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The catalytic resolution of racemic cyclic amines has been achieved by an enantioselective amidation reaction featuring an achiral N-heterocyclic carbene catalyst and a new chiral hydroxamic acid cocatalyst working in concert. The reactions proceed at room temperature, do not generate nonvolatile byproducts, and provide enantioenriched amines by aqueous extraction.

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The present invention is directed to compounds of Formula I: wherein X is O, S or NR7 and R1-R7, Y and Z are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, plasmin and urokinase. Certain of the compounds exhibit direct, selective inhibition of urokinase, or are intermediates useful for forming compounds having such activity.

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The pathogenic bacteria Chlamydia trachomatis, Neisseria gonorrhoeae and Neisseria meningitidis express the surface-exposed macrophage infectivity potentiator (MIP)-like protein, which plays a role in their pathogenicity. MIP exhibits a peptidyl-prolyl isomerase (PPIase) activity that is inhibited by rapamycin and FK506. In this study, pipecolic acid derivatives were tested for their activity against the chlamydial and neisserial MIP. Two MIP inhibitors were identified, PipN3 and PipN4, that affected the developmental cycle of C. trachomatis in HeLa cells. Furthermore, we could show that deletion of neisserial MIP or addition of the two MIP inhibitors affected the survival of N. gonorrhoeae in the presence of neutrophils. Furthermore, both compounds inhibited the adherence, invasion and/or survival of N. meningitidis in epithelial cells. These results confirm the importance of MIP-like proteins in infection and indicate the relevance of pipecolic acid derivatives as antimicrobials against C. trachomatis, N. gonorrhoeae and N. meningitidis.

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Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels.In a patent， COA of Formula: C8H15NO2, Which mentioned a new discovery about 15862-72-3

Reactions of no-carrier-added (NCA) [18F]beta-fluoroethyl tosylate with amine, phenol or carboxylic acid to form the corresponding [ 18F]N-(beta-fluoroethyl)amine, [18F]beta-fluoroethyl ether or [18F]beta-fluoroethyl ester, were found to be rapid (2-10 min) and efficient (51-89% conversion) under microwave-enhanced conditions. These conditions allow reactants to be heated rapidly to 150C in a low boiling point solvent, such as acetonitrile, and avoid the need to use high boiling point solvents, such as DMSO and DMF, to promote reaction. The microwave-enhanced reactions gave about 20% greater radiochemical yields than thermal reactions performed at similar temperatures and over similar reaction times. With a bi-functional molecule, such as DL-pipecolinic acid, [ 18F]beta-fluoroethyl tosylate reacts exclusively with the amino group. Copyright

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2-Fluorobenzaldehyde (1) and pipecolic acid (7) react in dimethyl sulfoxide with potassium carbonate to form benzylidene-oxaindolizidines 4. These diastereomers yield with acids uniform salts, so from 4 with hydrogen chloride results (E)-3-(2-fluorobenzylidene)-1-[1,2-bis(2-fluorophenyl)-2-hydroxyethyl]-3,4, 5,6-tetrahydropyridinium chloride (6·Cl), elucidated by X-ray structural analysis. Treatment of 6·Cl with alkali hydroxide regenerates 4. Similarly proline (13), when treated with two equivalents of 1, gives rise to oxapyrrolizidines 14. From 14 in presence of 1 the perchlorate of the benzylidene derivative 15·ClO4 can be obtained which is transformed to benzylideneoxapyrrolizidines 15 by bases.

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Starting from two acridine compounds identified in a high-throughput screening campaign (1 and 2, Table 1), a series of 4-aminoquinolines was synthesized and tested for their properties on the human alpha2- adrenoceptor subtypes (alpha2A, alpha2B, and alpha2C). A number of compounds with good antagonist potencies against the alpha2C-adrenoceptor and excellent subtype selectivities over the other two subtypes were discovered. For example, (R)-{4-[4-(3,4-dimethylpiperazin-1-yl)phenylamino]quinolin-3-yl}methanol 6j had an antagonist potency of 8.5 nM against, and a subtype selectivity of more than 200-fold for, the alpha2c-adrenoceptor. Investigation of the structure-activity relationship identified a number of structural features, the most critical of which was an absolute need for a substituent in the 3-position of the quinoline ring. The 3-position on the piperazine ring was also found to play an appreciable role, as substitutions in that position exerted a significant and stereospecific beneficial effect on the alpha2C- adrenoceptor affinity and potency. Replacing the piperazine ring proved difficult, with 1,4-diazepanes representing the only viable alternative.

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Chemistry is traditionally divided into organic and inorganic chemistry. Quality Control of: Ethyl pipecolinate. The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent，Which mentioned a new discovery about 15862-72-3

The present invention relates to novel terpene alkaloids and their use as antiparasitic agents. The present invention also relates to an antiparasitic agent which comprises a terpene alkaloid compound of this invention as an effective ingredient in an antiparasitic formulation. More particularly, the present invention relates to derivatives of the terpene alkaloid (1S,2R,4aS,5R,8R,8aR)-2-(acetyloxy)-8a-hydroxy-3,8-dimethyl-5-(1-methylethenyl)-1,2,4a,5,6,7,8,8a-octahydronaphthalen-1-yl (2S,3aR,9bR)-6-chloro-9b-hydroxy-5-methyl-1,2,3,3a,5,9b-hexahydropyrrolo[2,3-c][2,1]benzoxazine-2-carboxylate. Pharmaceutical compositions comprising the same are also disclosed.

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We expand the possibilities in hydrazone based dynamic combinatorial chemistry with a series of new building blocks incorporating heterocyclic motifs. The synthetic procedure allows efficient access to building blocks with the general structure (MeO)2CH-Heterocycle-C(O)NHNH2, originating from heterocycles with an amine and an ester functionality. The equilibrium distribution of macrocyclic N-acyl hydrazones formed upon deprotection of the building blocks with TFA in organic solvents is reported. The mixing behaviour of these heterocycle-based building blocks with our cholate-based building blocks is described, particularly the observation of kinetic intermediates that disappear following ‘proof-reading’. The Royal Society of Chemistry.

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The present invention provides a process for the efficient assembly of Boc-protected 3-aminohydantoins/thiohydantoins and 3-aminodihydrouracils/dihydrothiouracils via a one-pot solution phase or solid phase synthesis from readily available starting materials.

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The highly stereoselective formation of pipecolic acid N-oxide and related derivatives

N-Alkylated derivatives of pipecolic acid are shown to undergo highly stereoselective oxidation to give stable tertiary amine N-oxides. The ester derivatives show a high degree of stability compared to their proline analogues.

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