7037-49-2

Usage

Uses

Used in Pharmaceutical Synthesis:
Piperidine-4-propanol is used as a key intermediate in the synthesis of G-protein coupled receptor (GPR119) agonists based on a bicyclic amine scaffold. These agonists have potential applications in the treatment of type 2 diabetes and obesity by stimulating insulin secretion and reducing glucose production in the liver.
Used in Antimicrobial Applications:
Piperidine-4-propanol is used in the synthesis and antimicrobial activities of novel quinoline derivatives. These quinoline-based compounds have potential applications in the development of new antibiotics to combat drug-resistant bacterial infections.
Used in Chemical Research:
Piperidine-4-propanol is also used as a starting material or reagent in various chemical reactions and research studies, contributing to the discovery and development of new chemical entities and pharmaceuticals.

InChI:InChI=1/C8H17NO/c10-7-1-2-8-3-5-9-6-4-8/h8-10H,1-7H2

Upstream product

• 2629-72-3 4-(3-Hydroxypropyl)pyridine 
• 71879-55-5 ethyl 3-(piperid-4-yl)propionate 
• 156185-63-6 N-Boc-piperidin-4-yl-propanol 
• 15854-87-2 4-iodopyridine 
• 93524-95-9 3-(pyridin-4-yl)propane-2-yn-1-ol 

Downstream Products

• 7037-30-1 3-(1-methylpiperidin-4-yl)propan-1-ol 
• 156185-63-6 N-Boc-piperidin-4-yl-propanol 
• 193626-88-9 1-(3-(4-piperidyl)propyl)-2-(4-chlorophenoxymethyl)-4-methylbenzimidazole 
• 193626-34-5 1-(3-(4-(N-BOC-piperidyl))propyl)-2-(4-chlorophenoxymethyl)-4-methylbenzimidazole 
• 251369-19-4 2-(4-chloro-phenoxymethyl)-1-{3-[1-(3-[1,3]dioxolan-2-yl-propyl)-piperidin-4-yl]-propyl}-4-methyl-1H-benzoimidazole 
• 251369-17-2 1-(3-(4-(1-N-BOC-3-aminopropyl)piperidyl)propyl)-2-(4-chlorophenoxymethyl)-4-methylbenzimidazole 

Relevant academic research and scientific papers

N-ARYL AND N-HETEROARYL PIPERIDINE DERIVATIVES AS LIVER X RECEPTOR β AGONISTS, COMPOSITIONS, AND THEIR USE

Provided herein are certain substituted N-aryl and N-heteroaryl piperidine compounds of the formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, L, R4, L1, Q, R5 and R 6 are as defined. The said novel compounds, and pharmaceutically acceptable compositions comprising a compound thereof, may be useful as Liver X-β receptor(LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory disease and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.

Preparation of monoalkylpiperidines via the mild hydrogenation of monoalkynylpyridines

Monoalkynylpyridines were prepared via a Sonogashira cross-coupling reaction between monoiodopyridines and alkynes. Mild hydrogenation of the obtained monoalkynylpyridines was then conducted to produce the corresponding monoalkylpiperidines in moderate to excellent yields. The hydrogenation reaction was carried out under H2 (1?atm) in the presence of 10?wt% Pd/C (5?eq) in either AcOH or MeOH at room temperature. The present mild method is therefore useful for the quick and easy preparation of monoalkylpiperidines.

METHOD FOR PRODUCING PIPERIDINE COMPOUND

PROBLEM TO BE SOLVED: To provide a method for producing a piperidine compound in an industrially convenient manner. SOLUTION: This invention relates to a method for producing a compound represented by general formula (I) or a salt thereof that includes the step of converting a pyridine compound having an alkynylene group in a side chain, by a contact hydrogenation reaction, into the compound represented by general formula (I) or a salt thereof (in the general formula (I), R1 is a hydrogen atom, a hydroxy group, or an optionally substituted alkyl group having carbon atoms of 1 or more and 20 or less). SELECTED DRAWING: None COPYRIGHT: (C)2018,JPOandINPIT

9H-PYRROLO-DIPYRIDINE DERIVATIVES

The invention relates to 9H-pyrrolo-dipyridine derivatives of formula I, processes for preparing them, pharmaceutical compositions containing them and their use as radiopharmaceuticals in particular as imaging agents for the detection of Tau aggregates.

M2 Subtype preferring dibenzodiazepinone-type muscarinic receptor ligands: Effect of chemical homo-dimerization on orthosteric (and allosteric?) binding

A series of new dibenzodiazepinone-type muscarinic receptor ligands, including two homo-dimeric compounds, was prepared. Sixteen representative compounds were characterized in equilibrium binding studies with [3H]N-methylscopolamine ([3H]NMS) at the muscarinic receptor subtype M2, and seven selected compounds were additionally investigated at M1, M3, M4 and M5 with respect to receptor subtype selectivity. The side chain of the known M2 preferring muscarinic receptor antagonist DIBA was widely varied with respect to chain length and type of the basic group (amine, imidazole, guanidine and piperazine). Most of the structural changes were well tolerated with respect to muscarinic receptor binding, determined by displacement of [3H]NMS. Compounds investigated at all subtypes shared a similar selectivity profile, which can be summarized as M2 > M1 ≈ M4 > M3 ≈ M5 (46, 50, 57, 62-64) and M2 > M1 ≈ M4 > M3 > M5 (1, 58). The homo-dimeric dibenzodiazepinone derivatives UNSW-MK250 (63) and UNSW-MK262 (64) exhibited the highest M2 receptor affinities (pIC50 = 9.0 and 9.2, respectively). At the M2 receptor a steep curve slope of -2 was found for the dimeric ligand 63, which cannot be described according to the law of mass action, suggesting a more complex mechanism of binding. In addition to equilibrium binding studies, for selected ligands, we determined pEC50,diss, an estimate of affinity to the allosteric site of M2 receptors occupied with [3H]NMS. Compounds 58 and 62-64 were capable of retarding [3H]NMS dissociation by a factor >10 (Emax,diss >92%), with highest potency (pEC50,diss = 5.56) residing in the dimeric compound 64. As the monomeric counterpart of 64 was 100 times less potent (62: pEC50,diss = 3.59), these data suggest that chemical dimerization of dibenzodiazepinone-type M receptor ligands can enhance allosteric binding.

Synthesis and SAR studies of bicyclic amine series GPR119 agonists

We disclosed a novel series of G-protein coupled receptor 119 (GPR119) agonists based on a bicyclic amine scaffold. Through the optimization of hit compound 1, we discovered that the basic nitrogen atom of bicyclic amine played an important role in GPR119 agonist activity expression and that an indanone in various bicyclic rings was suitable in this series of compounds. The indanone derivative 2 showed the effect of plasma glucose control in oGTT and scGTT in the rodent model.

Process for the preparation of substituted pyrimidine derivatives

The present invention is directed to processes for the preparation of substituted pyrimidine derivatives, useful as intermediates in the synthesis of histamine H4 receptor modulators, and to intermediates in H4 modulator synthesis.

COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY

The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.

FUSED BENZENE DERIVATIVE AND USE

The present invention provides a compound represented by the general formula: [wherein Ring A represents an optionally substituted 5- to 8-membered ring, Ring B represents a further optionally substituted 4- to 10-membered ring, Ring C represents a further optionally substituted benzene ring, X1 represents carbon atom, X2 represents a carbon atom, an oxygen atom, etc., W represents a nitrogen atom, etc., Y11 represents a group represented by the formula CR2R3' (wherein R2 represents a hydrogen atom, a cyano group, a nitro group, etc., and R3' represents a hydrogen atom, a cyano group, a nitro group, etc., respectively), Y21 represents a group represented by the formula CR4R5' (wherein R4 represents a hydrogen atom, a cyano group, a nitro group, etc., and R5' represents a hydrogen atom, a cyano group, a nitro group, etc., respectively), etc., and R1 represents an electron-withdrawing group, respectively. The formula represents a single bond or a double bond] or a salt thereof, which is useful as an androgen receptor modulator.

Synthesis of cyclic prodrugs of Aggrastat and its analogue with a modified phenylpropionic acid linker

(formula presented) 1a, n=2; 1b, n=1 The objective of this work was to synthesize cyclic prodrugs 1a and 1b from Aggrastat 2a and its analogue 2b, respectively, to improve their membrane permeation. Cyclic prodrugs 1a and 1b were formed using an ester bond between the -COOH group of Aggrastat or its analogue and the phenylpropionic acid linker 3 and an amide bond between the piperidinylamine and the -COOH group of the linker 3, respectively, as outlined in Scheme 4.