1579992-37-2

Upstream product

• 17199-29-0 (S)-Mandelic acid 
• 13704-09-1 (S)-(-)-ethyl mandelate 
• 1579992-43-0 ethyl (S)-4-iodomandelate 
• 1579992-53-2 (1S)-1-(4-((trimethylsilyl)ethynyl)phenyl)ethane-1,2-diol 
• 90842-69-6 (2-(4-iodophenyl)-2-oxoethyl) acetate 
• 31827-94-8 2-bromo-1-(4-iodophenyl)ethanone 
• 160332-70-7 (S)-(+)-1-(4-bromophenyl)-1,2-ethanediol 

Downstream Products

• 1579992-45-2 (S)-2-(4,4'-dimethoxytrityloxy)-1-(4-ethynylphenyl)ethanol 

Relevant academic research and scientific papers

NOVEL METHOD FOR PRODUCING HYDROXAMIC ACID DERIVATIVE, AND INTERMEDIATE THEREFOR

A novel method for production of hydroxamic acid derivative using a compound represented by the formula [12] as an intermediate, and intermediate therefor. wherein R1 represents a methyl group or the like; R2 represents a methyl group or the like; and R5 represents a hydrogen atom or the like.

NOVEL CRYSTALS OF HYDROXAMIC ACID DERIVATIVE, PRODUCTION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION

Crystals of (2S)-2-((4-((4-((1S)-1,2-dihydroxyethyl)phenyl)ethynyl)benzoyl)(methyl)amino)-N-hydroxy-N′,2-dimethylmalonamide having diffraction peaks at diffraction angles (2θ) of 3.8±0.2°, 7.7±0.2°, and 10.8±0.2°, etc., or 8.2±0.2°, 12.4±0.2°, and 13.3±0.2°, etc., in powder X-ray diffraction, a production method thereof, and a pharmaceutical composition.

METHOD FOR USING NOVEL HYDROXAMIC ACID DERIVATIVE AND ANTIBACTERIAL SUBSTANCE IN COMBINATION

Pharmacological compositions containing a hydroxamic acid derivative selected from (2S)-2-((4-((4-((1S)-1,2-dihydroxyethyl)phenyl)ethynyl)benzoyl)(methyl)amino)-N-hydroxy-N',2-dimethylmalonamide, (2S)-2-((4-((4-((1R)-1,2-dihydroxyethyl)phenyl)ethynyl)benzoyl)(methyl)amino)-N-hydroxy-N',2-dimethylmalonamide, and (2S)-N-hydroxy-2-((4-((4-((1S)-1-hydroxy-2-methoxyethyl)phenyl)ethynyl)benzoyl)(methyl)amino)-N',2-dimethylmalonamide, or a salt of said derivatives, and an antibiotic substance are useful in the treatment of gram-negative bacterial infections.

NOVEL PHARMACEUTICAL COMPOSITION CONTAINING HYDROXAMIC ACID DERIVATIVE OR SALT THEREOF

This pharmaceutical composition contains a hydroxamic acid derivative, or a salt thereof, and a solubilizer, said hydroxamic acid derivative being selected from among (2S)-2-((4-((4-((1S)-1,2-dihydroxyethyl)phenyl)ethynyl)benzoyl)(methyl)amino)-N-hydroxy-N',2-dimethylmalonamide, (2S)-2-((4-((4-((1R)-1,2-dihydroxyethyl)phenyl)ethynyl)benzoyl)(methyl)amino)-N-hydroxy-N',2-dimethylmalonamide, and (2S)-N-hydroxy-2-((4-((4-((1S)-1-hydroxy-2-methoxyethyl)phenyl)ethynyl)benzoyl)(methyl)amino)-N',2-dimethylmalonamide. The pharmaceutical composition demonstrates strong antibacterial activity, has excellent solubility in water, and is useful as a drug.

NOVEL HYDROXAMIC ACID DERIVATIVE OR SALT THEREOF

A compound represented by general formula (1) (wherein R1 represents a hydrogen atom, an optionally substituted C1-6 alkyl group or the like; R2 represents a hydrogen atom, an optionally substituted C1-6 alkyl group or the like; R3 represents a hydrogen atom or an optionally substituted C1-6 alkyl group; R4 represents a hydrogen atom, an optionally substituted C1-6 alkyl group or the like; X1 represents an optionally substituted C2-6 alkynylene group or the like; A represents an optionally substituted bivalent aromatic hydrocarbon group or the like; X2 represents an optionally substituted C1-6 alkylene group or the like; Y1 represents an oxygen atom or the like; and R5 represents a hydrogen atom or the like) or a salt thereof is useful as an antibacterial agent.

Synthesis of ethynylbenzene-substituted glycol as a versatile probe for labeling oligonucleotides

Positron emission tomography (PET) is a highly sensitive quantitative imaging technique for studying molecular pathways and interactions in vivo. This imaging technique plays a key role in drug discovery, pharmacokinetics, pharmacodynamics, and assessing in vivo distribution. In this study, we designed an ethynylbenzene-substituted glycol (ME) as a versatile probe for PET labeling of oligonucleotides through a click reaction.