50563-72-9

Upstream product

• 111-45-5 ethylene glycol monoallyl ether 
• 98-59-9 p-toluenesulfonyl chloride 

Downstream Products

• 188636-73-9 (2S,4aR,6R,7R,8S,8aS)-7-(2-Allyloxy-ethoxy)-8-benzyloxy-2-phenyl-6-[(1R,2R)-2-((2S,3S,4R,5R,6S)-3,4,5-tris-benzyloxy-6-methyl-tetrahydro-pyran-2-yloxy)-cyclohexyloxy]-hexahydro-pyrano[3,2-d][1,3]dioxine 
• 1071218-57-9 4-Bromo-1-(3-oxa-5-hexenyloxy)benzene 
• 309947-38-4 1-Bromo-2-methyl-4-(3-oxahex-5-enyloxy)benzene 
• 876396-28-0 C₂₆H₃₂N₂O₆ 
• 876396-36-0 2-(2-allyloxyethoxy)acetanilide 
• 876396-21-3 methyl 2-(2-allyloxyethoxy)benzoate 
• 920978-37-6 C₂₈H₃₈O₈ 
• 111915-32-3 4-[2-(allyloxy)ethoxy]phenol 
• 89760-71-4 9-<2-(2,3-dihydroxy-propyloxy)ethyl>adenine 
• 1262899-05-7 N₁,N₃-bis(2-(4-(2-(allyloxy)ethoxy)phenoxy)ethyl)-5-ferrocenylisophthalamide 
• 1537217-83-6 1-[(6-triethoxysilyl-3-oxahexyl)]-4-phenyl-1H-1,2,3-triazole 
• 1537217-85-8 1-[(6-triethoxysilyl-3-oxahexyl)]-4-(methyldiphenylphosphine-borane)-1H-1,2,3-triazole 

Relevant academic research and scientific papers

Imidazolium-based catenane host for bromide recognition in aqueous media

The synthesis of a novel catenated system which is dense in cationic hydrogen bonding imidazolium units is described. The interlocked host system displays a preference for binding of bromide over other halides, overcoming basicity and Hofmeister trends, u

SYNTHESIS OF URACIL AND URACIL

A synthesis is reported for N1-mono- and N1,N3-disubstituted uracil derivatives containing a terminal carbon-carbon double bond in the side-chain. Alkylation of vinyl 2-chloroethyl ether by uracil potassium salts leads to

Structure-Based Design of High-Affinity Macrocyclic FKBP51 Inhibitors

The FK506-binding protein 51 (FKBP51) emerged as a key player in several diseases like stress-related disorders, chronic pain, and obesity. Linear analogues of FK506 called SAFit were shown to be highly selective for FKBP51 over its closest homologue FKBP52, allowing the proof-of-concept studies in animal models. Here, we designed and synthesized the first macrocyclic FKBP51-selective ligands to stabilize the active conformation. All macrocycles retained full FKBP51 affinity and selectivity over FKBP52 and the incorporation of polar functionalities further enhanced affinity. Six high-resolution crystal structures of macrocyclic inhibitors in complex with FKBP51 confirmed the desired selectivity-enabling binding mode. Our results show that macrocyclization is a viable strategy to target the shallow FKBP51 binding site selectively.

Macrocyclic FKBP51 Ligands Define a Transient Binding Mode with Enhanced Selectivity

Subtype selectivity represents a challenge in many drug discovery campaigns. A typical example is the FK506 binding protein 51 (FKBP51), which has emerged as an attractive drug target. The most advanced FKBP51 ligands of the SAFit class are highly selective vs. FKBP52 but poorly discriminate against the homologs and off-targets FKBP12 and FKBP12.6. During a macrocyclization pilot study, we observed that many of these macrocyclic analogs have unanticipated and unprecedented preference for FKBP51 over FKBP12 and FKBP12.6. Structural studies revealed that these macrocycles bind with a new binding mode featuring a transient conformation, which is disfavored for the small FKBPs. Using a conformation-sensitive assay we show that this binding mode occurs in solution and is characteristic for this new class of compounds. The discovered macrocycles are non-immunosuppressive, engage FKBP51 in cells, and block the cellular effect of FKBP51 on IKKα. Our findings provide a new chemical scaffold for improved FKBP51 ligands and the structural basis for enhanced selectivity.

Discotic liquid crystal epoxy resin monomer and preparation method thereof, and intrinsic high-thermal-conductivity liquid crystal epoxy resin material and preparation method thereof

The invention belongs to the technical field of epoxy resin materials, and provides a discotic liquid crystal epoxy resin monomer and a preparation method thereof, and an intrinsic high-thermal-conductivity liquid crystal epoxy resin material and a prepar

Novel unit B cryptophycin analogues as payloads for targeted therapy

Cryptophycins are naturally occurring cytotoxins with great potential for chemotherapy. Since targeted therapy provides new perspectives for treatment of cancer, new potent analogues of cytotoxic agents containing functional groups for conjugation to homing devices are required. We describe the design, synthesis and biological evaluation of three new unit B cryptophycin analogues. The O-methyl group of the unit B D-tyrosine analogue was replaced by an O-(allyloxyethyl) moiety, an O-(hydroxyethyl) group, or an O-(((azidoethoxy)ethoxy)ethoyxethyl) substituent. While the former two maintain cytotoxicity in the subnanomolar range, the attachment of the triethylene glycol spacer with a terminal azide results in a complete loss of activity. Docking studies of the novel cryptophycin analogues to β-tubulin provided a rationale for the observed cytotoxicities.

NOVEL TRIAZINE COMPOUND, ALL-SOLID-STATE POLYMER ELECTROLYTE COMPOSITION AND USE THEREOF

The present invention relates to a novel triazine compound represented by chemical formula 1, an all-solid-state polymer electrolyte composition comprising the same as a cross-linking agent and uses thereof. More specifically, the triazine compound effectively inhibits crystallization of a plasticizer at a low temperature (room temperature) to show significantly improved ion conductivity, and can realize significantly improved electrochemical stability and excellent battery properties, thereby being usefully used as an all-solid-state polymer electrolyte composition such as a lithium-polymer secondary battery, a dye-sensitized solar cell, etc.COPYRIGHT KIPO 2018

Synthesis and determination of physicochemical properties of new 3-(4-arylpiperazin-1-yl)-2-hydroxypropyl 4-alkoxyethoxybenzoates

Nine new dihydrochloride salts of 3-(4-arylpiperazin-1-yl)-2-hydroxypropyl 4-alkoxyethoxybenzoates were designed and synthesized. The physicochemical properties such as lipophilicity index (log kw) and dissociation constant (pKa) wer

Synthesis of oxacyclic scaffolds via dual ruthenium hydride/Bronsted acid-catalyzed isomerization/cyclization of allylic ethers

A ruthenium hydride/Bronsted acid-catalyzed tandem sequence is reported for the synthesis of 1,3,4,9-tetrahydropyrano[3,4-b]indoles (THPIs) and related oxacyclic scaffolds. The process was designed on the premise that readily available allylic ethers would undergo sequential isomerization, first to enol ethers (Ru catalysis), then to oxocarbenium ions (Bronsted acid catalysis) amenable to endo cyclization with tethered nucleophiles. This methodology provides not only an attractive alternative to the traditional oxa-Pictet-Spengler reaction for the synthesis of THPIs, but also convenient access to THPI congeners and other important oxacycles such as acetals.

Catenanes built around octahedral transition-metal complexes that contain two intertwined endocyclic but non-sterically hindering tridentate ligands

Sterically hindering bidentate chelates, such as 2,9-diphenyl-1,10- phenanthroline, form entwined complexes with copper(I) and other tetrahedrally coordinated transition-metal centres. To prepare octahedral complexes containing two entwined tridentate lig