99837-97-5

Upstream product

• 505-95-3 12-hydroxydodecanoic acid 
• 100-39-0 benzyl bromide 
• 947-05-7 oxacyclotridecan-2-one 
• 100-51-6 benzyl alcohol 

Downstream Products

• 152754-51-3 12-(benzyloxy)-12-oxo-1-dodecyl (2S)-1-(4-((benzyloxy)methoxy)-3,3-dimethyl-1,2-dioxobutyl)-2-piperidinecarboxylate 
• 341925-14-2 12-oxo-dodecanoic acid benzyl ester 
• 341925-17-5 13-methylcarbamoyl-tridec-12-enoic acid benzyl ester 
• 341925-15-3 tetradec-2-enedioic acid 14-benzyl ester 1-tert-butyl ester 
• 341925-16-4 tetradec-2-enedioic acid 14-benzyl ester 

Relevant academic research and scientific papers

The reaction mechanism for the organocatalytic ring-opening polymerization of L-lactide using a guanidine-based catalyst: Hydrogen-bonded or covalently bound?

We have investigated two alternative mechanisms for the ring-opening polymerization of L-lactide using a guanidine-based catalyst, the first involving acetyl transfer to the catalyst, and the second involving only hydrogen bonding to the catalyst. Using computational chemistry methods, we show that the hydrogen bonding pathway is considerably preferred over the acetyl transfer pathway and that this is consistent with experimental information.

OLIGONUCLEOTIDES CONTAINING NUCLEOTIDE ANALOGS

The present disclosure relates to double-stranded oligonucleotides, including double-stranded oligonucleotides such as siRNAs, comprising a sense strand oligonucleotide and an antisense strand oligonucleotide, and wherein the antisense strand oligonucleotide comprises one or more nucleotide analogs of formula (I-A) which are neither the 5'-overhang nucleotide nor the 3'-overhang nucleotide of the said antisense strand oligonucleotide, and wherein a nucleotide analog of formula (I-A) is as described in the disclosure. Oligonucleotides containing these analogs have superior biological activity, for example, increased in vitro stability and improved in vivo potency especially improved off-target profiles. The improved oligonucleotides are useful for silencing (e.g., reducing or eradicating) the expression of a target gene.

NUCLEOTIDE PRECURSORS, NUCLEOTIDE ANALOGS AND OLIGOMERIC COMPOUNDS CONTAINING THE SAME

The present disclosure relates to novel nucleotide precursors and nucleotide analogs that can be incorporated into oligonucleotides, including double-stranded oligonucleotides such as siRNAs. Oligonucleotides containing these analogs have superior biological activity, for example, increased in vitro stability and improved in vivo potency especially duration of action. The improved oligonucleotides are useful for silencing (e.g., reducing or eradicating) the expression of a target gene. In particular embodiments, this invention encompasses specific nucleotide analogs to be included in double-stranded RNAs (dsRNAs), and especially in siRNAs, that can hybridize to messenger RNAs (mRNAs) of interest, so as to reduce or block the expression of target genes of interest. The present compounds have general formula (I), wherein each of Ra, Rb, Rc and Rd is independently, H or a (C1-C6) alkyl group and B is a heterocyclic nucleobase.

A Convenient Protocol for the Esterification of Carboxylic Acids with Alcohols in the Presence of di-t-Butyl Dicarbonate

Stoichiometric mixtures of carboxylic acids and primary or secondary alkyl alcohols are cleanly converted into their corresponding esters by treatment with di-t-butyl dicarbonate [(BOC)2O] in the presence of catalytic amounts of N,N′-dimethylaminopyridine (DMAP). This convenient procedure provides a general access to a broad variety of esters including those bearing highly sensitive functional groups such as phenol esters or BOC-groups. Purification of the products is particularly easy since the byproducts t-BuOH and CO2 are volatile - a great advantage over the standard DCC/DMAP method.

Conjugates and compositions for cellular delivery

This invention features conjugates, degradable linkers, compositions, methods of synthesis, and applications thereof, including cholesterol, folate, galactose, galactosamine, N-acetyl galactosamine, PEG, phospholipid, peptide and human serum albumin (HSA) derived conjugates of biologically active compounds, including antibodies, antivirals, chemotherapeutics, peptides, proteins, hormones, nucleosides, nucleotides, non-nucleosides, and nucleic acids including enzymatic nucleic acids, DNAzymes, allozymes, antisense, dsRNA, siNA, siRNA, triplex oligonucleotides, 2,5-A chimeras, decoys and aptamers.

Nanowells on silica particles in water containing long-distance porphyrin heterodimers

Smooth and nonswelling spherical silica particles with a diameter of 100 nm and an aminopropyl coating are soluble in water at pH 11, coagulate quickly at pH 3, and redissolve at pH 9. Electron microscopy as well as visible spectra of covalently attached porphyrins indicate the aggregation state of the particles. Long-chain α,ω-dicarboxylic acids with a terminal oligoethyleneglycol (=OEG)-amide group were attached in a second self-assembly step to the remaining amine groups around the porphyrins. Form-stable 2-nm wells were thus obtained and were characterized by fluorescence quenching experiments using the bottom porphyrin as a target. The one-dimensional diffusion of fitting quencher molecules along the 2-nm pathway took several minutes. Porphyrins with a diameter above 2 nm could not enter the form-stable gaps at all. Added tyrosine stuck irreversibly to the walls of the nanowells and prevented the entrance of quencher molecules, the OEG-headgroups fixated 2,6-diaminoanthraquinone. A ring of methylammonium groups was then fixed at the walls of the wells at a distance of 5 or 10 A with respect to the bottom porphyrin. 2,6-Disulfonatoanthraquinone was attached only loosely to this ring, but the exactly fitting manganese(III) meso-(tetraphenyl-4-sulfonato)porphyrinate (Mn(III) TPPS) was tightly bound. Transient fluorescence experiments showed a fast decay time of 0.2 ns for the bottom porphyrin, when the Mn(III) TPPS was fixated at a distance of 5 A. Two different dyes have thus been immobilized at a defined subnanometer distance in an aqueous medium.

Methylammonium groups at the solid walls of nanometer-sized, water-filled monolayer gaps as binding sites for a tetraanionic porphyrin

Long-chain hydrosulfides containing two secondary amide functions and either electron-poor or electron-rich carbon - carbon double bonds were self-assembled on gold surfaces around a flat-lying, octaanionic porphyrin. Rigid and reactive surface monolayers

Design, synthesis, and kinetic evaluation of high-affinity FKBP ligands and the X-ray crystal structures of their complexes with FKBP 12

The design and synthesis of high-affinity FKBP12 ligands is described. These compounds potently inhibit the cis-trans-peptidylprolyl isomerase (rotamase) activity catalyzed by FKBP12 with inhibition constants (Ki,app) as low as 1 nM, yet they possess remarkable structural simplicity relative to FK506 and rapamycin, from which they are conceptually derived. The atomic structures of three FKBP12-ligand complexes and of one unbound ligand were determined by X-ray crystallography and are compared to the FKBP12-FK506 and FKBP12-rapamycin complexes.