C07D207/46

METHOD FOR PRODUCING HYDROPHOBIC PEPTIDE

A method for producing a purified peptide from a supported crude peptide having a support and a first peptide chain bonded to the support at the C-terminus. The method includes: introducing a linker and a hydrophilic unit to an amino group of the first peptide chain of the supported crude peptide; cleaving a bond between the first peptide chain and the support before or after at least one of the linker and the hydrophilic unit is introduced to the amino group of the first peptide chain such that a support-free hydrophilized peptide is obtained; treating the support-free hydrophilized peptide by liquid chromatography; and cleaving a bond between the linker and the first peptide chain in the support-free hydrophilized peptide by chemical treatment after the liquid chromatography treatment such that a peptide including the first peptide chain is obtained.

Fluorohydroxyproline derivatives useful in the preparation of proteolysis targeted chimeras
11234988 · 2022-02-01 · ·

There is provided novel small molecule E3 ubiquitin ligase protein binding ligand compounds, and to their utility in PROteolysis Targeted Chimeras (PROTACs), as well as processes for their preparation thereof, and use in medicine. There is particularly provided novel small molecule E3 ubiquitin ligase protein binding inhibitor compounds based on a fluorohydroxyproline scaffold, to their utility as ligands in synthesizing novel PROTACs, and to synthetic methods therefor.

Fluorohydroxyproline derivatives useful in the preparation of proteolysis targeted chimeras
11234988 · 2022-02-01 · ·

There is provided novel small molecule E3 ubiquitin ligase protein binding ligand compounds, and to their utility in PROteolysis Targeted Chimeras (PROTACs), as well as processes for their preparation thereof, and use in medicine. There is particularly provided novel small molecule E3 ubiquitin ligase protein binding inhibitor compounds based on a fluorohydroxyproline scaffold, to their utility as ligands in synthesizing novel PROTACs, and to synthetic methods therefor.

Rapid fluorescence tagging of glycans and other biomolecules with enhanced MS signals

Mass spectrometry (MS) active, fluorescent rapid tagging reagent is provided having three substituent groups: (a) a tertiary amino group or other MS active atom; (b) a highly fluorescent moiety; and (c) a reactive group that can react with an amine. The reactive group provides rapid tagging of desired bio-molecules. The fluorescent moiety provides the fluorescent signal. The tertiary amino group provides the MS signal.

Rapid fluorescence tagging of glycans and other biomolecules with enhanced MS signals

Mass spectrometry (MS) active, fluorescent rapid tagging reagent is provided having three substituent groups: (a) a tertiary amino group or other MS active atom; (b) a highly fluorescent moiety; and (c) a reactive group that can react with an amine. The reactive group provides rapid tagging of desired bio-molecules. The fluorescent moiety provides the fluorescent signal. The tertiary amino group provides the MS signal.

Chemical film on substrate, method of forming the same, and method of forming N-hydroxysuccinimide ester-functionalized paracyclophane

The present invention provides a method of forming N-hydroxysuccinimide ester-functionalized paracyclophane. The present method is carried out by adding 4-carboxyl-paracyclophane into N,N′-Dicyclohexylcarbodiimide (DCC) and N-Hydroxysuccinimide (NHS) to form N-hydroxysuccinimide ester-functionalized paracyclophane. The present invention further provides a chemical film on a substrate and a method of forming the same, wherein the chemical film includes N-hydroxysuccinimide ester-functionalized poly-para-xylylene.

Chemical film on substrate, method of forming the same, and method of forming N-hydroxysuccinimide ester-functionalized paracyclophane

The present invention provides a method of forming N-hydroxysuccinimide ester-functionalized paracyclophane. The present method is carried out by adding 4-carboxyl-paracyclophane into N,N′-Dicyclohexylcarbodiimide (DCC) and N-Hydroxysuccinimide (NHS) to form N-hydroxysuccinimide ester-functionalized paracyclophane. The present invention further provides a chemical film on a substrate and a method of forming the same, wherein the chemical film includes N-hydroxysuccinimide ester-functionalized poly-para-xylylene.

Precursors for Electron Beam-Induced Deposition of Gold and Silver

Precursors are prepared and employed in electron beam induced decomposition (EBID). The EBID precursors are complexes of the formula: X-M-Y, where M is Au or Ag; X is F, Cl, Br, I, CN, OR.sup.1, O.sub.2CR.sup.2, or R.sup.3; Y is P(OR).sub.3, NR.sub.3, unsubstituted or substituted pyrrole, unsubstituted or substituted pyridine, unsubstituted or substituted pyrrolidine, or unsubstituted or substituted piperidine; and where R, R.sup.1, R.sup.2, R.sup.3, and substituents of the substituted pyrrole, pyridine, pyrrolidine, or piperidine are independently H, C.sub.1-C.sub.8 alkyl, C.sub.6-C.sub.10 aryl, C.sub.1-C.sub.8 perfluoroalkyl, C.sub.1-C.sub.8 partially fluorinated alkyl, and SiR.sup.5R.sup.6R.sup.7 where R.sup.5, R.sup.6, and R.sup.7 are independently H, C.sub.1-C.sub.8 alkyl, or C.sub.1-C.sub.8 fluorinated alkyl. The decomposition of the EBID precursor results in the formation of one or more gold, silver, or any combination thereof features on a substrate.

Herbicidally active 2-(substituted-phenyl)-cyclopentane-1,3-dione compounds and derivatives thereof

The present invention relates to a compound of formula (I): wherein the substituents are as defined herein, and wherein the compound of formula (I) is optionally present as an agrochemically acceptable salt thereof. These compounds are thought to be suitable for use as herbicides. The invention therefore also relates to a method of controlling weeds, especially grassy monocotyledonous weeds, in crops of useful plants, comprising applying a compound of formula (I), or a herbicidal composition comprising such a compound, to the plants or to the locus thereof. ##STR00001##

Herbicidally active 2-(substituted-phenyl)-cyclopentane-1,3-dione compounds and derivatives thereof

The present invention relates to a compound of formula (I): wherein the substituents are as defined herein, and wherein the compound of formula (I) is optionally present as an agrochemically acceptable salt thereof. These compounds are thought to be suitable for use as herbicides. The invention therefore also relates to a method of controlling weeds, especially grassy monocotyledonous weeds, in crops of useful plants, comprising applying a compound of formula (I), or a herbicidal composition comprising such a compound, to the plants or to the locus thereof. ##STR00001##