Parallel Synthesis

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Parallel Synthesis

Overview of Parallel Synthesis

Parallel synthesis enables substantial time savings and compound differentiation by running multiple experiments simultaneously.

Parallel synthesis is used to accelerate the discovery of new compounds and to screen for optimal process conditions. In the pharmaceutical industry, parallel synthesis is used for the discovery and development of potential drug candidates. For example, this enables the synthesis of libraries with diverse chemical structures that can be screened for potential biological activity.

Parallel Synthesis applications run at different scales, including lead generation, lead optimization, and screening for optimal reaction conditions. Thus, in process scale-up and development, parallel synthesis methods speed process optimization by providing a better understanding of the effect of reaction variables including solvent systems, optimal temperatures and concentrations, correct reagents, reaction times, and selection of catalysts.

Parallel Synthesis Services

BioDuro-Sundia offers synthesis and purification services to deliver both small and large libraries, with expertise to overcome discovery stage challenges and capacity for process scale-up of drug substance.

Small libraries

10 – 50mg of each compound

Purity - ≥90% (95% if desired) by HPLC/LC-MS for all compounds

1H-NMR for 5- 10% (or more, if required) of the compounds

Large libraries

10mg of each compound

Purity - ≥85% by (90% if desired) HPLC/LC-MS for all compounds

In general 1H-NMR for 5 - 10% of the compounds

Multi-step preparations of novel library scaffolds

Large collections of standard commercial building blocks (amines, acids, isocyanates, sulfonyl chlorides etc.)

Small libraries (20 - 500 compounds) to allow for rapid SAR exploration

Large libraries (1,000 - 10,000 compounds)

High-throughput or parallel medicinal chemistry for more complex chemistry

Track record of delivering ~88,000 compounds in the library space (small and large libraries)

Capacity to deliver 6,000 compounds/month

Synthesis and Purification Infrastructure

Multiple standard orbital shakers; Multiple shakers with heating/cooling capacity

Parallel inert atmosphere equipment

CEM Discovery Microwave with robot

Large shaking table for large libraries

15 x Parallel synthesizers for small libraries

6 x Purification using automated prep-HPLC and prep-TLC

8 x MPLCs/Combi-Flash

Analytical Support for Parallel Synthesis

Provides both analysis and purification support

Method development

Open-access systems with trained chemists

Purification including chiral separation maintenance of instruments

7 x LC-MS (Agilent 1260/6120)

1 x GC MS

22 x HPLC (Agilent and Shimadzu)

1 x GC

8 x Prep-HPLC (Gilson 281)

8 x Prep-MPLC (Biotage/Agela)

1 x NMR (Bruker-400MHz AVANCEIII): 1D, 2D, 1H, 13C, 19F, 11B, 29Si, 31P

3 x Lyophilizer

Packaging/Shipment

Depending on the project needs, we could adopt the packaging in barcoded vials/ARPs (Assay Ready Plates)

Automated system in place for ARPs in 384 wells formats, if required

Shipment to client in a desired format weekly or bi-weekly basis (or at a desired frequency)

Chemistry

Medicinal Chemistry Parallel Synthesis Peptide Chemistry Computational Chemistry Synthetic Chemistry Analytical Chemistry Scale Up Chemistry

Drug Metabolism and Pharmacokinetics (DMPK)

In Vivo PK and TK In Vitro ADME Bioanalytical Service Toxicity In Rodents, Dogs and Monkeys Large Molecule Development and Bioanalysis

Discovery Biology

Fragment Based Drug Discovery (FBDD) Biochemical Assays Cellular Assays Protein Science Assay Technologies Biophysics SPR Safety Pharmacology Screening Services Key Instruments

Oncology

PDX CDX Orthotopic Models Syngeneic Models Humanized Mouse Models CAR-T and CAR-NK Mouse Models In Vitro Assays

Pharmacology

Immunology Inflammation Metabolic MASH Mouse Models Respiratory Neuroscience

Biologics

Systematic Antibody Discovery Service

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