71233-28-8

Upstream product

• 71233-25-5 ethyl 1-tert-butoxycarbonyl-3-oxopiperidine-4-carboxylate 
• 941571-79-5 ethyl 3-hydroxypiperidine-4-carboxylate 
• 24424-99-5 di-tert-butyl dicarbonate 
• 70637-75-1 ethyl 3-oxopiperidine-4-carboxylate 
• 52763-21-0 ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride 

Downstream Products

• 203663-26-7 t-butyl 4-(hydroxymethyl)-3,6-dihydropyridine-1(2H)-carboxylate 
• 1260876-51-4 1-tert-butoxycarbonyl-3-hydroxypiperidine-4-carboxylic acid 
• 203503-03-1 4-amino-3-hydroxy-piperidine-1-carboxylic acid tert-butyl ester 
• 1427170-55-5 C₆H₁₀N₂O₂*ClH 
• 906663-63-6 4-[1-(1-benzylsulfanylmethyl-4-butylcarbamoyl-2-hydroxypentylcarbamoyl)ethylcarbamoyl]-3-(5-hydroxypent-3-enyl)piperidine-1-carboxylic acid tert-butyl ester 
• 906663-62-5 4-[1-(1-benzylsulfanylmethyl-4-butylcarbamoyl-2-hydroxypentylcarbamoyl)ethylcarbamoyl]-3-(5-hydroxypent-3-enyl)piperidine-1-carboxylic acid tert-butyl ester 
• 906663-27-2 3-benzylsulfanyl-4-[1-(1-benzylsulfanylmethyl-4-butylcarbamoyl-2-hydroxypentylcarbamoyl)ethylcarbamoyl]piperidine-1-carboxylic acid tert-butyl ester 
• 906663-33-0 3-benzylsulfanyl-4-[1-(1-benzylsulfanylmethyl-4-butylcarbamoyl-2-hydroxypentylcarbamoyl)ethylcarbamoyl]piperidine-1-carboxylic acid tert-butyl ester 

Relevant academic research and scientific papers

Structure-based design and synthesis of macroheterocyclic peptidomimetic inhibitors of the aspartic protease β-site amyloid precursor protein cleaving enzyme (BACE)

Based on the X-ray cocrystal structure of the Tang-Ghosh heptapeptide inhibitor 1 (OM00-3), a series of macroheterocyclic analogues were designed and synthesized. Analogues containing dithia, dioxa, oxathia, and carbathia macrocycles were synthesized by m

C10-ALKYLENE SUBSTITUTED 13-MEMBERED MACROLIDES AND USES THEREOF

Provided are 13-membered macrolides for the treatment of infectious diseases. The 13-membered macrolides described herein are azaketolides. Also provided are methods for preparing the 13- membered macrolides, pharmaceutical compositions comprising the 13-membered macrolides, and methods of treating infectious diseases, and in particular, disease resulting from Gram negative bacteria using the disclosed macrolides. Formula (I)

QUINAZOLINE COMPOUND FOR EGFR INHIBITION

Disclosed is a novel quinazoline compound. Specifically, disclosed are a compound represented by the formula (I) and a pharmacologically acceptable salt.

Synthesis and in vitro antibacterial activity of quinolone/naphthyridone derivatives containing 3-alkoxyimino-4-(methyl)aminopiperidine scaffolds

We report herein the synthesis of a series of 7-[3-alkoxyimino-4-(methyl) aminopiperidin-1-yl]quinolone/naphthyridone derivatives. In vitro antibacterial activity of these derivatives was evaluated against representative strains, and compared with ciprofl

Reagents for assaying central local acetylcholinesterase activity

The present invention relates to N-alkylpiperidine derivatives represented by general formula (1) or (2); wherein R1represents optionally fluorinated lower alkyl; R2represents lower alkyl; and R3represents alkenyl substituted at the 1-position with hydroxy, lower alkoxy, lower alkoxyalkyloxy, lower alkoxyalkyloxyalkyloxy, or lower alkanoyloxy and substituted at the end with radioactive iodine, or alkenyloxymethyl substituted at the end with a radioactive iodine reagent containing the same for assaying central local AchE activity; a method for assaying the central local AchE activity; and labeled precursors of the above compounds. After easily passing through the blood-brain barrier, these compounds are hydrolyzed specifically by AchE in the brain into alcohols, which are then captured by the brain. In contrast, alcohols formed outside the brain do not migrate into the brain. The compounds of the invention emit γ-rays at an appropriate energy level. These characteristics make the compounds highly useful as tracers for SPECT in assaying the central AchE activity.

Synthesis of N-methyl-3-acetoxy-4-(1-hydroxy-3-[123I]iodoprop-2-enyl) piperidine, a novel acetylcholine analog

Lipophilic acetylcholine analogs (N-methylpiperidine derivatives) have been used to map central acetylcholinesterase (AchE) activity in animals and humans. In the former meeting, we reported synthesis of an analog with 4-acetoxy group and side chain at 3-position labeled with iodine-123 (MHIP4A) which showed moderate metabolic clearance. Now, we have synthesized another analog with higher metabolic clearance, namely, N-methyl-3-acetoxy-4-(1-hydroxy-3-[123I]iodoprop-2-enyl)piperidine (HIP3C3A). Eight isomers of HIP3C3A were isolated by diastereomeric and enantiomeric separation with silica gel chromatography and chiralcel HPLC. Tributylstannyl precursors were used for iodination with peracetic acid as an oxidizing agent. The iodination could be carried out quite easily yielding 50-60%. Of the isomers, one isomer showed extremely high metabolic clearance (4.19 mL/min/g with 84% specificity) and another isomer was hydrolyzed by AchE moderately (0.36 mL/min/g with 95% specificity) in rat cerebral cortical homogenate.

GABA agonists. Synthesis and structure-activity studies on analogues of isoguvacine and THIP

A series of analogues of the specific GABA receptor agonists isoguvacine, isonipecotic acid, and THIP (4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol) have been synthesized and tested as inhibitors of the binding of 3H-GABA to GABA receptor sites on rat brain membranes in vitro. Introduction of a hydroxy group into the 3- or 4-position of isonipecotic acid results in compounds with considerably reduced receptor affinity. The 7-membered ring analogues of isoguvacine and isonipecotic acid are more than two orders of magnitude weaker than the parent compounds. Replacement of the 3-isoxazolol unit of THIP by related heterocyclic rings also result in dramatic loss of activity. Thus iso-THIP (4,5,6,7-tetrahydroisoxazolo[3,4-c]pyridin-3-ol) is a weak inhibitor of 3H-GABA binding, whereas the 3-pyrazolol THIP analogues are inactive.