Arkè Organics is a private company founded in november 2001 by two process chemists with a collective experience of 40 years in the field of organic syntheses.

Our know how ranges from chemical development to the industrial scale production of API s.

Chemical development targeted to IND filing is one of our core competencies. We can grant an integrated project management working with a partner company specialized in analytical development.

Case studies in custom synthesis and process development

Target: Production of 200 g of a drug candidate for toxicology tests, “fixing” the syntetic route

Deadline: 5 months

In the existing route API candidate was obtained in four steps by semisynthesis from a natural compound. The medicinal chemistry route involved a fluorination with HF-pyridine , a coupling with boron trifluoride and a chromatographic purification. No crystalline form was known for the drug candidate and the target obtained in the last step was of variable HPLC grade.

We developed a new synthetic route substituting fluorination with bromination and eliminating boron trifluoride from the coupling step.

Target: developing a validable process for the same API, with a scale up on a 35 L reaction volume.

Dedline: 6 months

A new process research stage was started, with the following results:

1)Elimination of the chromatographic purification of the last intermediate, replaced by a crystallization.

2)New chemistry developed for the last step: drug candidate obtained by crystallization from the reaction mixture, HPLC grade 98-99%, title 98%

3)During the scale-up individuation of a stirring dependant step; we planned for further tests in dynamic similarity conditions to predict reaction behaviour in pilot plant Phase I operations.

Target: production of 40g of a medicinal chemistry intermediate

Deadline: 2 months

The original synthetic route was in 6 steps, with 5 chromatographic purifications and an atmospheric pressure hydrogenation. The alternative route was in 4 steps with no hydrogenation involved and only one chromatographic separation.