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The catalytic activity of commercially available [Al(NMe2) 3]2 (1) and a dimethyl aluminum guanidinate complex toward the hydro-amination/-hydrazination of carbodiimides was studied. The guanidinate-supported complex 2 was prepared via salt metathesis reactions of AlMe2Cl and an in situ generated lithium guanidinate reagent. X-ray crystallographic studies revealed the influence of the guanidinate ligand on the Al metal center. Hydroamination reactions were successfully carried out at room temperature with 2 as the catalyst, while 1 proved to be ineffective under these conditions. On the contrary, both 1 and 2 were active toward the hydro-hydrazination of carbodiimides, which were run at elevated temperatures (120 C). Consequently, the reaction temperature had a significant influence on the choice of the catalyst since the catalytically active species can be generated from various precatalysts under different conditions. The formation of guanidines and aminoguanidines showed a high functional group tolerance and typically proceeded with excellent yields at low catalyst loadings. X-ray crystallographic studies of compound 4a revealed interesting structural features of the previously unknown aminoguanidine products. The independently isolated Al aminoguanidinate complex 5 showed catalytic activity toward hydro-hydrazination chemistry and provided valuable evidence in support of the proposed reaction mechanism.

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Piperidine – Wikipedia,
Piperidine | C5H829N – PubChem

 

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Starting from semisquaric acid (1), the semisquaric esters 6a-d and semisquaric chloride (7) were prepared.Reaction of 6c or 7 with amines as well as the method of mixed anhydrides, starting from 1, afforded the semisquaric amides 10a-n (Methods A, B, C, respectively).The semisquaric amides 10g,h,i were also obtained by the reaction of semisquaric chloride (7) with the trimethylsilylamines 11a-c (Method D); 10h was furthermore prepared by the DCC-method (Method E).The reaction of butyl squarate (6) with hydrazines and N-alkylhydroxylamines afforded the semisquaric hydrazides 13a-d and the semisquaric hydroxylamides 15a-c, respectively.

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Based on the fact that timosaponin A-III (TA-III) exhibits potent cytotoxic effects and has been considered as a potential anti-tumor agent, a range of novel sarsasapogenin derivatives 1, 2a-2g, 3, 4, 5, 6a-6g have been synthesized by a simple and facile synthetic route. The in vitro cytotoxic activity of these synthetic compounds has been evaluated against ten human cancer cell lines. The pharmacological results showed that most of the sarsasapogenin derivatives displayed excellent selective cytotoxicity toward the cancer cell lines. An amino group at C-3 or C-26 position of the sapogenin had a profound influence on the cytotoxic activity. In particular, compound 6c exhibited significantly inhibitory activity against A375-S2 (IC50 = 0.56 muM) and HT1080 (IC50 = 0.72 muM) cells. However, introducing a bromo or morpholinyl substituent at the C-3 and C-26 position of the sapogenin generally rendered it inactive against the human cancer cell lines. This research provides a theoretical reference for the exploration of new anti-tumor drugs.

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Piperidine – Wikipedia,
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Described are methods for preparing phenols, benzene carboxylic acids, esters and anhydrides thereof from furanic compounds by reaction with a dienophile, wherein the furanic compounds are reacted with a hydrazine and/or oxime and then reacted with a dienophile.

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Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 2213-43-6, molcular formula is C5H12N2, introducing its new discovery. Recommanded Product: 2213-43-6

The synthesis of solution phase libraries of chiral monodentate phosphoramidite by using the automated parallel protocol was analyzed. It was observed that the method leads to the analysis of effective enantioselective catalysts for tranformations and association with the monodentate ligand combination approach. The automated parallel protocol provided a powerful tool for the combinatorial asymmetric catalysis. The chromatography was performed at the end of the phosphoramidite synthesis by a filtration process, due to more simple automated procedure.

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Chemistry is traditionally divided into organic and inorganic chemistry. Computed Properties of C5H12N2. The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent,Which mentioned a new discovery about 2213-43-6

A series of conformationally constrained bicyclic derivatives derived from SR141716 was prepared and evaluated as hCB1-R antagonists and inverse agonists. Optimization of the structure-activity relationships around the 2,6-dihydro-pyrazolo[4,3-d]pyrimidin-7-one derivative 2a led to the identification of two compounds with oral activity in rodent feeding models (2h and 4a). Replacement of the PP group in 2h with other bicyclic groups resulted in a loss of binding affinity.

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Piperidine – Wikipedia,
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The reaction of [Pd(CH3CN)2Cl2] with N-cyclopentyl-1-(pyridin-2-yl)methanimine (L1), N-cyclohexyl-1- (pyridin-2-yl)methanimine (L2), N-(piperidin-1-yl)-1-(pyridin-2-yl) methanimine (L3) or N-cyclopentyl-1-(quinolin-2-yl)methanimine (L4) in ethanol yields the bidentate (NN’) PdCl2 complexes [L1PdCl2], [L2PdCl2], [L 3PdCl2] and [L4PdCl2], respectively. The X-ray crystal structure of the Pd(II) complexes revealed that the Pd atom in [LnPdCl2] (Ln = L1, L 2, L3, L4) shows a distorted square planar geometry involving two nitrogen atoms and two chloro ligands. The complexes [L1PdCl2] and [L4PdCl2] (of which the ligands are N-cyclopentyl substituted) showed the highest catalytic activity for the polymerisation of methyl methacrylate (MMA) in the presence of modified methylaluminoxane (MMAO) with an activity of 1.45 × 105 g PMMA/mol Pd h at 60 C and a PMMA syndiotacticity (characterized using 13C NMR spectroscopy) of ca. 0.70.

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The present invention comprises a new class of compounds capable of modulating the activity of PI3 kinase and, accordingly, useful for treatment of PI3 kinase mediated diseases, including melanomas, carcinomas and other cancer-related conditions. The compounds have a general Formula I wherein each of A1, A2, A3, A4, X, R1 and R2 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of PI3 kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.

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Piperidine – Wikipedia,
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A series of 4,5-dihydro-1H-benzo[g]indazole-3-carboxamides (2a-k) as analogues of the previously reported CB2 ligands 6-chloro- and 6-methyl-1-(2?,4?-dichlorophenyl)-N-piperidin-1-yl-1, 4-dihydroindeno[1,2-c]pyrazole-3-carboxamides (1a,b) was synthesized and their affinity and selectivity towards CB1 and CB2 receptors were evaluated. Several of the new compounds (2a,b,c,d and i) exhibited CB 1 affinity in the nanomolar range with moderate or negligible affinity towards CB2 receptors. Compounds 2a and c increased intestinal propulsion in mouse. Their pro-kinetic effects were reversed by the reference CB agonist CP-55,940. Consequently, in vivo CB1 antagonistic activity was highlighted for these compounds.

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Fumagillin, an irreversible inhibitor of MetAP2, has been shown to potently inhibit growth of malaria parasites in vitro. Here, we demonstrate activity of fumagillin analogs with an improved pharmacokinetic profile against malaria parasites, trypanosomes, and amoebas. A subset of the compounds showed efficacy in a murine malaria model. The observed SAR forms a basis for further optimization of fumagillin based inhibitors against parasitic targets by inhibition of MetAP2.

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