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Microwave-assisted synthesis of cycloalkanespirohydantoins and piperidinespirohydantoins as precursors of restricted alpha-amino acids

Cycloalkanespirohydantoins 3 and piperidinespirohydantoins 4 were synthesized from cycloalkanones 9 and piperidones 10 under microwave-assisted conditions. Results are compared with those obtained under thermal conditions. Cycloalkanespirohydantoins 3 were N-protected with Boc group and hydrolyzed under basic conditions to obtain five, six and seven-membered ring restricted alpha-amino acids 12 in very good overall yields (76-94%). ARKAT USA, Inc.

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Reference£º
Piperidine – Wikipedia,
Piperidine | C5H320N – PubChem

 

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3-(4-piperidinyl)- and 3-(8-aza-bicyclo[3.2.1]oct-3-yl)-2-phenyl-1H-indoles as bioavailable h5-HT(2A) antagonists

A series of 3-(4-piperidinyl)- and 3-(8-aza-bicyclo[3.2.1]oct-3-yl)-2-phenyl-1H-indoles have been prepared and evaluated as ligands for the h5-HT(2A) receptor. 3-(8-Phenethyl-8-aza-bicyclo[3.2.1]oct-3-yI)-2-phenyl-1H-indole is a high-affinity (1.2nM), selective (>800 fold over h5-HT(2C) and hD2 receptors) antagonist at the h5-HT(2A) receptor with oral bioavailability in rats. (C) 2000 Elsevier Science Ltd.

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INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL

The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.

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A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, COA of Formula: C5H9NO, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 41661-47-6, Name is 4-Piperidinone, molecular formula is C5H9NO. In a Article, authors is Moriarty, Robert M.£¬once mentioned of 41661-47-6

Steric Effects in the Hypervalent Iodine Oxidation of Ketones

Oxidation of 3-cholestanone (1) with C6H5I(OAc)2 or o-OIC6H4COOH or C6H5IO2 in KOH/MeOH yields 2alpha-carbomethoxy-A-norcholestane (2).This result is interpreted on mechanistic grounds and compared with the course of the reaction with other sterically hindered ketones such as friedelin, 3-keto, 12-keto, 17-keto steroids and 2,2,6,6-tetramethyl-4-piperidone.

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Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family

We have previously found that the 4-[4-(N-substituted carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazolines can function as potent and selective inhibitors of platelet-derived growth factor receptor (PDGFR) phosphorylation. A series of highly potent, specific, orally active, small molecule kinase inhibitors directed against members of PDGFR receptor have been developed through modifications of the novel quinazoline template I. Systematic modifications in the A-bicyclic ring and D-rings of protype I were carried out to afford potent analogues, which display IC50 values of <250 nM in cellular betaPDGFR phosphorylation assays. An optimized analogue in this series, 75 (CT53518), inhibits Flt-3, betaPDGFR, and c-Kit receptor phosphorylation with IC50 values of 50-200 nM, whereas 15-20-fold less potent activity against CSF1R was observed. This analogue also inhibits autophosphorylation of Flt-3 ligand-stimulated wild-type Flt-3 and a constitutively activated Flt-3/internal tandem duplication (ITD) with IC50 values of 30-100 nM. Through this optimization process, 75 was found to be metabolically stable and has desirable pharmacokinetic properties in all animal species studied (F% > 50%, T1/2 > 8 h). Oral administration of 75 promotes mice survival and significantly delayed disease progression in a Flt-3/ITD-mediated leukemia mouse model and shows efficacy in a nude mouse model of chronic myelomonocytic leukemia.

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Piperidine | C5H39N – PubChem

 

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Cytotoxic Amides from Fruits of Kawakawa, Macropiper excelsum

Cytotoxic amides have been isolated from the fruits of the endemic New Zealand medicinal plant kawakawa, Macropiper excelsum (Piperaceae). The main amide was piperchabamide A and this is the first report of this rare compound outside the genus Piper. Eleven other amides were purified including two new compounds with the unusual 3,4-dihydro-1(2H)-pyridinyl group. The new compounds were fully characterized by 2D NMR spectroscopy, which showed a slow exchange between two rotamers about the amide bond, and they were chemically synthesized. In view of the antitumor activity of the related piperlongumine, all of these amides plus four synthetic analogs were tested for cytotoxicity. The most active was the piperine homolog piperdardine, with an IC50 of 14 muM against HT 29 colon cancer cells.

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Piperidine | C5H319N – PubChem

 

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Herbicidal 1,2,4,6-thiatriazines

Compounds of formula (I), in which R1, R2 and R3 are as defined in claim 1, are particularly suitable as herbicides.

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Stereoselective strategies for the construction of polysubstituted piperidinic compounds and their applications in natural products’ synthesis

Nitrogen-encompassing bioactive molecules can be regarded as the most frequently cited moieties, occurring either as natural products or as synthetically constructed chemical entities. One such framework which is abundantly found in both natural and synthetic chemical structures is the piperidinic core. A functionalized piperidinic core, either in natural products or in pharmaceuticals, is one of those immensely prevalent moieties. The piperidine frame can be seen in innumerable drug entities and this can be attributed to various reasons like the spacing obtained by piperidine structural conformers during the drug-receptor interactions, and solubility enhancement, hence resulting in improved pharmacokinetics and, most importantly, making the drug architecture metabolically stable. Further tapering down, 2, 4 and 6 substituted piperidines in general and with chiral centres in specific have attracted a substantial amount of attention in the recent past. This can be attributed to their diverse biological activities like analgesic, antimicrobial, sedative, antiasthmatic etc. In this communication, we aim to sum up and review all the reported methods since 2009 for the construction of the polysubstituted piperidinic core. Each method cited herein is exemplified with the synthesis of a natural compound and particularly alkaloids.

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CDK4/6 inhibitors and its preparation method and application (by machine translation)

The invention relates to CDK4/6 inhibitors and its preparation method and application. In particular, the invention relates to the general formula (I) compound of formula, its preparation method and containing pharmaceutical compositions of the compounds, and their use as CDK4/6 kinase inhibitor in the preparation of the prevention and/or treatment of cancer or tumor-related disorders especially bladder cancer, ovarian cancer, peritoneal carcinoma, pancreatic cancer, breast cancer, uterine cancer, cervical cancer, endometrial cancer, prostate cancer, female […], testicular cancer, gastrointestinal stromal tumor or prostate tumor medicament for use in the, is expected to be developed into a new generation of CDK4/6 inhibitor drugs. Wherein the general formula (I) of each substituent in the definition in the description of the same. (by machine translation)

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A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, Computed Properties of C5H9NO, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 41661-47-6, Name is 4-Piperidinone, molecular formula is C5H9NO. In a Patent, authors is £¬once mentioned of 41661-47-6

Preparation rifamycin S derivatives (by machine translation)

The invention relates to a process for preparing rifamycin S derivatives. In accordance with the certain charging mode, as shown in formula II 3 – amino -4 – imino rifamycin S shown in formula III 4 – piperidone derivative in an organic solvent, in the presence of acetic acid to plated zinc powder, a condensation reaction, shown as formula I obtained of the rifamycin S derivatives; the feed way: the 3 – amino -4 – imino rifamycin S in the last step are added to a reaction system, the method avoids the 3 – amino -4 – imino rifamycin S is reduced and is hydrolysis of the, improving utilization ratio, mild reaction conditions, the relative shortening the reaction time, it can be efficient, high yield to obtain the rifamycin S derivatives, yield 80% or more, the content of 95% or more, overcomes the problems in the prior art long reaction time, the yield is low, a plurality of impurities, and the cost is high, and the operation is simple, high efficiency and environmental protection, is conducive to large-scale production. (by machine translation)

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Piperidine – Wikipedia,
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