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Accelerated Multiphosphorylated Peptide Synthesis
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2022-07-12 , DOI: 10.1021/acs.oprd.2c00164 Dana Grunhaus 1 , Estefanía Rossich Molina 1 , Roni Cohen 1 , Tamar Stein 1 , Assaf Friedler 1 , Mattan Hurevich 1
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2022-07-12 , DOI: 10.1021/acs.oprd.2c00164 Dana Grunhaus 1 , Estefanía Rossich Molina 1 , Roni Cohen 1 , Tamar Stein 1 , Assaf Friedler 1 , Mattan Hurevich 1
Affiliation
Preparing phosphorylated peptides with multiple adjacent phosphorylations is synthetically difficult, leads to β-elimination, results in low yields, and is extremely slow. We combined synthetic chemical methodologies with computational studies and engineering approaches to develop a strategy that takes advantage of fast stirring, high temperature, and a very low concentration of 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) to produce multiphosphorylated peptides at an extremely rapid time and high purity.
中文翻译:
加速多磷酸化肽合成
制备具有多个相邻磷酸化的磷酸化肽在合成上是困难的,会导致 β-消除,导致产量低,而且速度极慢。我们将合成化学方法与计算研究和工程方法相结合,开发了一种利用快速搅拌、高温和极低浓度的 1,8-二氮杂双环[5.4.0]undec-7-ene (DBU) 的策略以极快的速度和高纯度生产多磷酸化肽。
更新日期:2022-07-12
中文翻译:
加速多磷酸化肽合成
制备具有多个相邻磷酸化的磷酸化肽在合成上是困难的,会导致 β-消除,导致产量低,而且速度极慢。我们将合成化学方法与计算研究和工程方法相结合,开发了一种利用快速搅拌、高温和极低浓度的 1,8-二氮杂双环[5.4.0]undec-7-ene (DBU) 的策略以极快的速度和高纯度生产多磷酸化肽。