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Boric acid: a new regiospecific decarboxylating agent. Syntheses of cyclic imines, beta-enaminones, and beta-enaminodiketones from beta-enaminoesters

The synthesis of cyclic imines 2, beta-enaminones 6, and beta-enaminodiketones 7 is described.Regio- and stereospecific thermolysis of beta-enaminoesters 4 with boric acid permit these preparations in generally good yields. Key words: boric acid, cyclic beta-enaminoesters, decarboxylation, cyclic imines, cyclic beta-enaminones.

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Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem

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Synthesis of 5-amino-4-(2-azacycloalkylidene)-2-phenyl-2,4-dihydro-3H- pyrazol-3-ones

The reaction 5-amino-2-phenyl-3,4-dihydro-3H-pyrazol-3-one with activated lactams (lactim ethers, lactam acetals, and methylthioalkylidene iminium salts) was investigated. It occurs on the active methylene group of 5-amino-2-phenyl-3,4-dihydro-3H-pyrazol-3-one to furnish cyclic enamines, 5-amino-4-(2-azacycloalkylidene)-2-phenyl-2,4-dihydro-3H-pyrazol-3-ones and 5-amino-4-(1-methyl-2-azacycloalkylidene)-2-phenyl-2,4-dihydro-3H-pyrazol-3- ones. Georg Thieme Verlag Stuttgart.

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Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem

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Synthesis and stereochemistry of 8,13-diaza-2,3-dimethoxygona-1,3,5(10),9(11)-tetraen-12-one and D-homo derivatives

From the condensation reaction of O-methylbutyrolactim (2), O-methylvalerolactim (3), O-methylcaprolactim (4) and O-methyl-4-t-butylcaprolactim (5) with ethyl 6,7-dimethoxy-alpha-<1,2,3,4-tetrahydro-isoquinoyl)>acetate (1), 8,13-diaza-2,3-dimethoxygona-1,3,5(10),9(11)-tetraen-12-one (6) D-homo-derivatives (7-9), and medium sized ring cyclic diamides (10,11) were obtained.The stereoselective reduction of compounds 6-9 by Adam’s platinum catalyst afforded 8,13-diaza-2,3-dimethoxygona-1,3,5(10)-trien-12-one (12) and its D-homo derivatives (13-15).The structures of thecompounds obtained were established by NMR and X-ray crystallographic analyses. – Keywords: 8,13-diazasteroids; stereochemistry; X-ray structure analysis

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Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem

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Discovery of R-142086 as a factor Xa (FXa) inhibitor: Syntheses and structure-activity relationships of cinnamyl derivatives1,2

To develop a novel and effective anticoagulant with potent and selective factor Xa (FXa) inhibitory activity, a new series of cinnamyl derivatives with enhanced lipophilicity and prodrug forms were synthesized and their biological activities were evaluated. As a result, we found that cinnamyl derivative (N-{4-[1-(acetimidoyl)-piperidin-4-yloxy]-3-carbamoylphenyl}-N-[(Z) -3-(3-amidinophenyl)-2-fluoro-2-propenyl]sulfamoyl)acetic acid di-hydrochloride (26d, R-142086) with a fluorine atom on the double bond exhibited potent anticoagulant activity and no mutagenic potential. Moreover, orally administered R-142086 exhibited potent anti-FXa activity and anticoagulant activity in dogs.

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Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem

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N-(1-PHENYL-2-ARYLETHYL)-4,5-DIHYDRO-2H-PYRROL-5-AMINE COMPOUNDS AS SUBTYPE SELECTIVE MODULATORS OF ALPHA2B OR ALPHA2B AND ALPHA2C ADRENOCEPTORS

The present invention provides compounds which are N-(1-phenyl-2-arylethyl)-4,5-dihydro-2H-pyrrol-5-amine compounds and are subtype selective modulators of alpha 2B or alpha 2B and alpha 2C adrenoreceptors and are selected from the group of compounds represented by the formula

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Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem

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METALLOENZYME INHIBITOR COMPOUNDS

Provided are compounds having HDAC6 modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by HDAC6.

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Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem

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PYRAZOLINES AS PAR-1 ANTAGONISTS FOR TREATMENT OF CARDIOVASCULAR DISEASES

The invention relates to pyrazolines of formula (I), where E = methylene, NH, O or S and R2 = a group of formula (II), methods for the production and use thereof for the production of medicaments for the treatment and/or prophylaxis of diseases, in particular, cardiovascular diseases, such as thromboembolitic diseases.

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Reference£º
Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem

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Synthesis of lipoxygenase inhibitors. Part 2: Synthesis of lactamarylhydrazones and tetrahydroazepinochinazolinon-arylhydrazones

The synthesis of lactamarylhydrazones as cyclic amidrazones is described starting from 5-, 6- and 7-membered lactames. Tetrahydroazepinochinazolinonarylhydrazones were prepared from caprolactam. The compounds were tested against soja lipoxygenase. A few compounds were very strong inhibitors (IC50 value up to 4.10-9 mol/l).

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Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem

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Substituted triazole compound, pharmaceutical composition, containing same, and, preparation method and application thereof (by machine translation)

The present invention relates to (I) a substituted triazole-based compound, of Formula (I,), a pharmaceutical composition comprising the same, a method for 1(ASK1) preparing the same, and a use. of the same for the prevention or treatment of a disease or condition mediated by an apoptosis signal-modulating kinase. (by machine translation)

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Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem

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Potent antimalarial activity of 2-aminopyridinium salts, amidines, and guanidines

We describe the design, synthesis, and antimalarial activity of 60 bis-tertiary amine, bis-2(1H)-imino-heterocycle, bis-amidine, and bis-guanidine series. Bis-tertiary amines with a linker from 12 to 16 methylene groups were active against the in vitro growth of Plasmodium falciparum within the 10 -6-10-7 M concentration range. IC50 decreased by 2 orders of magnitude for bis-2-aminopyridinium salts, bis-amidines, and bis-guanidines (27 compounds with IC50 < 10 nM). Increasing the alkyl chain length from 6 to 12 methylene groups led to increased activity, while beyond this antimalarial activity decreased. Antimalarial activities appear to be strictly related to the basicity of the cationic head with an optimal pKa over 12.5. Maximal activity occurs for bis-2-aminopyridinium, two C-duplicated bis-amidines, and three bis-guanidines, with IC50 values lower than 1 nM. In comparison to similar quaternary ammonium salts, amidinium compounds have distinct structural requirements for antimalarial activity and likely additional binding opportunities on account of their hydrogen-bond-forming properties. The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 5264-35-7 is helpful to your research. Related Products of 5264-35-7

Reference£º
Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem