141177-22-2

Upstream product

• 4541-15-5 5-(benzyloxy)-1-pentanol 
• 98-59-9 p-toluenesulfonyl chloride 
• 111-29-5 1 ,5-pentanediol 
• 100-39-0 benzyl bromide 

Downstream Products

• 1014-93-3 1-(benzyloxy)-5-bromopentane 
• 77154-72-4 C₅₁H₇₀N₂O₁₀S₄ 
• 284666-35-9 N-(5-benzyloxypentyl)-N-(tert-butoxycarbonyl)-O-benzylhydroxylamine 
• 84885-76-7 (((5-iodopentyl)oxy)methyl)benzene 
• 929619-00-1 5-(adamantan-1-yl-methoxy)-1-benzyloxy-pentane 
• 956470-70-5 hexadec-15-enyloxymethyl-benzene 
• 202577-32-0 5-(adamantan-1-yl-methoxy)-1-pentanal 
• 216758-20-2 AMP-DNM 
• 929619-05-6 2,3,4-tri-O-benzyl-6-O-[1-(adamantan-1-yl-methoxy)-pentyl]-1-deoxynojirimycin 
• 929619-18-1 allyl 2,4,6-tri-O-benzyl-3-O-[5-(adamantan-1-yl-methoxy)-pentyl]-D-glucopyranoside 
• 857254-45-6 2,3,4,6-tetra-O-benzyl-N-[5-(adamantan-1-yl-methoxy)-pentyl]-1-deoxynojirimycin 
• 929619-06-7 2,3,4-tri-O-benzyl-N-butyl-6-O-[1-(adamantan-1-yl-methoxy)-pentyl]-1-deoxynojirimycin 
• 929619-04-5 2,3,4-tri-O-benzyl-N-pent-4'-enoyl-6-O-[1-(adamantan-1-yl-methoxy)-pentyl]-1-deoxynojirimycin 
• 850888-02-7 3,4,6-tri-O-benzyl-N-benzyloxycarbonyl-2-O-[5-(adamantan-1-yl-methoxy)-pentyl]-1-deoxynojirimycin 

Relevant academic research and scientific papers

Systematic Investigation of the Permeability of Androgen Receptor PROTACs

Bifunctional molecules known as PROTACs simultaneously bind an E3 ligase and a protein of interest to direct ubiquitination and clearance of that protein, and they have emerged in the past decade as an exciting new paradigm in drug discovery. In order to investigate the permeability and properties of these large molecules, we synthesized two panels of PROTAC molecules, constructed from a range of protein-target ligands, linkers, and E3 ligase ligands. The androgen receptor, which is a well-studied protein in the PROTAC field was used as a model system. The physicochemical properties and permeability of PROTACs are discussed.

Compounds and Their Use in Treating Cancer

The specification generally relates to compounds of Formula (I): and pharmaceutically acceptable salts and prodrugs thereof, where R1, R4, R5, R6, R7, Linker, X, Y, A, G, D and E have any of the meanings defined herein. This specification also relates to the use of such compounds and pharmaceutically acceptable salts and prodrugs thereof in methods of treatment of the human or animal body, for example in prevention or treatment of cancer. This specification also relates to processes and intermediate compounds involved in the preparation of such compounds and to pharmaceutical compositions containing them.

SMALL MOLECULES

Compounds having the general structure A - L - B are presented wherein A and B are independently an E3 ubiquitin ligase protein binding ligand compound of formula 1A or 1 B. Pharmaceutical compositions comprising these compounds and methods of use are also presented.

TAU-PROTEIN TARGETING PROTACS AND ASSOCIATED METHODS OF USE

The present disclosure relates to bifunctional compounds, which find utility as modulators of tau protein. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a VHL or cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds tau protein, such that tau protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of tau. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of tau protein. Diseases or disorders that result from aggregation or accumulation of tau protein are treated or prevented with compounds and compositions of the present disclosure.

Catalytic nucleophilic fluorination by an imidazolium ionic liquid possessing trialkylphosphine oxide functionality

Abstract The synthesis of a new alkylmethylimidazolium ionic liquid wherein the alkyl group is functionalized with dihexylphosphine oxide moiety at the terminal position has been achieved in four steps from 1-methylimidazole. This hybrid ionic liquid effectively catalyzed the nucleophilic fluorination of primary alkyl mesylates under mild conditions using CsF as the fluoride source with a faster rate compared to butylmethylimidazolium mesylate. The hybrid catalyst was recycled 5 times without compromising the yield and purity of the product. The nucleophilic fluorination has been used for the synthesis of diethyl 2-(5-fluoropentyl)-2-methyl malonate, a precursor of 18F isotopomer of an apoptosis imaging agent and the protected form of O-(2'-fluoroethyl)-l-tyrosine, a 18F isotopomer of a tumor imaging agent.

Towards the development of new subtype-specific muscarinic receptor radiopharmaceuticals - Radiosynthesis and ex vivo biodistribution of [ 18F]3-(4-(2-(2-(2-fluoroethoxy)ethoxy)ethylthio)-1,2, 5-thiadiazol-3-yl)-1-methyl-1,2,5,6-tetrahydropyrid

Muscarinic receptors have been implicated in neurological disorders including Alzheimer's disease, Parkinson's disease, and schizophrenia. Nineteen derivatives of thiadiazolyltetrahydropyridine (TZTP), a core that has previously shown high affinities towa

NON-AMPHIPHILE-BASED WATER-IN-WATER EMULSION AND USES THEREOF

The present invention relates to a non-amphiphile-based water-in-water emulsion composition. The non-amphiphile-based water-in-water emulsion composition includes a water-soluble polymer, a non-amphiphilic lyotropic mesogen encapsulated by the water-solub

METABOLICALLY STABLE ALKOXYALKYL ESTERS OF ANTIVIRAL OR ANTIPROLIFERATIVE PHOSPHONATES, NUCLEOSIDE PHOSPHONATES AND NUCLEOSIDE PHOSPHATES

The present invention relates to phosphonate, nucleoside phosphonate or nucleoside phosphate compounds, compositions containing them, processes for obtaining them, and their use in treating a variety of medical disorders, in particular viral infections, cancers and the like.

Nitrone dipolar cycloaddition routes to piperidines and indolizidines. Part 9. Formal synthesis of (-)-pinidine and total synthesis of (-)-histrionicotoxin, (+)-histrionicotoxin and (-)-histrionicotoxin 235A

An intramolecular hydroxylamine-alkyne cyclisation is used for the enantioselective synthesis of the cyclic nitrones 36 and 44. We have demonstrated the use of a novel nitrone protection strategy by cycloaddition of styrene to the cyclic nitrone 44 in the synthesis of the spirocyclic core of the histrionicotoxin family of alkaloids. Deprotection by dipolar cycloreversion of the styrene adduct (the bicyclic isoxazolidine 39) and in situ intramolecular dipolar cycloaddition of a pendant (Z)-α,β-unsaturated nitrile to the intermediate nitrone 50 gave the isoxazolidine 51 in high yield with a surprising degree of regioselectivity compared with the corresponding (Z)-enyne 36. The method is amenable to the synthesis of both enantiomers 51 and 62 of the tricyclic core structure which can be converted by way of the common intermediates (e.g. 53 and ent-53) respectively into the natural configuration of alkaloids (-)-histrionicotoxin 1 and (-)-histrionicotoxin 235A 65 as well as the unnatural (+)-histrionicotoxin 63.

Silver(I) oxide-mediated facile and practical sulfonylation of alcohols

Primary and secondary alcohols were efficiently sulfonylated in the presence of silver(I) oxide and potassium iodide in dichloromethane. The sulfonylation occurs under mild, neutral reaction conditions. The ease of isolation of the final product presents a marked advantage over the known methodologies.