ORGN 237 |
| The process development of the cholecystokinin (CCK2) receptor ligand 1 is described with the emphasis on the scale-up modifications needed to manufacture kilogram quantities of crystalline material. The modifications include (a) the use of 2-chloro-1-cyclopentylethanone as the alkylating agent rather than the less stable bromo-analog, (b) the use of thionyl chloride/acetonitrile to introduce the amide linkage, and (c) the selection of the choline salt. Moreover a cost efficient synthesis of a key intermediate will be disclosed. This synthesis is based on a highly regio-selective addition of an aryl isocyanate to a substituted hydrazine.
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Combinatorial and Process Chemistry
8:00 AM-11:40 AM, Monday, March 26, 2007 McCormick Place East -- Room E350, Level 3, Oral
Division of Organic Chemistry |
