borrowing conditions. A vast range of aliphatic, aromatic amines, drug molecules, and natural product derivatives underwent successful hydroamination with primary and secondary allylic alcohols with excellent functional group tolerance (57 examples). The catalysis could be performed on a gram scale and has been applied for the synthesis of drug molecules. The mechanistic studies revealed the metal-ligand bifunctionality as well as hemilability of the ligand backbone as the key design principle for the success of this catalysis.
- Das, Kuhali,Sarkar, Koushik,Maji, Biplab
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p. 7060 - 7069
(2021/06/30)
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- Synthesis and antimicrobial activity of some new 1,2,4-triazine and benzimidazole derivatives
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1-(4-Substituted phenyl)-3-(substituted)propan-1-(1H-benzo[d]imidazol-2-yl) hydrazines and 1-(4-substituted phenyl)- 3-(substituted)propan-1-(5H-[1,2,4] triazino[5,6-b]indol-3-yl) hydrazines have been synthesized by the fusion of triazine and benzimidazole derivatives with Mannich bases. The synthesized compounds have been characterized and screened against ITCC 5226 Sclerotium rolfsii and ITCC 0482 Macrophomina phaseolina and MTCC739 Escherichia coli, ATCC6533 Bacillus subtilis, ATCC9144 Staphylococcus aureus, ATCC25619 Pseudomonas aeruginosa and ATCC24433 Candida albicans.
- Bishnoi, Abha,Singh, Suruchi,Tiwari, Anil K.,Rani, Archna,Jain, Sapna,Tripathic
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p. 325 - 331
(2014/05/06)
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- A straightforward and efficient method for the synthesis of diversely substituted β-aminoketones and γ-aminoalcohols from 3-(N,N-dimethylamino)propiophenones as starting materials
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Bibliotecas de novos β-aminocetonas e γ-aminoa?lcoois que mostram uma grande diversidade estrutural foram facilmente obtidas a partir de uma abordagem simple, utilizando os derivados da 3-(N,N-dimetilamino) propiofenona como material de partida chave. O p
- Abonia, Rodrigo,Arteaga, Danny,Castillo, Juan,Insuasty, Braulio,Quiroga, Jairo,Orti?z, Alejandro
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p. 1396 - 1402
(2013/09/24)
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- Synthesis and appetite suppressant activity of 1-aryloxy-2-substituted aminomethyltetrahydronaphthalenes as conformationally rigid analogues of fluoxetine
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Several 1-aryloxy-2-substituted aminomethyltetrahydronaphthalenes (7-21) as conformationally rigid analogues of fluoxetine were synthesized and evaluated for their anorexigenic and antidepressant activities. For SAR studies the related acyclic analogues (
- Bhandari, Kalpana,Srivastava, Shipra,Shankar, Girija,Nath, Chandishwar
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p. 2535 - 2544
(2007/10/03)
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- 5-Phenylthio-1,3-oxazinan-4-ones via hetero Diels-Alder reactions: synthesis of (R)- and (S)-Duloxetines and Fluoxetines
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The synthesis of 5-phenylthio-1,3-oxazinan-4-ones, through a hetero Diels-Alder strategy, is described. The cycloadducts thus prepared have been shown to be useful intermediates for the synthesis of 1,3-aminoalcohols, valuable intermediates in the preparation of biologically significant molecules, e.g., optically active Duloxetines and Fluoxetines. In the course of this elaboration a novel microwave assisted desulfurization reaction is reported.
- Panunzio, Mauro,Tamanini, Emiliano,Bandini, Elisa,Campana, Eileen,D'Aurizio, Antonio,Vicennati, Paola
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p. 12270 - 12280
(2007/10/03)
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- PROPANAMINE DERIVATIVES AS SEROTONIN AND NOREPINEPHRINE REUPTAKE INHIBITORS
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There is provided a heretoaryloxy/thio 3-substituted propanamine compound of formula (I) wherein A is selected from -O- and -S-; X is selected from phenyl optionally substituted with up to 5 substituents each independently selected from halo, C1-C4 alkyl and C1-C4 alkoxy, thienyl optionally substituted with up to 3 substituents each independently selected from halo and C1-C4 alkyl, and C2-C8 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n- where n is 0, 1 or 2, -CF3, -CN and -CONH2; Y is selected from dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, and thienopyridyl, each of which may be optionally substituted with up to 4 or, where possible, up to 5 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n- where n is 0, 1 or 2, nitro, acetyl, -CF3, -SCF3 and cyano; Z is selected from H, OR3 or F, wherein R3 is selected from H, C1-C6 alkyl and phenyl C1-C6 alkyl; R1 and R2 are each independently H or C1-C4 alkyl; and pharmaceutically acceptable salts thereof.
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- Synthesis, CNS and chloroquin resistance reversal activity of benzenepropanamines
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Several benzenepropanamines with a benzyl group attached to the 3-amino function are synthesized and evaluated for their CNS and chloroquin resistant reversal activity. The compounds are fully characterized by spectral and elemental analyses. These compounds are tested for their effect on gross behaviour and for antidepressant, anticonvulsant and anorexigenic activity. No effect is observed on gross behaviour where as most of them show fluoxetine like antireserpine and anorexigenic activity. Since this class of compounds have been reported to modulate the chloroquin resistance in P. falciparum, therefore these compounds are tested for chloroquin resistance reversal activity in vitro. Five compounds selectively inhibit P. falciparum heme oxygenase like fluoxetine.
- Sharma,Bhandari, Kalpana,Shankar, Girija,Singh,Srivastava, Pratima,Pandey
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p. 207 - 211
(2007/10/03)
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- Synthesis, anorexigenic activity and QSAR of substituted aryloxypropanolamines
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Substituted aryloxypropanolamines (6-20) were synthesized and evaluated for their anorexigenic activity. Among them 4-cyanoaryloxy (7), 2-methylaryloxy (9), 2-methoxyl aryloxy (10), 4-acetamidoaryloxy (15), 4-bromoaryloxy (16) and 4-ethylaminoaryloxy (20) exhibited potent anorexigenic activity. According to QSAR studies, the electronic parameter 'σ' plays an important role in describing the variance in activity. Birkhaeuser Boston 2004.
- Srivastava, Shipra,Bhandari, Kalpana,Shankar, Girija,Singh,Saxena, Anil K.
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p. 631 - 642
(2007/10/03)
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- The Reductive Cleavage of Cyclic Aminol Ethers to N,N-Dialkylamino-derivatives: Modifications to the Eschweiler-Clarke Procedure
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The reductive cleavage of cyclic aminol ethers to give N-alkylamino-derivatives in very high yields can be achieved using chlorotrimethylsilane in the presence of sodium cyanoborohydride: in the case of cyclic aminol ethers derived from formaldehyde the Eschweiler-Clarke reaction can be carried out in formic acid heated under reflux in the absence of formaldehyde.
- Page, Philip C. Bulman,Heaney, Harry,Rassias, Gerasimos A.,Reignier, Serge,Sampler, Edward P.,Talib, Salem
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p. 104 - 106
(2007/10/03)
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