Advancing the traceless organic synthesis into Cyclophase Synthesis Cyclover as a lipophilic anchor has the flexibility to install a variety of linkers for specific purposes, useful for a multi-step synthesis process. The installed linker reacts with a target compound to form a Cyclover derivative which can be isolated in a solid form from the reaction mixture by changing the solution composition. Subsequent reaction steps can be carried out by using Cyclover as an anchor which can reproducibly change from a soluble state to a solid state and pure compounds can be routinely obtained in a solid form with little skill and with good certainty.

The development of Cyclover which is soluble in a specific organic solvent but not in others provides a powerful alternative to the insoluble resin beads used in solid-phase synthesis. Therefore, Cyclover can easily extend its use for tactical synthesis of a broad range of structural types of organic compounds in a traceless manner, avoiding the traditional effort in process development to search for purification conditions based on the characteristic properties of a compound synthesized in each of the steps. The target intermediate can be easily precipitated in a batch reactor by adding a miscible solvent which is insoluble for the desired product. The precipitates can then be obtained by filtration, and a simple wash with suitable solvents can remove all reagents used in reactions. This simple process can eliminate the use of silica gel for column chromatography, the purification method normally employed in solution phase synthesis and reduce the consumption of large volume of solvents, resulting in cost saving in production and green practice in environmental protection.

Cyclover aims to offer a universal Cyclophase synthetic process of

(1) dissolving in solution,

(2) reacting to completion,

(3) precipitating for separation and

(4) filtering for collection for making any kind of organic compounds and lead a new revolution in organic synthesis to minimize waste generation and to out-date the use of silica gel column chromatography.

Meeting the challenge of manufacturing peptide and oligonucleotide-based drug therapies

Bio-molecules such as peptide and oligonucleotide therapeutics have been attracting attention as a new drug platform in recent years. Cyclover can be employed in manufacturing peptides and oligonucleotides in a conventional batch reactor, removing the scalability limitation due to the conventional solid phase synthesis. Cyclover makes it possible to perform process analysis directly during the synthesis of the target compound, enabling timely processing. Through stringent process control, the manufacture of active pharmaceutical ingredients, or APIs, can be performed on the order of several tens of kilograms at a time while still ensuring high quality. Being able to synthesize very small to very large quantities of API without changing the production process ensures drug companies a stable supply for clinical trial and eventually therapeutic application.

Developing therapeutics that treat diseases faster

If the manufacturing process differs from clinical testing to pharmaceutical commercialization, extra valuable time must be spent to develop a method suitable for industry scale production and re-evaluate a drug’s safety, which may potentially delay the drug approval. Therefore, identical process is most favorable for drug research and development. Cyclover can facilitate the process development since its simple and robust manufacturing method is feasible to scale up from small quantity synthesis to large scale industrial production using the same production process. While drug development can benefit the health of people around the world, a benign process of drug manufacturing will reduce the amount of reagents and solvents used and maximize the protection of the earth we all live on.

Biotide Core, LLC is deeply committed to working with drug researcher and developer in academia and pharmaceutical companies to innovate the process technology with high quality and high scalability at the very beginning in order to ultimately deliver cutting-edge therapeutics to the people who need.