17367-31-6

Upstream product

• 76-83-5 trityl chloride 
• 504-63-2 trimethyleneglycol 
• 596-43-0 bromo-triphenyl-methane 

Downstream Products

• 67057-68-5 3-(triphenylmethyloxy)propionaldehyde 
• 218461-39-3 trifluoro-methanesulfonic acid 3-trityloxy-propyl ester 
• 141855-78-9 2-(2-Triphenylmethoxyethyl)thiazolidin-4-one 
• 141855-80-3 Chloro-[4-oxo-2-(2-trityloxy-ethyl)-thiazolidin-3-yl]-acetic acid 4-nitro-benzyl ester 
• 141855-79-0 Hydroxy-[4-oxo-2-(2-trityloxy-ethyl)-thiazolidin-3-yl]-acetic acid 4-nitro-benzyl ester 
• 141855-81-4 p-Nitrobenzyl <4-oxo-2-(2-triphenylmethoxyethyl)thiazolidin-3-yl>triphenylphosphoranylideneacetate 
• 213738-49-9 C₄₀H₅₄O₃ 
• 1421957-05-2 3-(trityloxy)propyl 3-nitrobenzoate 
• 128532-51-4 ethyl 5-hydroxy-7-trityloxy-3-oxoheptanoate 
• 218461-33-7 1-(3-trityloxy-propyl)-4-vinyloxy-azetidin-2-one 
• 218461-43-9 formic acid 4-oxo-1-(3-trityloxy-propyl)-azetidin-2-yl ester 
• 676347-46-9 3,5-bis-(tert-butyl-dimethyl-silanyloxy)-2-[2-methoxycarbonyl-2-(3-trityloxy-propionylamino)-ethylsulfanylmethyl]-6-methyl-benzoic acid 4-nitro-benzyl ester 

Relevant academic research and scientific papers

Stereoselective synthesis of tri- and tetrasubstituted α,β-unsaturated esters via copper-catalyzed coupling of enol triflates of β-ketoesters with Grignard-based zinc ate complexes

Tri- and tetrasubstituted α,β-unsaturated esters were stereoselectively prepared via the copper-catalyzed couplings of the enol triflates of β-ketoesters with Grignard-based zinc ate complexes. Some insights into the mechanistic considerations are describ

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.

A large ring sulfate and its preparation method and application

The invention relates to novel macrocyclic cyclic sulfate, and a preparation method and application thereof. The novel macrocyclic cyclic sulfate comprises macrocyclic cyclic sulfite and macrocyclic cyclic sulfate, wherein the structures of the macrocyclic cyclic sulfite and the macrocyclic cyclic sulfate are shown in a formula I and a formula II respectively; X and Y are respectively or jointly alkane, olefin, oxo-alkane, thio-alkane or aza-alkane and the like, with the total atom number being more than 4, on a ring-forming shortest chain. The macrocyclic cyclic sulfite is obtained by cyclizing a long-chain glycol compound by using thionyl chloride under the action of alkali; the macrocyclic cyclic sulfate is obtained through oxidation under metal catalysis; various derivatives of the long-chain glycol can be obtained through ring-opening reaction. The macrocyclic cyclic sulfate provided by the invention has a novel structure, can serve as an important organic synthesis intermediate, are abundant in raw material source, low in cost, mild in preparation condition, high in yield and easy to operate, can simplify the synthesis route of a large amount of chemical raw materials and medical intermediates, and has an important application prospect.

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.

Highly efficient synthesis of monodisperse poly(ethylene glycols) and derivatives through macrocyclization of oligo(ethylene glycols)

A macrocyclic sulfate (MCS)-based approach to monodisperse poly(ethylene glycols) (M-PEGs) and their monofunctionalized derivatives has been developed. Macrocyclization of oligo(ethylene glycols) (OEGs) provides MCS (up to a 62-membered macrocycle) as versatile precursors for a range of monofunctionalized M-PEGs. Through iterative nucleophilic ring-opening reactions of MCS without performing group protection and activation, a series of M-PEGs, including the unprecedented 64-mer (2850Da), can be readily prepared. Synthetic simplicity coupled with versatility of this new strategy may pave the way for broader applications of M-PEGs. Macrocycles make synthesis easier: Convenient macrocyclization of the OEGs provides versatile macrocyclic sulfates. These compounds are cornerstones for both monofunctionalization of OEGs and highly efficient synthesis of monodisperse PEGs and derivatives, including an unprecedented 64-mer.

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

MELANIN PRODUCTION INHIBITOR

Disclosed is a melanin production inhibitor which has an excellent inhibitory activity on the production of melanin and is highly safe. The melanin production inhibitor comprises a compound represented by general formula (1) (excluding clotrimazole), and/or a pharmacologically acceptable salt thereof. In the formula, A1, A2 and A3 are independently selected from a hydrogen atom, an aryl group which may have a substituent, and an aromatic heterocyclic group which may have a substituent, wherein at least one of A1, A2 and A3 is selected from the aryl group and the aromatic heterocyclic group, the total number of carbon atoms contained in A1, A2 and A3 is 6 to 50 and, when at least two of A1, A2 and A3 represent the aryl groups or the aromatic heterocyclic groups, the adjacent two aryl or aromatic heterocyclic groups may be bound to each other via an alkyl chain or an alkenyl chain to form a ring; m represents an integer of 0 to 2; X represents a hetero atom, a hydrogen atom, or a carbon atom; R1 and R2 are independently selected from a hydrogen atom and an oxo group, wherein when one of R1 and R2 is an oxo group, the other is not present; and R3 is selected from a hydrogen atom, and a C1-8 hydrocarbon group in which one or some of hydrogen atoms or carbon atoms may be substituted by a hetero atom or hetero atoms, wherein the number of R3's present in the compound corresponds to the number of X's and, when two or more R3's are present, the R3's are independently present and the adjacent two R3's may be bound to each other to form, together with X, a ring, and the terminal of R3 may be bound to a carbon atom to which A1, A2 and A3 are bound, thereby forming a ring.

N1-substituted thymine derivatives as mitochondrial thymidine kinase (TK-2) inhibitors

Novel N1-substituted thymine derivatives related to 1-[(Z)-4-(triphenylmethoxy)-2-butenyl]thymine have been synthesized and evaluated against thymidine kinase-2 (TK-2) and related nucleoside kinases [i.e., Drosophila melanogaster deoxynucleosid

Compositions containing lysophosphatidic acids which inhibit apoptosis and uses thereof

The invention provides anti-apoptotic compositions lysophosphatidic acids and methods for making and using the compositions. Such compositions can also contain LPA potentiating agents, including proteins, lipid membrane structures and polymers such as polyethylene glycols. The compositions can additionally contain other pharmaceutically effective agents such as drugs, antibiotics, wound healing agents and antioxidants.

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.