1 research outputs found
Route Development and Multikilogram GMP Delivery of a Somatostatin Receptor Antagonist
Route development and demonstration on multikilogram
scale for
the first GMP delivery of MK-4256 are described. Key aspects of the
convergent route include a regioselective green iodination, one-pot
oxadiazole synthesis, and an efficient ketone Pictet–Spengler
reaction with diastereomeric upgrade via crystallization to afford
6 kg of API. A recycle procedure augmented the yield of desired diastereomer
in the Pictet–Spengler reaction from a mixture of diastereomers
heavily enriched in the undesired diastereomer