183673-66-7

Usage

Uses

Used in Pharmaceutical Industry:
4-(9H-FLUOREN-9-YLMETHOXYCARBONYLAMINO)-PIPERIDINE-1,4-DICARBOXYLIC ACID MONO-TERT-BUTYL ESTER is used as a synthetic intermediate for the preparation of various pharmaceutical compounds. Its unique structure allows it to be a valuable building block in the synthesis of complex molecules with potential therapeutic applications.
Used in Peptide Synthesis:
In the field of peptide chemistry, 4-(9H-FLUOREN-9-YLMETHOXYCARBONYLAMINO)-PIPERIDINE-1,4-DICARBOXYLIC ACID MONO-TERT-BUTYL ESTER serves as a key component in the preparation of synthetic peptide amides. It is particularly useful for the development of kappa opioid receptor agonists, which are important for the treatment of pain, pruritis, and inflammation associated with a variety of diseases.
Used in the Synthesis of Water-Soluble Peptides:
4-(9H-FLUOREN-9-YLMETHOXYCARBONYLAMINO)-PIPERIDINE-1,4-DICARBOXYLIC ACID MONO-TERT-BUTYL ESTER is also utilized in the synthesis of cyclic α,α-disubstituted amino acids. These amino acids are crucial for the preparation of water-soluble, highly helical peptides, which have potential applications in drug design and delivery due to their unique structural and functional properties.

InChI:InChI=1/C26H30N2O6/c1-25(2,3)34-24(32)28-14-12-26(13-15-28,22(29)30)27-23(31)33-16-21-19-10-6-4-8-17(19)18-9-5-7-11-20(18)21/h4-11,21H,12-16H2,1-3H3,(H,27,31)(H,29,30)/p-1

Upstream product

• 102774-86-7 9-fluorenylmethyl N-succinimidyl carbonate 
• 183673-71-4 4-amino-1-(tert-butoxycarbonyl)piperidine-4-carboxylic acid 
• 24424-99-5 di-tert-butyl dicarbonate 
• 79099-07-3 N-tert-butyloxycarbonylpiperidin-4-one 
• 40064-34-4 piperidine-4,4-diol hydrochloride 
• 13625-39-3 1,3,8-triaza-spiro[4.5]decan-2,4-dione 
• 183673-70-3 tert-butyl 2,4-dioxo-1,3,8-triazaspiro[4.5]decane-8-carboxylate 
• 183673-68-9 1-tert-butyloxycarbonylpiperidine-4-spiro-5'-(1',3'-bis(tertbutyloxy-carbonyl))hydantoin 
• 82911-69-1 N-(9H-fluoren-2-ylmethoxycarbonyloxy)succinimide 
• 28920-43-6 (fluorenylmethoxy)carbonyl chloride 

Downstream Products

• 877273-27-3 C₃₇H₄₁N₃O₇ 
• 406235-17-4 tert-butyl 4-(((9H-fluoren-9-ylmethoxy)carbonyl)amino)-4-(hydroxymethyl)piperidine-1-carboxylate 
• 161529-14-2 (R)-3-(9H-fluoren-9-ylmethyloxycarbonylamino)-4-hydroxybutyric acid tert-butyl ester 
• 1059175-69-7 tert-butyl 4-(((9H-fluoren-9-yl)methoxy)carbonylamino)-4-(3,5-bis(trifluoromethyl)phenylcarbamoyl)piperidine-1-carboxylate 
• 1246024-65-6 Fmoc(BocApi)2OBn 
• 1246024-63-4 Fmoc(BocApi)OBn 

Relevant academic research and scientific papers

INHIBITORS OF MTOR-MEDIATED INDUCTION OF AUTOPHAGY

The invention provides amides that inhibit apoptosis or induce autophagy through mTOR-mediated induction of autophagy, or inhibit a related disease such as cerebral ischemia/reperfusion or neurodegenerative diseases, including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.

Spiro compound

The invention discloses a spiro compound, application thereof and a pharmaceutical composition containing the spiro compound. The structure of the compound is shown as a formula I, and the compound has a good inhibition effect on RET kinase.

MULTIVALENT RAS BINDING COMPOUNDS

The present invention provides, inter alia, compounds that selectively bind a RAS protein at two or more sites and methods for their synthesis. Compositions and kits containing the compounds, as well as methods of using the compounds and compositions for ameliorating or treating the effects of a disease associated with altered RAS signaling, such as a cancer, in a subject and methods for effecting cancer cell death are also provided herein. Methods of identifying a multivalent compound which binds selectively to a target protein also are provided herein.

Exploration of N-(2-aminoethyl)piperidine-4-carboxamide as a potential scaffold for development of VEGFR-2, ERK-2 and Abl-1 multikinase inhibitor

VEGFR, ERK and Abl had been respectively identified as good drug targets, and their crosstalk also had been well elaborated. Multitarget drugs were more advantageous for cancer treatment, however, no inhibitors simultaneously acting on the three proteins were developed due to their structural diversities. Herein, N-(4-((2-(2-(naphthaen-1-yl)acetamido)ethyl)carbamoyl)piperidin-4-yl)-6- (trifluoromethyl)nicotinamide (NEPT, 6a) was discovered as an active scaffold against VEGFR-2, ERK-2 and Abl-1 kinases through the combination of support vector machine, similarity searching and molecular docking. NEPT and its derivatives were synthesized by convenient routine, their in vitro anti-proliferative abilities against human liver cancer cell line HepG2 were preliminarily evaluated. A representative compound 6b showed an IC50 value of 11.3 μM and induced significant HepG2 cells apoptosis. Besides, these compounds displayed better anti-proliferative abilities against K562 cells (a cell line with typical hyperactivity of the above multikinases), for example compound 6b exhibited an IC50 value of 4.5 μM. Based on hepatotoxicity case reports of Abl inhibitors, cytotoxicity of synthetic compounds against normal liver cell lines (QSG7701 and HL7702) was studied, 6b had a similar toxic effect with positive control imatinib, and most compounds showed less than 35% inhibition activities at 100 μM. Molecular docking study disclosed interactions of 6b with VEGFR-2, ERK-2 and Abl-1 kinases, respectively. Our data suggested the biological activities of 6b may derived from collaborative effects of VEGFR-2, ERK-2 and Abl-1 inhibition.

Short amphipathic peptides with activity against bacteria and intracellular pathogens

“Minimalist” antimicrobial peptides are disclosed based on 50 to 80% α,α-dialkylated amino acids. The peptides are short, cationic, amphipathic, and possess a high helix propensity. Polar α,α-dialkylated amino acids are also disclosed. These peptides are easy and inexpensive to synthesize via solid-phase techniques. The peptides exhibit in vitro anti-bacterial properties at concentrations that are not lethal to normal mammalian cells. The peptides exhibit in vivo bioactivity against intracellular pathogens.

Therapeutic and diagnostic ligand systems comprising transport molecule binding properties and medicaments containing the same

The invention relates to transport molecule binding ligand compounds which comprise a therapeutically and/or diagnostically active substance and a carrier molecule-affine substance with a high association constant to the carrier molecule. The invention also relates to medicaments containing these ligand compounds and to diagnostic kits.