Various aliphatic and aromatic dimethyl and diethyl acetals and ketals were found to hydrolyse in essentially quantitative yield when heated to 80 • C in neat water or aqueous medium without a catalyst or any other additive, while cyclic acetals were stable under these conditions. Selective deprotection is possible when both types of acetal are present.This journal is
A series of pyrrolo [2,3-d]pyrimidines were designed in silico as potential bumped kinase inhibitors targeting P. falciparum calcium dependent protein kinase 4 (PfCDPK4), with the potential to inhibit PfCDPK1 based on earlier studies of the two kinases. A small series of these compounds were prepared and assessed for inhibitory activity against PfCDPK4 and PfCDPK1 in vitro. Four of the compounds displayed promising inhibitory activity against either PfCDPK4 (IC 50 = 0.210-0.530 μM), or PfCDPK1 (IC 50 = 0.589 μM). These data will enable optimisation of the molecular model to better predict inhibitory activity against PfCDPK4.
Da die Ausb. an α‐Amidoalkylaryl‐ketonen des Typs (III) auf dem bekannten Wege über ein durch ein Phenacylbromid N‐substituiertes Alkylamin, wie (II), nur gering sind [wegen der überwiegenden Tendenz zur Bis‐phenacylierung des Amins und der dadurch bedingten schlechten Ausb. schon an (II)], wird die Eignung der von einem Toluolsulfonsäureamid ausgehenden und in einem bestimmten Fall brauchbaren Gabriel‐Methode zur N‐Phenacylierung in einem weiteren Rahmen untersucht.
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