Technology Bundle ID
TAB-3587

Process for Practical, Scalable, Commercially-viable Method for the Synthesis of Enantio-enriched Aminoalcohols, Including the Novel Antifungal VT-1129 Used to Treat Cryptococcal Meningitis

Applications
Linked ID
E-046-2013-0
Lead Inventors
Asaf Alimardanov (NCATS)
Co-Inventors
Christopher Yates (Viamet Pharmaceuticals Inc.)
Douglas Fry (Ricerca Biosciences, LLC)
Mark Behnke (NCATS)
Scott David (Ricerca Biosciences, LLC)
William Hoekstra (Viamet Pharmaceuticals Inc.)
ICs
This technology relates to the discovery and development of a practical, scalable, and commercially viable method for the synthesis of the novel antifungal VT-1129. Cryptococcal meningitis (CM) is a fungal infection that is particularly prevalent in immune-compromised patients and can be treated by VT-1129. CM has a current estimated patient population of 1-1.25 million, predominately in sub-Saharan Africa and the developing world. Several deficiencies and difficulties preclude large-scale preparation and manufacturing with previous processes, which include high cost and potential safety issues. The method described in this invention enables the practical and economical synthesis of VT-1129 at a large scale.
Commercial Applications
The discovery described here can generally be used to prepare enantioenriched aminoalcohols that contain tertiary alcohol fragments, and their derivatives, including the novel antifungal VT-1129 used for treating cryptococcal meningitis.
Competitive Advantages
This discovery has the following advantages over previous synthesis methods: 1) avoids using expensive chiral chromatography for separation and preparation of enantiomerically enriched aminoalcohols and derivatives 2) avoids using expensive chromatographic purification of intermediates 3) avoids using of cryogenic conditions in the process 4) avoids using unstable/explosive reagents 5) allows cost-efficient and scalable preparation applicable to commercial scale manufacturing

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