83881-37-2Relevant academic research and scientific papers
NOVEL WATER BASED PROCESS FOR THE PREPARATION OF SUBSTITUTED DIPHENYLMETHYL PIPERAZINES
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Page/Page column 8, (2011/08/03)
The present invention relates to a novel water based process for the preparation of substituted diphenylmethyl piperazines of Formula I and pharmaceutically acceptable salts wherein X1 and X2 represent independently a hydrogen, a halogen, a straight or branched chain lower alkyl, alkoxy or a hydroxyl radical and R is selected from groups such as acyl, alkyl, alkenyl, aralalkyl, aralalkenyl aralkyl, and aralalkenyl or aralkenyl hydroxyalkyl, aryloxyalkyl, alkoxyalkyl, aminoalkyl or its derivative comprising, reacting a compound of Formula II, with a compound of formula R—X where R is as defined above and X is suitable leaving group which includes halides, but not limiting use of other leaving groups such as tosylate, mesylate and activated acid groups such as acyl halide, anhydrides, mixed anhydrides etc. using water as a solvent, in presence of a catalyst and a base, at 25-100° C.;
A large-scale synthesis of enantiomerically pure cetirizine dihydrochloride using preparative chiral HPLC
Pflum, Derek A.,Wilkinson, H. Scott,Tanoury, Gerald J.,Kessler, Donald W.,Kraus, Hali B.,Senanayake, Chris H.,Wald, Stephen A.
, p. 110 - 115 (2013/09/07)
Enantiomerically pure cetirizine can be prepared by preparative HPLC separation of cetirizine amide. The amide has an α value of 2.76 (USP resolution of 8.54) using a Chiralpak AD column, and 0.5 wt % of the amide (based on packing material) can be injected per run.
Enantiomers of 1-[(4-chlorophenyl)phenylmethyl]-4-[(4-methylphenyl) sulfonyl]piperazine
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, (2008/06/13)
Levorotatory and dextrorotatory enantiomers of 1-[(4-chlorophenyl)phenylmethyl]-4-[(4-methylphenyl)sulfonyl]piperazine of the formula STR1 their preparation and use for the preparation of substantially optically pure enantiomers of 1-[(4-chlorophenyl)phenylmethyl]piperazine, which are themselves valuable intermediate products for the preparation of optically active therapeutic compounds having a very high degree of optical purity.
2-[4-(Diphenylmethyl)-1-piperazinyl]-acetic acids and their amides
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, (2008/06/13)
New 2-[4-(diphenylmethyl)-1-piperazinyl]-acetic acids, their amides and their salts, processes for the preparation thereof and therapeutic compositions. These compounds have the formula STR1 wherein Y=--OH or --NH2 ; X and X'=H, halogen, alkoxy or trifluoromethyl; m=1 or 2 and n=1 or 2. The amides of the 2-[4-(diphenylmethyl)-1-piperazinyl]-acetic acids are prepared either by reacting a 1-(diphenylmethyl)-piperazine with an omegahaloacetamide, or by reacting an alkali metal salt of an omega-[4-(diphenylmethyl)-1-piperazinyl]-alkanol with a 2-haloacetamide, or yet by reacting ammonia with a halide or alkyl ester of a 2-[4-(diphenylmethyl)-1-piperazinyl]-acetic acid, whereas the 2-[4-(diphenylmethyl)-1-piperazinyl]-acetic acids are prepared by hydrolyzing the corresponding amide or lower alkyl ester. These compounds have in particular an antiallergic, spasmolytic and antihistaminic activity.
