67057-68-5

Upstream product

• 17367-31-6 3-trityloxy-1-propanol 
• 79-37-8 oxalyl dichloride 
• 76-83-5 trityl chloride 

Downstream Products

• 128532-51-4 ethyl 5-hydroxy-7-trityloxy-3-oxoheptanoate 
• 262299-53-6 (R)-1-Trityloxy-hex-5-en-3-ol 
• 262299-52-5 (S)-1-Trityloxy-hex-5-en-3-ol 
• 24243-01-4 3-(triphenylmethyloxy)propionic acid 
• 769936-23-4 1-trityloxy-octan-3-one 
• 1447820-21-4 C₃₀H₃₅NO₂ 
• 1447820-16-7 (S)-N,N-diallyl-3-hydroxy-5-(trityloxy)pentanethioamide 

Relevant academic research and scientific papers

Effect of Partially Fluorinated N-Alkyl-Substituted Piperidine-2-carboxamides on Pharmacologically Relevant Properties

The modulation of pharmacologically relevant properties of N-alkyl-piperidine-2-carboxamides was studied by selective introduction of 1–3 fluorine atoms into the n-propyl and n-butyl side chains of the local anesthetics ropivacaine and levobupivacaine. The basicity modulation by nearby fluorine substituents is essentially additive and exhibits an exponential attenuation as a function of topological distance between fluorine and the basic center. The intrinsic lipophilicity of the neutral piperidine derivatives displays the characteristic response noted for partially fluorinated alkyl groups attached to neutral heteroaryl systems. However, basicity decrease by nearby fluorine substituents affects lipophilicities at neutral pH, so that all partially fluorinated derivatives are of similar or higher lipophilicity than their non-fluorinated parents. Aqueous solubilities were found to correlate inversely with lipophilicity with a significant contribution from crystal packing energies, as indicated by variations in melting point temperatures. All fluorinated derivatives were found to be somewhat more readily oxidized in human liver microsomes, the rates of degradation correlating with increasing lipophilicity. Because the piperidine-2-carboxamide core is chiral, pairs with enantiomeric N-alkyl groups are diastereomeric. While little response to such stereoisomerism was observed for basicity or lipophilicity, more pronounced variations were observed for melting point temperatures and oxidative degradation.

Deacetylcolchicine deriv.

Provided are 4-modified colchicine compounds and medicines using the same. Specifically provided are colchicine derivatives represented by general formula (1), salts thereof, and solvates of the same. In general formula (1), R1 is a halogen atom, a hydroxyl group, a nitro group, an amino group, or a mono-, di- or tri-fluoromethyl group; R2, R3 and R4 are each a methoxy group or a hydroxyl group, or alternatively R2 and R3, or R3 and R4 together represent a methylenedioxy group; R5 and R6 may be the same or different and are each a hydrogen atom, a C1-6 alkyl group, an arylalkyl group, a C2-6 alkenyl group, -COR7, -COOR8, -SO2R9, -CONR10R11, or -CSNR12R13, or alternatively R5 and R6 together with the nitrogen atom to which R5 and R6 are bonded may form a three- to seven-membered cyclic amino group; R7 is a C1-6 alkyl group or the like; R8 is a C1-6 alkyl group or the like; R9 is a C1-6 alkyl group or the like; R10 and R11 may be the same or different and are each a hydrogen atom, a C1-6 alkyl group, or the like; and R12 and R13 may be the same or different and are each a hydrogen atom, an alkyl group, or the like.

An inhibitor of glutathione S-transferase omega 1 that selectively targets apoptotic cells

On (cell) suicide watch: The increased permeability of apoptotic cells was used to identify a peptide-based, covalent inhibitor (NJP2) for glutathione S-transferase omega (GSTO1) that is highly selective for apoptotic cells, with no inhibition of healthy

New Antibacterial Agents Derived from the DNA Gyrase Inhibitor Cyclothialidine

Cyclothialidine (1, Ro 09-1437) is a potent DNA gyrase inhibitor that was isolated from Streptomyces filipinensis NR0484 and is a member of a new family of natural products. It acts by competitively inhibiting the ATPase activity exerted by the B subunit of DNA gyrase but barely exhibits any growth inhibitory activity against intact bacterial cells, presumably due to insufficient permeation of the cytoplasmic membrane. To explore the antibacterial potential of 1, we developed a flexible synthetic route allowing for the systematic modification of its structure. From a first set of analogues, structure-activity relationships (SAR) were established for different substitution patterns, and the 14-hydroxylated, bicyclic core (X) of 1 seemed to be the structural prerequisite for DNA gyrase inhibitory activity. The variation of the lactone ring size, however, revealed that activity can be found among 11- to 16-membered lactones, and even seco-analogues were shown to maintain some enzyme inhibitory properties, thereby reducing the minimal structural requirements to a rather simple, hydroxylated benzyl sulfide (XI). On the basis of these "minimal structures" a modification program afforded a number of inhibitors that showed in vitro activity against Gram-positive bacteria. The best activities were displayed by 14-membered lactones, and representatives of this subclass exhibit excellent and broad in vitro antibacterial activity against Gram-positive pathogens, including Staphylococcus aureus, Streptococcus pyogenes, and Enterococcus faecalis, and overcome resistance against clinically used drugs. By improving the pharmacokinetic properties of the most active compounds (94, 97), in particular by lowering their lipophilic properties, we were able to identify congeners of cyclothialidine (1) that showed efficacy in vivo.

Total synthesis of macquarimicins using an intramolecular Diels-Alder approach inspired by a biosynthetic pathway

A total synthesis of the macquarimicins A-C (1-3), novel natural products with intriguing tetra- or pentacyclic frameworks, has been achieved. The synthesis features an extensive investigation of the biosynthesis-based intramolecular Diels-Alder (IMDA) re

Oxidative deprotection of 1,3-dithiane group using NaClO2 and NaH2PO4 in aqueous methanol

The 1,3-dithiane group was oxidatively deprotected under the conditions of sodium chlorite, sodium dihydrogenphosphate, and 2-methyl-2-butene in 3:1 methanol-water at room temperature in good yield.

Sulfenamide-catalyzed oxidation of primary and secondary alcohols with molecular bromine

Primary and secondary alcohols were smoothly oxidized to the corresponding aldehydes and ketones in high yields at room temperature with 1.1 equiv. of molecular bromine by using a catalytic amount of N-t-butyl-2-nitrobenzenesulfenamide in the coexistence of potassium carbonate and molecular sieves 4A.

Synthesis and reactivity of mevinolin-like lactone precursors

The synthesis of mevinolin-like lactone precursors and the evaluation of their ability in the N-alkylation of N-potassium-phthalimide are reported.

DNA gyrase inhibitors and pharmaceutical preparations therefor

Bicyclic derivatives of the formula STR1 wherein X1, X2, R1, R2, R3, R4, R5, R6, R7a, R7b, and R8 are as defined in the specification. These compounds are antimicrobially active.

Synthesis of Novel 2-Oxo-4-thia-1-azabicyclooct-7-ene-8-carboxylic Acid Derivatives

The bicyclic thiazolidinone-carbapenem analogues, 18, 19 and 37 have been prepared from thioglycolamide 5 and 3-triphenylmethoxypropionaldehyde 7, via 2-(2-triphenylmethoxyethyl)thiazolidin-4-one 8.Elaboration of the thiazolidin-4-one 8 to the phosphorane