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Care 2020, 23 (2), 7681

Despite the high overall yield in the described solid phase approach, it has several drawbacks for the scale-up process such as the application of the highly toxic and corrosive hydrogen fluoride for cleavage of the peptide from the resin, low loading (0.300.35 mmol/g of resin) proved necessary for successful on-resin cyclization, and the use of excess amounts of reagents (3-fold of DIC, 2.4-fold of HOBt, etc.) on each step

P., Raad M., Zuckermann R

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