Available cartridges and reactions
How does Synple work?
Settings up a reaction on Synple 2
Comparison of Synple 1 vs manual synthesis
Available reaction classes
N-Heterocycle formation
- 10 different Heterocycle structures currently available
- Scale: up to 0.5 mmol
Advantages compared to classical batch chemistry are:
- Minimise user exposure to toxic tin reagents
- Multistep reactions completed at the touch of a button
- High reproducibility
What is in the heterocycle formation cartridges:
Reductive Amination
The cartridge contains all reagent for the condensation, reduction and purification steps of the process.
- Scale: up to 0.5 mmol
- Time-saving – reaction, work up and purification in a single process
- Automation of routine chemistry to allow more time for technically demanding reactions
- Generic methods, selected based on reaction partners, minimize need for reaction optimization.
What is in the reductive amination cartridges:
Mitsunobu Reaction
- Scale: up to 0.5 mmol
- Applicable to a range of pronucleophiles (phenols, phthalimides, tosylamides, tosylhydrazones).
- Only 5-10 working time required to obtain Mitsunobu product.
- No tedious removal PPh3O necessary.
What is in the Mitsunobu cartridges:
PROTAC formation
The cartridge contains all reagents for the linking the carbonyl group of a protein binder with the partial PROTAC and components for the purification steps of the process.
- Scale: up to 0.1 mmol
What is in the PROTAC cartridges:
Biotin Tags
Biotin Tags
The cartridge contains all reagents for the linking the compound of choise to a variety of biotin tags and also includes components for a simple purification step.
- Scale: up to 0.1 mmol
What is in the Biotin cartridges:
For Amine-Linker
For Amide-linker
Deoxyfluorination
Deoxyfluorination
Fluorinations are among the most interesting reaction in medicinal chemistry and mostly used for late stage functionalization.
The subgroup of Deoxyfluorination involves the reaction between an alcohol and a fluorinating agent to generate the corresponding fluorinated product.
Using the approach the Synple Chem synthesizer offers an easy and fast automated method for the deoxyfluorination of primary and secondary alcohols without the need of handling fluorinating agents.
- Scale: up to 0.2 mmol
What is in the Fluorination cartridges:
Boc Protection
Boc protection
- Scale: two sizes available; up to 0.5 mmol and up to 1.2 mmol
What is in the Boc protection cartridges:
Boc Deprotection
Boc deprotection
N-Boc deprotection involves the reaction between an N-Boc protected amine and acid (TFA, HCl, TsOH and etc…) to generate the corresponding free amine salt.
Using the approach in this application note, the Synple Chem synthesizer offers an easy and quick automated method for the N-Boc deprotection of primary and secondary amines and avoid the handling of volatile and corrosive acids such as TFA or HCl.
What is in the Boc deprotection cartridges:
Azide formation
Azide formation
Azide formation by diazo transfer of primary amines is a highly important reaction in organic chemistry and chemical biology. Azides have been widely utilized as the key partner in Cu-catalyzed azide-alkyne cycloaddition reactions for bioorthogonal click chemistry, peptide conjugation and polymerization processes. Azides also show good chemical stability so that they can serve as a protecting group for primary amines, in particular in the field of carbohydrate chemistry. Previous methods of converting amines into azides require fresh preparation of diazo transfer agents (not commercially available) using highly hazardous reagents, which has largely limited its broad adoption.
- Scale: up to 0.5 mmol
- Avoid handling azidation reagents
What is in the Azide cartridges:
Amide formation
Amide formation
The amide (carboxamide) group is one of the most important functionalities broadly occurring in small molecules, peptides, proteins and various natural/synthetic polymers. In pharmaceutical industry, amide bond formation covers nearly 25% of the patent reactions, thus presents as the most widely used synthetic method in drug discovery. Amide formation between a carboxylic acid and an amine initated with the pre-activation of the carboxylic acid with a coupling agent to form an active intermediate, such as acyl halides, acid anhydrides and active esters, which undergoes a nucleophilic replacement of the amine to form the amide product. Numerous coupling agents have been developed and become readily available from commercial vendors. Recently, increased concerns over these coupling agents as skin sensitizers prompt research in finding safer alternatives and/or improving existing protocols to meet the upgraded laboratory standards. Using a solid-supported coupling agent for the amide formation has turned into a suitable and welcoming solution in both bath and flow setup for minimizing the exposure of sensitizing chemicals and simplifying the purification of the amide product.
- Scale: up to 0.5 mmol
What is in the Amide cartridges:
Silyl Deprotection
Silyl deprotection
Silyl group deprotection involves the reaction between a silyl protected alcohol and an acid (TFA, HCl, CSA and etc.) or a fluoride (TBAF, HF pyridine and etc.) to generate the corresponding free alcohol. This transformation is a widely used reaction in organic chemistry.
Using the approach in this application note, the Synple Chem synthesizer offers an easy and quick automated method for the silyl deprotection of primary and secondary alcohols and avoid the handling of volatile and corrosive acids such as TFA or HCl or fluorine source as TBAF.
- Scale: up to 0.5 mmol
- Avoid handling volatile and corrosive acids
What is in the Silyl deprotection cartridges:
