The development of a scalable synthesis for S-MRI1867, a novel dual inhibitor to the CB1R and iNOS

Authors

• J Huang
• A Alimardanov

Abstract

(S)-MRI1867, a novel duel inhibitor to the CB1R and iNOS without brain-penetrant, was discovered as a treatment for Hermansky-Pudlak syndrome (HPS), a rare genetic disease. A scalable route to produce (S)-MRI1867 has been developed that improves from the first generation synthesis and produced hundreds of grams material in 1 single batch to support pre-clinical development activities. The synthesis starts from a commerical availble material, and a novel chiral resolution on key intermediate via crystallization eliminating the previous need for SFC or reversed-phase chromatography to reject undesired enantiomer. A final purification via recrystallization produced (S)-MRI1867 in over 99% purity and 98%ee.

Scientific Focus Area: Research Support Services

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