Biomedical subjects

Mark Ladlow

Publications and source records attributed to Mark Ladlow.

23 records · Page 2Linked to original sources

PubMedDate not supplied

Which sites react first? Functional site distribution and kinetics on solid supports investigated using confocal Raman and fluorescence microscopy.

Fluorescence microscopy is a powerful technique for analyzing beads with very low loadings of fluorophores; however, the method is flawed when looking at more highly loaded beads as a result of severe problems with absorption. To probe distributions at higher loading levels, Raman spectroscopy avoids many of these issues. These studies show that there is a uniform distribution of reactive sites throughout the beads but that the spatial distribution of reacted sites depends on the polymer type, with a fine balance between reaction and diffusion rate.

Binding Sites↗

PubMedDate not supplied

A highly automated, polymer-assisted strategy for the preparation of 2-alkylthiobenzimidazoles and N,N'-dialkylbenzimidazolin-2-ones.

A multistep, polymer-assisted solution phase strategy for the highly automated (auto-PASP) synthesis of 2-alkylthiobenzimidazole and N,N'-dialkylbenzimidazolin-2-one libraries is presented. The approach incorporates in-line purification techniques to afford library products directly with high purities and is exemplified by the preparation of a 96-member 2-alkylthiobenzimidazoline library 1[1-12,1-8] and a 72-member N,N'-dialkylbenzimidazolin-2-one library 9[1-12,1-6].

Journal Article↗

PubMedDate not supplied

A fluorous-tagged, acid-labile protecting group for the synthesis of carboxamides and sulfonamides.

A new acid-labile, fluorous-tagged protecting group that facilitates the preparation of carboxamides and sulfonamides by parallel solution-phase synthesis is introduced. Its use is exemplified by the preparation of a 27-member library of biaryl sulfonamides and an 18-member library of biaryl carboxamides. Intermediates were purified by solid-phase extraction over reversed-phase fluorous silica gel to afford library members in high yields and purities (>95%) without the need for column chromatographic purification.

Journal Article↗

PubMedDate not supplied

Automated flow-through synthesis of heterocyclic thioethers.

The fully automated, sequential flow-through synthesis of a 44-member array of thioethers 10[1-4,1-11] employing a resin "capture and release" reactor column is described. The array incorporates four different heterocyclic scaffolds, and the synthesis was performed using a custom-built robotic synthesizer that is able to (i) load and regenerate the reactor column and (ii) array each product into a single vial using UV threshold detection. All the compounds were obtained in high yield (>75%) and excellent purity (>95%) without the need for further purification.

Journal Article↗

PubMedDate not supplied

Fully automated polymer-assisted synthesis of 1,5-biaryl pyrazoles.

The polymer-assisted solution-phase (PASP) synthesis of a 192-member 2-D array of 1,5-biaryl pyrazoles 4[1-12,1-16] is reported. The synthesis was performed in a fully automated manner using a multiprobe top-filtration robot and incorporates a "catch and release" step to afford library compounds directly in high yield and purity.

Catalysis↗