37675-19-7Relevant academic research and scientific papers
HMPA-catalyzed transfer hydrogenation of 3-carbonyl pyridines and other N-heteroarenes with trichlorosilane
Fu, Yun,Sun, Jian
, (2019/02/06)
A method for the HMPA (hexamethylphosphoric triamide)-catalyzed metal-freetransfer hydrogenation of pyridines has been developed. The functional group tolerance of the existing reaction conditions provides easy access to various piperidines with ester or ketone groups at the C-3 site. The suitability of this method for the reduction of other N-heteroarenes has also been demonstrated. Thirty-three examples of different substrates have been reduced to designed products with 45–96% yields.
SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF
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Page/Page column 30; 31, (2018/03/28)
Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders. Orally delivered formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
JAK INHIBITOR
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Paragraph 0065; 0066; 0067, (2017/12/15)
The present invention discloses a series of JAK inhibitors, and particularly discloses a compound of formula (I) or a pharmaceutically acceptable salt thereof and the use thereof in preparation of drugs for treating diseases related to JAK.
PROCESS FOR PREPARING ENANTIOMERICALLY ENRICHED 3-HYDROXYMETHYLPIPERIDINE
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Page/Page column 16, (2014/11/13)
The present invention relates to a process for preparing enantiomerically enriched 3-hydroxymethylpiperidine and in particular of the S-enantiomer of (S)-3-hydroxymethyl- piperidine in high chemical and optical purity. The invention also relates to extremely pure (S)-3-hydroxymethylpiperidine and (R)-3-hydroxymethylpiperidine.
BENZOXAZOLE CARBOXAMIDE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP)
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Page/Page column 80, (2009/08/16)
A compound having the structure set forth in Formula (I) or Formula (II): wherein the variables Y, R1, R2, R3, and R4 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.
NOVEL INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP)
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Page/Page column 47-48, (2009/04/24)
A compound having the structure set forth in Formula (I): wherein the variables Y, R1, R2, R3, R4 and R5 are as defined herein. Compounds described herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of such compounds and pharmaceutical compositions to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity
A General, Selective, High-Yield N-Demethylation Procedure for Tertiary Amines by Solid Reagents in a Convenient Column Chromatography-like Setup
Rosenau, Thomas,Hofinger, Andreas,Potthast, Antje,Kosma, Paul
, p. 541 - 544 (2007/10/03)
(Equation presented) A traditional preparative chromatographic column can be used to achieve quantitative N-demethylation of tertiary N-methylamines and alkaloids. The filling is the crucial part and is loaded with different solid reagents in three reaction zones. The parent compound is charged on the column, and the neat N-demethylated secondary amine leaves the column some minutes later.
Oligomers of β2- and of β3-homoproline: What are the secondary structures of β-peptides lacking H-bonds?
Abele, Stefan,Voegtli, Kurt,Seebach, Dieter
, p. 1539 - 1558 (2007/10/03)
To study the role of H-bonds in stabilizing β-peptidic secondary structures, we have synthesized β-oligopeptides (up to the octadecamer 12) consisting of β2- and β3-homoproline, i.e., β-peptides lacking amide protons. The enantiomer purity of the building block β2-homoproline (nipecotic acid, 4) was determined by HPLC analysis of the N-(2,4- dinitrophenyl) derivative 5 on a Chiralcel-OD column (cf. Fig. 2). The CD spectra of the all-(S)-β2- and all-(S)-β3-HPro-containing, β-peptides display novel and intensive CD patterns which may be indicative of a secondary structure (cf. Fig. 3). It is noteworthy that a distinct CD pattern was observed with the β3-HPro derivatives containing as few as three residues (7a). The crystal structure of a N-deprotected β3-HPro-tripeptide 7c is presented (cf. Figs. 4 and 5), and a model for the structure of β- peptides consisting of β3-HPro is discussed (cf. Figs. 6 and 7).
