NARD Institute technical keywords

Compound Library Synthesis Service

We provide small samples of many chemicals derived from a base structure.

Based on existing procedures, we will draw from our experience to propose a process suitable for multi-sample synthesis, working consistently from synthetic design to production and purification.

As we tailor sample shipments to the customers' needs, your sample will arrive in a state appropriate for your planned experiments.

Disclosure of candidate compounds (candidate optimization)

Disclosure of candidate compounds (candidate optimization)

By proposing efficient parallel synthesis processes, we work to accelerate synthesis.

  • Compound library synthetic process proposal
  • Synthesis
  • Purification
  • Quality assurance
  • Delivery

From ordinary organic synthesis to a multi-sample synthetic process

Conduct studies of parallel liquid-phase synthesis, solid-state synthesis, purification methods, and synthetic route proposals

Library Synthesis

Proceed with production in accordance with the optimized synthetic process

Library Purification

Improve product quality by purification with liquid-phase preparatory equipment, solid-phase reagents, MS-triggered chromatography systems, etc.

Quality Control

Structural and purity analyses are carried out with LC/MS, NMR, HPLC, etc.The sample will be delivered in accordance with your request.

Library Synthesis, Example 1

Library Synthesis, Example 1-1
Library Synthesis, Example 1-2

Library Synthesis, Example 2

Suzuki coupling Buchwald amination Heck reaction Stille coupling
Sonogashira reaction Ullmann reaction Negishi coupling Mitsunobu reaction
Mannich reaction Wittig reaction HWE reaction Grignard reaction
Gabriel synthesis Jones Oxidation Michael Addition Simmons-Smith
cyclopropanation
Williamson
Ether synthesis
Heterocyclic
synthesis
Pd/C H2 NaBH4 reduction
LiAlH4reduction Condensation
reagent
etc …

Results of an FTE contract based library synthesis

Short term contract (1–2 projects)

·Synthesis of 100–400 compounds in one month (synthetic process study included)

  • Project A
    100–400 compounds
  • Precursor synthesis
  • Library synthesis
Long-term contract (multiple projects)

·Synthesis of 150–400 compounds every month (synthetic process study included)

  • Project A
    50 compound
  • Precursor synthesis
  • Library synthesis
  • Project B
    50 compound
  •  
  • Precursor synthesis
  • Library synthesis
  • Project C
    50 compound
  •  
  •  
  • Precursor synthesis
  • Library synthesis

Procedure for FFS contracts

  • Library synthesis
    Preliminary study
  • Library synthesis
  • LC-MS isolation
    Purification
  • QC(LC-MS)
Basic conditions for isolation and analysis
Column
YMC Triat C18, 5μm 4.6mm×50mm
Method
Flow rate: 2 ml / min
Temperature: ambient
Gradient conditions
Min 0.1% TFA
in H2O
CH3CN
0 95 5
0.5 95 5
3 5 95
5 5 95
Column
YMC-Actus Triat C18, 5μm 150mm×30mm
Method
Flow rate: 60 ml / min
Temperature: ambient
Gradient conditions
Min 0.1% TFA
in H2O
CH3CN
0 95 5
1 95 5
11 20 80
12 5 95

Unique building blocks

Over 4000 varieties of aminocarboxylates
(oxetanes, spiro compounds, tertiary carbon, organofluorines)

Optimization of lead (hit) compounds

By using our unique building blocks we realize optimization of compounds.

Search for hit compounds

We synthesize from a virtual library (over 900,000 compounds) constructed from our unique building blocks.

Unique building blocks

Optimization of lead (hit) compounds
Optimization of lead (hit) compounds
Search for hit compounds
Search for hit compounds

Library synthesis 'in silico'

Library synthesis 'in silico'

Fragment activity assessment with 19F-NMR (joint research)

Library synthesis 'in silico'

Main equipment for parallel synthesis

Reactors and equipments for parallel synthesis.
Parallel synthesis equipment 13 x 20 ml (-78–150℃)
6 x 150 ml (-78–150℃)
Parallel synthesis equipment 50 x 20 ml (0–150℃)
Parallel synthesis equipment 96 x 2 ml
Parallel solvent removal equipment (rotary, air dry)  
Parallel dispensing technology  
Purification
Automatic preparative column chromatography (silica, amine, ODS, etc.)
MS-triggered automatic preparative chromatography system x2
Solid-state reaction purification techniques
Analysis
NMR (400 MHz)
High-throughput HPLC (PDA, UV)
High-throughput HPLC (PDA, UV)
There are many more examples of our achievements and capabilities. Please feel free to inquire.
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