2-methoxy-2-phenylpropyl phenyl

The preparation of the Step 1 co-reagent, l-(4-aminomethylphenyl)-3-(3-hydroxy-3-phenylpropyl)-4-(4-methoxy-phenyl)azetidin-2-one and other hydroxy-substituted azetidinone derivatives useful in treating hypocholesterolemic diseases is described by Rosenblum (1). 

The reaction between dimethyl 2-bromo-l-phenylpropylidenemalonate and sodium methoxide in methanol affords a complex reaction mixture consisting of dimethyl 2-methyl-3-phenyl-2-cyclopropene-l,l-dicarboxylate (303,19%), dimethyl (2,2-dimethoxy-l-methyl-2-phenylethyl)malonate (304, 4%), dimethyl 2-methoxy-l-phenylpropyl-idenemalonate (305, 11%), dimethyl 2-bromo-l-phenyl-1-propenylmalonate (306 -isomer, 10% Z-isomer, 13%) and dimethyl (l,2-dimethoxy-l-phenylpropyl)malonate... 

The pitfalls that can accompany the development of the amorphous form of a drug substance were shown for the capsule formulation of (3i ,4.Sy)-l,4-bis(4-methoxy-phenyl)-3-(3-phenylpropyl)-2-azetidi-none [17]. A variety of spectroscopic techniques were used to study the amorphous-to-crystalline phase transition, and it was determined that problems encountered with dissolution rates could be related to the amount of crystalline material generated in the formulation. 

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