39124-19-1

Upstream product

• 29943-42-8 Tetrahydro-4H-pyran-4-one 
• 151-50-8 potassium cyanide 
• 506-87-6 ammonium carbonate 
• 773837-37-9 sodium cyanide 

Downstream Products

• 39124-20-4 4-aminotetrahydro-2H-pyran-4-carboxylic acid 
• 172843-97-9 4-(Boc-amino)tetrahydropyran-4-carboxylic acid 
• 1367370-17-9 C₃₂H₄₉N₇O₉ 
• 1367370-34-0 C₅₇H₈₆N₁₂O₁₄ 
• 1361185-26-3 cyclopentyl 4-{[(benzyloxy)carbonyl]amino}tetrahydro-2H-pyran-4-carboxylate 
• 138402-13-8 4-{[(benzyloxy)carbonyl]amino}oxane-4-carboxylic acid 
• 951401-15-3 (4-isobutylcarbamoyl-tetrahydro-pyran-4-yl)-carbamic acid benzyl ester 

Relevant academic research and scientific papers

SUBSTITUTED-PYRIDINYL COMPOUNDS AND USES THEREOF

The present application relates generally to compounds useful for the treatment and/or enhancement of cognitive dysfunction and negative symptoms associated with CNS disorders where the circuitry involving fast spiking PV+ interneurons and the production of cortical gamma oscillations is disrupted. The subject disclosure enables the manufacture of medicaments as well as compositions containing same for use in methods of therapy and prophylaxis of cognitive dysfunction and negative symptoms.

A 4 - amino-tetrahydro -2 - pyran -4 - carboxylic acid

The invention discloses a 4 - amino-tetrahydro - 2 - pyran - 4 - carboxylic acid, belongs to a chemical intermediate, its technical point includes the step one, will be four dihydropyrone adding water and in ethanol, then adding ammonium carbonate and sodium cyanide, heated to 60 - 70 °C reaction 3 - 4 h, subsequently cooling down to 5 - 10 °C, filtering and drying after a to the intermediate; step two, the intermediate in a added to the DMF, then adding DMAP, [...] carbon acid di-tert-butyl, heating up to 80 - 100 °C, reaction 16 - 20 h poured into the water after stirring 2 - 3 h, obtained after filtering the intermediate b; step three, the intermediate II by adding in tetrahydrofuran, then adding 40 - 60 wt % of sodium hydroxide solution, heating to reflux 5 - 6 h, steams tetrahydrofuran, then hydrochloric acid for pH adjustment to 2 - 4 after solid precipitation, filtration and drying to obtain the 4 - amino-tetrahydro - 2 - pyran - 4 - carboxylic acid.

Microwave-assisted synthesis of functionalized spirohydantoins as 3-D privileged fragments for scouting the chemical space

Fragment-based drug design has been successfully applied to a large set of proteins, however in order to expand this concept to the most demanding targets, such as protein-protein interactions, it is required to enrich current fragment libraries with new and original 3D privileged fragments. Our goal was to develop a rapid microwave-assisted synthesis of 27 new privileged spirohydantoin fragments. Among them 24 compounds showed a high water solubility. These molecules were plotted according to the normalized principal moments of inertia of their minimized conformers, and most of the compounds were prone to occupy under-populated regions of the triangular plot. Finally we demonstrated that the hydantoin ring can be selectively N-monoalkylated providing the access to rapid functionalization for further elaboration.

PEPTIDYL NITRIL COMPOUNDS AS DIPEPTIDYL PEPTIDASE I INHIBITORS

The invention relates to compounds of Formula (I) and their use as selective dipeptidyl peptidase I inhibitors, as well as pharmaceutical compositions comprising said compounds, and methods of treatment involving said compounds.

NIPECOTIC ACID DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES

The present invention aims to provide a compound having an sEH-inhibiting activity and to provide a pharmaceutical having a therapeutic effect and a prophylactic effect on chronic renal disease and pulmonary hypertension based on the sEH-inhibiting action. The present invention provides nipecotic acid derivatives represented by the chemical formula below and pharmaceutically acceptable salts thereof.

ALPHA, ALPHA - DI SUBSTITUTED GLYCINE ESTER DERIVATIVES AND THEIR USE AS HDAC INHIBITORS

Compounds selected from the following group and their salts are inhibitors of HDAC activity, useful in the treatment of, inter alia, cell proliferative disease and inflammation: Cyclopentyl 1 -[({5-[(1E)-3-(hydroxyamino)-3-oxoprop-1-en-1-yl]pyridin-2- yl}methy)amino]cyclopropanecarboxylate; Cyclopentyl 1 -[({5-[(1E)-3-(hydroxyamino)-3- oxoprop-1-en-1-yl]pyridin-2-yl}methy)amino]cyclobutanecarboxylate; Cyclopentyl 1-[({5- [(1E)-3-(hydroxyamino)-3-oxoprop-1-en-1-yl]pyridin-2yl}methyl)amino]- cyclopentanecarboxylate; Cyclopentyl 1-[({5-[(1E)-3-(hydroxyamino)-3-oxoprop-1-en-1- yl]pyridin-2-yl}methyl)amino]cyclohexanecarboxylate; Cyclopentyl 4-[({5-[(1E)-3- (hydroxyamino)-3-oxoprop-1 -en-1 -yl]pyridin-2-yl}methyl)amino]tetrahydro-2H-pyran-4- carboxylate; Cyclopentyl 4-[({6-[(1E)-3-{[1 -(2-methylpropoxy)ethoxy]amino}-3-oxoprop-1 - en-1 -yl]pyridin-3-yl}methyl)amino]tetrahydro-2H-pyran-4-carboxylate; Cyclopentyl 1 -({4- [(1E)-3-(hydroxyamino)-3-oxoprop-1-en-1-yl]-2-methylbenzyl}amino)- cyclohexanecarboxylate; Cyclopentyl 1-({4-[(1E)-3-(hydroxyamino)-3-oxoprop-1-en-1-yl]- 2-methylbenzyl}amino)cyclopentanecarboxylate; Cyclopentyl 1-({4-[(1E)-3- (hydroxyamino)-3-oxoprop-1-en-1-yl]-2-methylbenzyl}amino)cyclobutanecarboxylate; Methylcyclopentyl 4-[({6-[(1E)-3-(hydroxyamino)-3-oxoprop-1-en-1-yl]pyridin-3- yl}methyl)amino]tetrahydro-2H-pyran-4-carboxylate; Cyclopentyl 4-{[1 -({6-[(1E)-3- (hydroxyamino)-3-oxoprop-1-en-1-yl]pyridin-3-yl}methyl)piperidin-4-yl]amino}tetrahydro- 2H-pyran-4-carboxylate; Cyclopentyl 4-{[1-({5-[(1E)-3-(hydroxyamino)-3-oxoprop-1-en-1- yl]pyridin-2-yl}methyl)piperidin-4-yl]amino}tetrahydro-2H-pyran-4-carboxylate; Cyclopentyl 4-({4-[(1E)-3-(hydroxyamino)-3-oxoprop-1-en-1-yl]benzyl}amino)tetrahydro- 2H-pyran-4-carboxylate; Cyclopentyl 4-({3-[(1E)-3-(hydroxyamino)-3-oxoprop-1 -en-1 - yl]benzyl}amino)tetrahydro-2H-pyran-4-carboxylate; and (3R)-Tetrahydrofuran-3-yl N-{4- [(1E)-3-(hydroxyamino)-3-oxoprop-1-en-1-yl]benzyl}-2-methyl-D-leucinate.

Chemical communication: Conductors and insulators of screw-sense preference between helical oligo(aminoisobutyric acid) domains

1H NMR studies quantify the abilities of achiral amino acids to communicate a left-handed screw-sense preference from one helical Aib 4 domain to another: certain quaternary amino acids (e.g. Ac 6c) act as effective conductors of conformational preference while others (e.g. diphenylglycine) acts as insulators.

AMIDE STABILIZED HYDROXYETHYLAMINES

This invention pertains to amide and ester derivatives of hydroxyethylamine compounds that serve as effective beta-secretase inhibitors. The invention further relates to intermediates for preparation of such compounds; pharmaceutical compositions comprisi

A new series of cyclic amino acids as inhibitors of S-adenosyl L- methionine synthetase

Optically active 3-amino-3-(tetrahydrofuranyl) carboxylic acid, 3- amino-3-(tetrahydrothienyl) carboxylic acid and their corresponding six membered ring analogues have been synthesised and examined as potential inhibitors of the enzyme S-adenosylmethionine (AdoMet) synthetase. The kinetic behaviour of these compounds was studied using recombinant rat liver AdoMet synthetase (α-isoform) fractionated from E. coli transformed with the plasmid pSSRL-T7N. All the compounds tested were competitive inhibitors of the enzyme with respect to L-methionine.

Hydrogen-bonded tapes based on symmetrically substituted diketopiperazines: A robust structural motif for the engineering of molecular solids

A series of eight symmetrically substituted diketopiperazines (DKPs) derived from 1-amino-1-carboxycycloalkanes (n = 3-7; 3,3,5,5-tetramethylcyclohexane; 4,4-dimethylcyclohexane; 2-indan) were synthesized and their crystal structures determined. In the solid state, all eight compounds form two pairs of hydrogen bonds with two adjacent molecules to form a one-dimensional structure that we refer to as 'tapes'. These molecules represent a range of volumes and shapes that contain a common molecular fragment (DKP ring). We examined this series of compounds with three objectives in mind: (i) to establish the ability of the hydrogen-bonded 'tape' motif to persist through these differences in volume and shape; (ii) to provide a series of structurally related compounds to use to test computational methods of predicting crystal structure from molecular structure; (iii) to search for qualitative correlations between molecular structure and crystal packing. All compounds form tapes and with one exception, all tapes pack with their long axes parallel. When viewed down their long axis, two types of tapes emerge: planar and nonplanar. The type of tape that forms reflects the conformation adapted by the DKP ring-planar or boat. Planar tapes form when the angle (α) between the two planes defined by the cis-amides in the DKP ring is 180°; nonplanar tapes form when α 180°. Five of the eight compounds studied form planar tapes, the remaining three compounds form nonplanar tapes. Despite the variability in volume and shape represented by this series of molecules, the persistence of the tape motif in their crystalline solids suggests that the hydrogen-bonding interactions between parallel alignment of tapes that pack in a manner that permits the interdigitation of substituents on adjacent tapes.