Organic Process Research and Development p. 208 - 217 (2017)
Update date:2022-09-26
Topics:
Hansen, Marvin M.
Kallman, Neil J.
Koenig, Thomas M.
Linder, Ryan J.
Richey, Rachel N.
Rizzo, John R.
Ward, Jeffrey A.
Yu, Hannah
Zhang, Tony Y.
Mitchell, David
A practical pilot plant convergent synthesis of MR antagonist LY2623091 was established. For synthesis convergence, a vinyl bromide geometric isomer and chiral alaninol derivative were required building blocks. Key to the synthesis route development is a stereoselective synthesis of the E-vinyl bromide via a sequential double Heck reaction, Suzuki-Miyaura cross-coupling of the vinyl bromide, a selective nitro reduction, and a highly sensitive cyanamide hydrolysis to the urea. Improvements in yield and processing were accomplished by two sets of telescoping methods which decreased the manufacturing time and provided purity enhancements.
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