Granulation of Effervescent Ingredients for Optimization of Gastroretentive Properties of Floating Proroxan Prolonged-Release Tablets

Anti‐Markovnikov Hydroamination and Hydroalkoxylation of Allylic Alcohols Promoted by a Simple Rare‐Earth Metal Trialkyl Complex

“…[24] This protocol could be used for the modification of drugs, which was demonstrated by the synthesis of γ-amino alcohols 44 and 45 via the anti-Markovnikov hydroamination of allyl alcohols in the presence of the Y catalyst. Subsequently, the oxidation led to the formation of β-aminoketones of Propipocaine [25] using as an important local anesthetics, and Proroxan [26] regarding as a nonselective αdrenoblocker (Scheme 2).…”

Recent progress in the chemistry of β-aminoketones

“…5 Also, they are prevalent in native anesthetics such as propipocaine in pharmaceutical synthesis and medical treatment. 6,7 In addition, the incorporation of b-aminoketones in drugs such as amine salts "tolperisone (vasodilation)" and "oxyfedrine (therapeutic coronary disease)", and uoroalkyl derivatives such as "sitagliptin (antidiabetic)". Drugs derived from the b-aminoketone moiety are known to exhibit remarkable biological potency.…”

Metal-free synthesis of β-aminoketones by the reductive hydroamination of ynones

“…4 For instance, proroxan is a nonselective α-drenoblocker with peripheral and central action to treat and prevent hypertonic crises and other types of sympathetic-adrenal pathology. 5 Propipocaine is one of the most popular local anesthetics in pharmaceutical preparations and medical praxis. 6…”