Process development and chiral resolution of LP-184

Through this collaborative research project. the Center for Innovative Drug Discovery (CIDD) will provide Southwest Research Institute (SwRI) with process development support and chiral resolution of the target compound (+)-LP-184. The CIDD will provide all the necessary services. highly experienced/qualified personnel. materials. equipment and the facilities to ensure the requested tasks are completed to meet the milestones and project schedule. The CIDD will receive intermediate 11 from SwRI and will perform process and method development to optimize the syntheses as shown in Scheme 1 in order to provide 1 gram batch of the target compound (+)-9 for the GLP TOX study. The CIDD will investigate and optimize the chemistry method accordingly to complete the synthesis of the final target with purity >96%. Additionally. the CIDD will develop method to perform chiral resolution of the racemic (+/-)-9 in order to provide the enantiomeric pure form (+)-LP-184. Finally. the CIDD will optimize the chemistry on a reasonable scale (200 mg-1 g). provide SWRI a technical transfer package on the optimized route such that the scale-up can be done at SwRI for the GLP tox studies.The CIDD will include full analytical characterization (1H and HPLC/MS) of the final compounds with a delivery sheet and supporting analytical data in accordance to the contract requirement.